ALBERT-PULEO,M
The Obstetrical Use in Ancient and Early Modern Times of Convolvulus Scammonia Or Scammony: Another Non-fungal Source of Ergot Alkaloids.
J Ethnopharmacol 1 2: 193-195 (1979) English
ANLEZARK, GILL; MELDRUM, BRIAN
Blockade of photically induced epilepsy by 'dopamine agonist' ergot alkaloids.
Psychopharmacology; 1978 Vol 57(1) 57-62
Studied the effect of iv administration of ergot alkaloids on epileptic responses to intermittent photic stimulation (IPS) in adolescent Senegalese baboons ( Papio papio ). Ergocornine, (1-2 mg/kg) produced marked autonomic and behavioral effects, slowed the EEG, and abolished myoclonic responses to IPS for 30-90 min. Ergometrine (1 mg/kg) activated the EEG and blocked the induction of myoclonic responses for 1-3 hrs. Bromocriptine (0.5-4 mg/kg) did not consistently prevent myoclonic responses to IPS. After pretreatment with a subconvulsant dose of allylglycine (180-200 mg/kg), LSD (0.1 mg/kg) retained the capacity to block myoclonic responses to IPS, and ergocornine (1 mg/kg) reduced such responses. The convulsant effect of allylglycine was enhanced, however, so that prolonged seizure sequences began 19-96 min after ergocornine administration. The protective action of ergot alkaloids against epileptic responses induced by sensory stimulation is interpreted in terms of effects at several sites, including dopaminergic and serotoninergic synapses.
Bacon, Charles W.
Procedure for isolating the endophyte from tall fescue and screening isolates for ergot alkaloids
Applied and Environmental Microbiology v54 p2615-18 November 1988
SUBJECTS: Ergot Fescue Alkaloids Acremonium
BARNETT PS; DAWSON JM; BUTLER J; COSKERAN PB; MACCABE JJ; MCGREGOR AM
CV205-502, a new non-ergot dopamine agonist, reduces prolactinoma size in man.
Clin Endocrinol Oxf. 1990 Aug; 33(2): 307-16
Seven patients with large prolactin-secreting pituitary adenomas were treated for 8 weeks with once-daily doses of the new, potent, non-ergot, long-acting dopamine agonist CV205-502. In five patients previous treatment with bromocriptine had failed to control their disease or been poorly tolerated and had therefore ceased. In all seven patients serum prolactin levels fell over the 8-week period of CV205-502 treatment with the decrease ranging from 33 to 99%. Associated with this decline in prolactin all patients showed symptomatic improvement with two of the five women beginning to menstruate and the two patients with visual field impairment showing marked improvement. Tolerance of the drug, with doses at 8 weeks ranging from 0.075 to 0.3 mg, was excellent with only minimal and transient side-effects being noted in three patients in none of whom was discontinuation of therapy necessary. In one patient noncompliance after 6 weeks of therapy was associated with a rapid return of her serum prolactin towards pretreatment levels. In all seven patients the clinical and biochemical improvement was accompanied by a marked reduction in tumour size.
Barnett PS; Palazidou E; Miell JP; Coskeran PB; Butler J; Dawson JM; Maccabe J; McGregor AM.
Endocrine function, psychiatric and clinical consequences in patients with macroprolactinomas after long-term treatment with the new non-ergot dopamine agonist CV205-502.
Q J Med 81(295): p891-906, Nov 1991.
Topic: Bromocriptine, prosexual substances, nootropics
BENKER G; JASPERS C; HAUSLER G; REINWEIN D
Control of prolactin secretion.
Klin Wochenschr. 1990 Dec 4; 68(23): 1157-67
1. Prolactin is a 21,500 Dalton single-chain polypeptide hormone but may occur in 50 kDa and 150 kDa molecular variants. 2. These large PRL variants may be secreted predominantly; this condition is termed 'macroprolactinemia'. It is characterized by high immunological and normal biological serum levels of prolactin, and lack of clinical symptoms of hyperprolactinemia. 3. The information on PRL is encoded on chromosome 6. Transcription can be enhanced and suppressed by a variety of hormonal factors. 4. PRL is secreted in a pulsatile fashion; it displays a circadian rhythm (with a maximum during sleep) and is stimulated by some amino acids. PRL also responds to mechanical stimulation of the breast. 5. PRL rises during pregnancy, and maintainance of hyperprolactinemia (and, thereby, physiological infertility) is dependent on the frequency and duration of breast feedings. 6. Hypothalamic regulation of prolactin mainly involves tonic inhibition via portal dopamine. The physiological importance of various stimulating factors present in the hypothalamus is still incompletely understood. In particular, there is still no place for TRH in PRL physiology. 7. PRL is released in response to stress; this response may be mediated by opioids. The low-estrogen, low-gonadotropin amenorrhea of endurance-training women is not mediated by prolactin, however. 8. Estrogens stimulate PRL gene transcription via at least two independent mechanisms. There are many clinical examples of this estrogen effect on prolactin serum levels, and also on the growth of prolactinomas. 9. Mild hyperprolactinemia remains an enigma which cannot satisfactorily be resolved by biochemical or radiological testing. The border between 'normal' and 'elevated' prolactin is ill-defined. The possibility of macroprolactinemia complicates this matter even further. 10. The number of drugs which suppress prolactin by acting on pituitary D2 receptors, and which are useful in the treatment of hyperprolactinemia, continues to increase. In the field of ergot alkaloids, parenteral application appears to be a logical solution to the problem of the high first-pass effect; in addition, this form of treatment is frequently better tolerated than the oral route. 11. Prolactinoma development is presently being studied employing molecular biological techniques; the question of whether tumorigenesis can be attributed to specific defects of gene regulation remains to be answered.
BENNET JW; LASURE LL
Gene Manipulation in Fungi
Gene Manipulation in Fungi. pg 368-404 ISBN 0-12-088641-3 QK682.946 (1985)
There is accumulating evidence for the widespread occurrence of plasmids or plasmidlike DNA species in eukaryotes, including fungi. Plasmids are present as both linear and cyclic DNA strands. Genera in which plasmids have been found include Claviceps, Neurospora, Aspergillus, Podospora, Dictostelium, Saccharomyces, Ascolobus, Cephalosporum, Gaumannomyces, Kluveromyces, Morchella [an ascomycete mushroom], Pichia, Rhizoctonia, Schizosaccharomyces & Torulopsis. Fungal plasmids may be associated with either mitochondrial and nuclear DNA, and range in size from 1.2 kilobases to 21 kilobases, with the majority occuring in the range of 5-7 kilobases. A strain improvement program with the mold Penicillium notatum has employed monospore selection and mutagenesis with ultraviolet light, nitrous acid, and monoiodoacetic acid. Irradiation has successfully generated more potent strains with a 40% increase yeild of erythorbic acid from glucose (Takahashi, 1969)... Tryptophan ... has been produced with a strain of Hansenula anomala resistant to high levels of anthranilic acid (Terui, 1973) which produces up to 6 grams of tryptophan per liter from the added precursor, anthranilic acid (Terui & Niizu, 1969), and as much as 14 grams per liter from indole (Ebihara et al, 1969). Indole-resistant producing strains have also been isolated. General control of amino acid biosynthesis appears to operate in this yeast since starvation of methionine or histidine mutants for the respective amino acid also elevates tryptophan excretion (Enatsu, et al 1963). They tryptophan-hyperproducing strains all have lower anthranilic acid and tryptophan degrading activity and show altered repression and feedback inhibition by tryptophan. Attempts to improve available strains by crossing haploids have failed (Terui, 1975). The production of indole or anthranilic acid has been reported in Claviceps purpurea (Malin and Westhead, 1959) and numerous strains of yeasts (Nickerson & Brown, 1965; Hutter, 1973). However these processes are not commercially practical.
Bove, Frank James.
The Story of Ergot.
Basel & New York: S. Karger. (1970)
Brauer, Karen L.; Robbers, James E.
Induced parasexual processes in Claviceps sp. strain S1958
Applied and Environmental Microbiology v53 p70-3 January 1987
SUBJECTS: Fungi, Sex in Ergot
BURIAN, ERNEST
An ergot alkaloid preparation (Hydergine) in the treatment of presenile brain atrophy (Alzheimer's disease): Case report.
Journal of the American Geriatrics Society; 1974 Mar Vol. 22(3) 126-128
Administered 1 mg Hydergine 3 times/day for 90 days to 4 patients with presenile brain atrophy (Alzheimer's disease). 2 Ss did not improve, 1 showed moderate improvement, and 1 S-a 62-year-old man who had become a total nursing-care problem-improved dramatically. His case is described in detail. It is concluded that the improvement and the absence of side effects justify further trials of Hydergine in presenile brain atrophy.
BURNETT JH
Mycogenetics. Mutagenic Agents (Chapter)
Mycogenetics; an introduction to the general genetics of fungi. p32 ISBN 0-471-12551-1 QK602.B87
Spontaneous mutants occur in most cases with low frequency. Tatum and others (1950) tested Neurospora [a mold] for a wide range of auxotrophic mutants and found only 1 in 3000 cultures tested, i.e., only one mutant gene from all the thousands tested. In tests for mutations at specific loci the frequency is equally low ... 3/10^6 oidia (3 mutants per million) from methionine-requiring met-8 to wild-type, met-8+ in the mushroom Coprinus lagopus (Moore, 1969). Mutation-inducing agents: 245nm UV irradiation, ethylmethane sulphonate (EMS), and N-methyl-N-nitrosoguanidine (NG) are effective mutagens in the mushroom Coprinus lagopus. It should be realized that no two fungi necessarily respond alike to the same mutagenic agencies, nor indeed in the same way as do other organisms. For example, NG is a most potent chemical mutagen for E. coli [a bacterium] and quite effective with Saccharomyces cerevisiae [brewer's yeast] but it is no more effective with Coprinus lagopus than UV irradiation. It is necessary, therefore, to experiment with different mutagenic agents if work with any fungus not hitherto studied is contemplated. It is usually found with all mutagens that an effective yield of mutants is only achieved when the proportion of survivors from the material exposed is very low, say 5%-1% or less. Large numbers of spores or nuclei, therefore, must be exposed to obtain a worthwhile yield. In the case of the mushroom Agaricus bisporus the mycelium is macerated in a blender to give fragments of, preferably, 2-4 cells in length and these are then treated with the mutagenic agent (Raper & Miles, 1958; Raper, Raper & Miller, 1972) (see also: Day & Anderson, 1961). Nitrous acid, which deaminates nucleotides, substituting hydroxyl groups for the amino groups and thus altering base-pairing in DNA, is one of the most effective chemical mutagens. It is an unstable compound prepared by dissolving sodium nitrite at a pH of 4.6.
D'IAKOV NK
Sochetannoe primenenie metodov detoksikatsii v kompleksnom lechenii ostrykh otravlenii u detei. [Combined use of detoxification methods in the complex treatment of acute poisoning in children]
Vestn Khir. 1990 Oct; 145(10): 79-80
Dihydroergocristine (DHEC) and dihydroergotamine (DHE) were investigated on canine saphenous veins in vivo and on canine saphenous veins and basilar arteries in vitro. Following local i.v. infusion in vivo, the venoconstrictor response to DHEC was about 30% weaker than that produced by DHE. When administered orally, however, both ergot alkaloids elicited similar venoconstrictor effects. In vitro maximal contractile responses to DHEC and DHE of basilar arteries were only 20-30% of those produced by 5-HT, whereas in saphenous veins both DHEC and DHE elicited similar maximal effects as those observed with 5-HT. In saphenous veins, methiothepin antagonized venoconstrictor responses to 5-HT, DHEC, and DHE within the same concentration range, being significantly less potent when tested against noradrenaline. The reverse was true for yohimbine, which was significantly more potent against noradrenaline than against 5-HT, DHEC, and DHE. It is suggested that the venoconstrictor responses to both DHEC and DHE are mediated through 5-HT1-like receptors.
DAVIS, VIRGINIA E
Neuroamine-derived alkaloids: A possible common denominator in alcoholism and related drug dependencies.
Annals of the New York Academy of Sciences; 1973 Apr Vol. 215 111-115
Assigned 40 random-bred golden hamsters to groups receiving 0, 2, 6, or 10 mg/kg of agroclavine, a nonpeptide ergot alkaloid. The 2 highest dosage levels severely retarded avoidance learning, whereas the 2 mg/kg group showed no decrement in learning. Gnawing was prevalent in the 6 and 10 mg/kg groups. Findings are compared with those obtained with LSD.
DELAY J, PICHOT P
Diethylamide de l'acide d-lysergique et troubles psychiques de l'ergotisme. (LSD and psychic disorders in ergotism)
C.r. Soc. Biol. 145,1609 (1951)
The authors observed after 20-50 mcg. LSD euphoria with compulsive laughter, depression, mental disorders and even slight states of confusion. In some cases, there were visual illusions, hallucinations resembling those caused by mescaline, disorders of synaesthesia and posture sense. The authors find a [superficial] similarity between the effects of LSD and the psychic symptoms observed in epidemics of ergotism.
DUBINI F; BIGNAMI P; ZANOTTI A; COPPI G
Mutagenicity studies on dihydroergocristine.
Drugs Exp Clin Res. 1990; 16(6): 255-61
Dihydroergocristine (DHEC) is an ergot derivative used for the therapy of patients with cerebrovascular insufficiency. It was tested for mutagenicity by means of four tests. In the mutagenicity in vitro assay on Salmonella typhimurium, DHEC was checked at 10,000 micrograms/plate on TA98 and TA1538 strains and at 3000 micrograms/plate on TA1535, TA1537 and TA100 strains with and without metabolic activation. In a quantitative in vitro test for mutagenicity in V79 Chinese hamster cells, DHEC was studied at concentrations between 30 and 0.3 microgram/ml with and without metabolic activation. DHEC was tested for its ability to induce chromosomal damage in human lymphocyte cultures utilizing the concentrations of 10, 3 and 1 microgram/ml. In the in vivo mouse (Swiss strain) micronucleus assay, DHEC was orally administered at two dosages (50% and 16% of LD50) following the schedule of the test. Dihydroergocristine is a drug free of mutagenic activity on the basis of all the results obtained from the above in vitro and in vivo tests.
DUNFORD, MARTIN; HOLLAND, JACK
Smoking.
THE REAL GUIDE - AMSTERDAM (The Guide for the '90s; Prentice Hall Travel
('SMOKING' COFFEE HOUSES) BASJOE: Kloveniersburgal 62. Dark and convivial coffee shop. BIBA: HAZANSTRAAT 15. iN A STREET OF COFFEE SHOPS, THIS IS ONE OF THE BEST. BON AMI: Brouwersgracht 137. Very loud music. THE BULLDOG: Leidseplein 13-17; O.Z. Voorburgwal 90; O.Z. Voorburgwal 132 Helkveld 7. The biggest and most famous of the coffee-shop chains, this has come a long way from its pokey Red Light district-dive origins. With a main branch housed in the former police station on glitzy Leidseplein (the 'Palace'), the Bulldog has now reached the height of - and commerical success. The dope they sell comes in neat little brand-labeled packets and the Leidsplein branch has a large cocktail bar, coffee shop, juice bar, souvenir shop, and a GVB ticket counter. EXTASE: Oude Hoogstraat 2. Part of a chain run by the initiator of the Hash Info Museum. Considerably less chichi than the big cheeses. FAIRY NUFF: 2e Laurierdwarstraat 1b. Small and quiet, with a low-key atmosphere. FANCY FREE, Martelaarsgracht 4; Haarlemmerstraat 64; Leliegracht 6. Slick plush, and commerical, very much in The Bulldog mold. GOA, Kloveniersburgwal 42. A member of the Extase chain (see above) GRAND PRIX, Reguliersdwarsstraat 29. Once part of the Prix d'Ami outfit, and little changed since. GRASSHOPPER, N.Z. Voorburgwal 59. One of the city's more welcoming 'smoking' coffee shops, though at times overwhelmed by tourists. HAUSSMANN, Singel 485; Zieseniskade 2. White, modernistic coffee shop with more than a hint of soulessness PIE IN THE SKY, 2e Laurierdwarsstraat 64. Beautiful canal-corner setting, great for outside summer lodging PRIX D'AMI, Haringpakkersteeg 3; Nieuwendijk 239. Super-entrepreneurial Amsterdam chain, but with little of the character of its rivals. ROMA, O.Z. Achterburgwal 162. Red Light district smoker, par of the Extase/Goa concern. RUSLAND, Rusland 16. One of the first Amsterdam coffee shops, and a cramped and vibrant place that's a favorite with both dope fans and tea addicts (43 different kinds). A little worse for the recent extension, but still a cut above the rest. SIBERIE, Brouwersgracht 11. Set up by the former staff of Rusland and notable for the way it has avoided the over-commercialization of the large chains. Very relaxed, very friendly, and worth a visit whether you want to smoke or not. SO FINE, Prinsengracht 30. Long-established, coffee shop, big on atmosphere at night with good food and music. a pool table, and a video room.
DURANTEAU L; CHANSON P; LAVOINNE A; HORLAIT S; LUBETZKI J; KUHN JM
Effect of the new dopaminergic agonist CV 205-502 on plasma prolactin levels and tumour size in bromocriptine-resistant prolactinomas.
Clin Endocrinol Oxf. 1991 Jan; 34(1): 25-9
Bromocriptine is currently and successfully used for the treatment of pituitary prolactinomas. However, bromocriptine appears unable to normalize plasma prolactin levels in about 10% and to reduce tumour size in one-third of cases. The lack of normalization of plasma prolactin levels in spite of a daily dose of bromocriptine equal to or higher than 15 mg suggests a bromocriptine resistance. We compared the long-term effects of bromocriptine and CV 205-502 (a non-ergot derivative D2 dopamine agonist) on plasma prolactin levels and tumour size in seven bromocriptine-resistant prolactinomas. Bromocriptine reduced significantly (P less than 0.001) plasma prolactin levels (from 2307 +/- 518 to 568 +/- 279 micrograms/l) (conversion to Sl units: 1 microgram/l = 20 mU/l). Visual field defects observed in five patients improved in four. However, CT scan analysis showed a decrease in tumour size in only three patients. Except for transient and minor side-effects at the beginning of the treatment, CV 205-502 was well tolerated in five of seven patients. In the remaining two patients nausea and vertigo occurred with high dosages of CV 205-502 and it was necessary to reduce the daily dose. CV 205-502 lowered plasma prolactin to levels similar to those obtained after bromocriptine therapy in four cases. In the three remaining patients, CV 205-502 was more potent than bromocriptine as demonstrated by the further 90% reduction in plasma levels obtained in one case and by the normalization of plasma prolactin levels in the two other cases. One woman became pregnant during CV 205-502 treatment. ...
ELKIND AH
Drug abuse and headache.
Med Clin North Am. 1991 May; 75(3): 717-32
Substance abuse has been reported frequently in chronic headache patients. The problem exists in most Western countries. Abuse of various compounds frequently leads to a state of dependency. Prescription as well as over-the-counter agents are often abused. Aspirin, acetaminophen, and caffeine are the most frequently abused compounds. Butalbital, ergot alkaloids, NSAIDS, and narcotic and oral or intranasal sympathomimetics are often abused. Patients with chronic daily headache complain of symptoms that may suggest a mixed-type headache. Features of migraine and muscle contraction headache often coexist in these individuals. It has been suggested that the most frequent cause for the transformation of a periodic headache into a daily headache is substance abuse. Substance abuse and drug dependency have multiple causes, and the etiology will reside with the compounds that are used to excess. The problem may arise as a result of poor instructions from the physician, improper diagnosis with gradual escalation in amounts of drug consumed, or a reinforcement mechanism and a brain stimulation-reward effect. The brain reward system has been studied with narcotics and psychomotor stimulants. It may be activated to a lesser degree with ergotamine, barbiturates, and other abused substances. The long-term effects of substance abuse are contingent on the compounds that are used. They may result in organ damage, medical complications, vascular injury, and a refractory state with chronic headache that eludes successful management of the headache disorder. Patients exhibit a less-than-satisfactory quality of life and are often depressed. Treatment includes outpatient care in cooperative, less dependent patients. Often patients will require inpatient management in order to discontinue use of the abused agents. Pharmacologic agents, behavior modification, psychotherapy, dietary intervention, and acupuncture may be necessary to treat the patient. Each patient must be treated by an interested physician, and the patient will require one or more of the preceding measures for a successful outcome. Often abused compounds must be discontinued in order to obtain a satisfactory response in an individual with chronic headache.
FENIUK W; HUMPHREY PP; PERREN MJ; CONNOR HE; WHALLEY ET
Rationale for the use of 5-HT1-like agonists in the treatment of migraine.
J Neurol. 1991; 238 Suppl 1: S57-61
Migraine headache is thought to be associated with a dilatation of cranial blood vessels, particularly those in the dura mater, and an accompanying localized sterile inflammatory response. Sumatriptan is a highly selective 5-HT1-like receptor agonist which selectively constricts cranial blood vessels (including those in the dura mater). It also inhibits neurogenically-mediated plasma protein extravasation in the dura mater. Haemodynamic studies in anaesthetized animals have shown that sumatriptan selectively constricts the carotid arterial circulation and this effect appears to be restricted to an effect on carotid arteriovenous anastomoses. Sumatriptan has a much more selective pharmacological profile than ergot preparations which are also used in the acute treatment of migraine. The development of sumatriptan has been based on a vascular theory of migraine and its high degree of efficacy in the treatment of migraine strengthens the argument that dilatation of cranial blood vessels is the cause of vascular headache.
Geronimus, Lippman H., Abramson, Harold A., & Ingraham, Laura J
Lysergic Acid Diethylamide (LSD-25): XXIII. Comparative Effects of LSD-25 and Related Ergot Drugs on Brain Tissue Respiration and on Human Behavior.
J. Psychol. 42:157-168. (1956)
GOMEZ, EVARISTO
Clinical observations in the treatment of tardive dyskinesia with dihydrogenated ergot alkaloids (Hydergine): Preliminary findings.
Psychiatric Journal of the University of Ottawa; 1977 Jul Vol 2(2) 67-71
Presents a preliminary clinical report of observations in 10 patients who were suffering from schizophrenia of long standing, concomitantly with cerebral arteriosclerosis and tardive dyskinesia, and who were given dihydrogenated ergot alkaloids (Hydergine). The dyskinetic movements of 7 patients disappeared after 2-4 wks. Follow-up of these patients for up to 8 mo showed them to be free from tardive dyskinesia. Some hypotheses for the mechanisms of action of Hydergine in these patients are presented.
GRINSPOON, LESTER; BAKALAR, JAMES B
Purity of street LSD
'Psychedelic Drugs Reconsidered'; 1979
According to data compiled by the PharmChem Research Foundation, a California organization, the only psychedelic drugs now generally available on the street are LSD, PCP, and to a lesser extent MDA. Almost no one takes the trouble to manufacture mescaline or psilocybin, because their effects resemble those of LSD and the much larger amounts required make the expense too great. Mescaline is available only in the form of peyote buttons and psilocybin only in the form of psychedelic mushrooms, which have been discovered growing all over the United States; they are increasingly sought after in the wild (see Pollock 1975 a; Weil 1977 a) and, with difficulty, can also be cultivated (see Oss and Oeric 1976). (Many 'psilocybin mushrooms,' incidentally, are just commercial mushrooms laced with LSD.) Anything labeled as pure or synthetic mescaline, psilocybin, or THC is almost certainly either LSD or PCP, or else contains no drug. Some chemicals closely related to LSD have been synthesized to sidestep the law; the one most often available is the acetylated variant, ALD-52, which is almost as potent as LSD itself. As for the quality of illicit LSD, adulterants and substitutes must be distinguished from products of improper synthesis. Since the variable physical and psychological effects of LSD sometimes resemble those of strychnine, belladonna, or amphetamine, there are rumors that illicit LSD often contains these substances. But laboratory analysis, especially the work of PharmChem Research Foundation, shows that illicit LSD rarely contains adulterants, although the advertised dose is usually two to five times the actual one. The major problem is imputities that are by-products of careless or inadequate synthesis. In the manufacturing process, ergotamine or other ergot alkaloids are reduced to lysergic acid (d-lysergic acid monohydrate), which is then converted to LSD. The whole procedure, and especially the last stage, in which LSD is separated from iso-LSD by chromatography, is rather delicate; it requires skill and good equipment. The government has tried to cut off the supply of chemical precursors; but illicit chemists are usually able to obtain enough, because several ergot derivatives are used as medicines and the quantities needed are small: by on estimate, 70 kg of ergotamine tartrate is enough to supply the American LSD market for a year (McGlothlin 1974 b). The only impurity regularly found by the PharmChem Laboratory, aside from occasional traces of ergotamine, is iso-LSD: it is very similar to LSD in chemical structure (the same atoms in a slightly different arrangement) but pharmacologically inactive. It is rarely present in a proportion of more than 15 percent and appears to have no effect on the drug action. So street LSD seems to be reasonably pure.
Harrington, Peter J.; Hegedus, Louis S.
Palladium-catalyzed reactions in the synthesis of 3- and 4-substituted indoles. Approaches to ergot alkaloids
The Journal of Organic Chemistry v49 p2657-62 July 27 1984
SUBJECTS: Indoles/Synthesis Ergot
HOELDTKE RD; DAVIS KM
The orthostatic tachycardia syndrome: evaluation of autonomic function and treatment with octreotide and ergot alkaloids.
J Clin Endocrinol Metab. 1991 Jul; 73(1): 132-9
Orthostatic tachycardia is a poorly understood syndrome in which patients develop dizziness, diaphoresis, or palpitations upon shifting from the supine to the upright posture. The present study was performed to determine whether autonomic neuropathy might be present in these patients, and whether the abnormal hemodynamic response to standing might be the result of failure of reflex vasoconstriction. We measured autonomic function in 9 patients with idiopathic orthostatic tachycardia and 2 patients with orthostatic tachycardia and insulin-dependent diabetes mellitus and compared them to 33 age-matched controls. Although most patients with orthostatic tachycardia had normal vasomotor reflexes and normal surface potential amplitudes, the latency of the autonomic response, a measure of sympathetic nerve conduction velocity, was prolonged in the soles (2.44 +/- 0.08 s in patients with idiopathic orthostatic tachycardia vs. 2.12 +/- 0.04 s in controls; P less than 0.005). In 6 of 9 patients, however, the latencies were within the normal range. Autonomic surface potentials were absent in 1 diabetic patient with orthostatic tachycardia; the latency of the response in the feet was greatly prolonged (2.95 s) in the second patient. We also assessed the response of orthostatic tachycardia patients to octreotide and dihydroergotamine, which are known to have a pressor effect in patients with recognized forms of autonomic neuropathy. These agents, in combination, suppressed orthostatic tachycardia (from 116 +/- 7 to 89 +/- 6 beats/min; P less than 0.001) in patients with this syndrome. In summary, our data indicate that evidence of autonomic dysfunction is present in only a minority of patients with orthostatic tachycardia. Nevertheless, administration of the vasoconstrictor drugs dihydroergotamine and octreotide can prevent the abnormal hemodynamic response to the upright posture shown by patients with this syndrome.
HOFMANN; WASSON; RUCK
The Road to Eleusis
The Road to Eleusis
Summary: A secret religion existed for 2,000 years in Greece (until the christians displaced it around 400 AD). The initiation was open to anyone who spoke Greek and hadn't committed murder, once in their life. After 6 month long preporatory rituals, members walked to Eleusius whereupon they underwent secret rituals. The rituals remained secret until the 1970's. Wasson, an ethnomycological scholar and former banker (and the first white to trip on shrooms with the mexican indians) proposed the following explanation of the Eleusian mysteries to Hoffman, an ergot-alkaloid expert chemist, and Ruck, a greek scholar: The Secret of the ritual involved the personal visions induced by drinking the grain decoction administered to the inititiates. The domestication of grains permitted the development of greek civilization; it also brought ergot fungus (of St. Anthony's fire infamy). The thin book contains their argument for the use of the ergot fungus in Eleusian rites, Wasson providing some backround on the use of mushrooms and grains and their role in the culture; Hoffman on the psychoactivity of ergot strains; and Ruck on the mythological and cultural backround of the sect. Evidence includes: Hoffman dosed himself with large (ergot-derived) doses of obstestric compounds to assay their hallucinogenic potential, and found them to possess such activity. The Eleusian temple site still remains, but there is no room to view theatric performances, just rows of tripping initiates, further supporting their argument. An interesting read, and its neat to think that the culture that more or less lead to the western industrial one had psychedelic rites. (Various greek prominant figures attended the rituals, including Plato).
KAMPHUES J; DROCHNER W
Mutterkorn in Futtermitteln--ein Beitrag zur Klarung moglicher mutterkornbedingter Schadensfalle. [Ergot in feed--the clarification of possible ergot-related infirmity cases]
Tierarztl Prax. 1991 Feb; 19(1): 1-7
Practicing veterinarians should realize that the symptoms of ergot intoxication may differ markedly. Gangrenous alterations (ears, feet, tail) as well as convulsive signs (excitability) are described as typical symptoms of ergotism. It is noteworthy that inadequate development of the udder and lactation failure may also be related to ergot contaminated diets. Ergot contamination of diets is caused by grain infection with Claviceps purpurea and sometimes by infection of grass and weed (in grain). The frequency of ergot contamination is high in rye, triticale and wheat and varies in relation to region, climatic conditions and kind of wheat. For diagnosis of ergot contamination a thorough visual inspection of the used diet is to be recommended. Due to the variation of ergots (infected grain, infected weed) it is difficult to determine the contamination in prepared feed mixtures. The anamnestic procedure, method of visual feed inspection as well as a chromatographic method for detection of ergot alkaloids in feed samples are described to facilitate the detection of possible ergot related cases.
Keller, Ullrich; Han, Mehmet; Stoffler-Meilicke, Marina
D-lysergic acid activation and cell-free synthesis of D-lysergyl peptides in enzyme fractions from the ergot fungus Claviceps purpurea
Biochemistry (American Chemical Society) v27 p6164-70 August 9 1988
SUBJECTS: Ergot Lysergic acid Enzymes, Fungal
Keller, Ullrich; Madry, Norbert; Kleinkauf, Horst
Isolation and characterization of vacuoles from the ergot fungus Claviceps purpurea
Applied and Environmental Microbiology v47 p710-14 April 1984
SUBJECTS: Ergot Vacuoles
Kobayashi, Motomasa; Floss, Heinz G.
Biosynthesis of ergot alkaloids: origin of the oxygen atoms in chanoclavine-I and elymoclavine
The Journal of Organic Chemistry v52 p4350-2 September 18 1987
SUBJECTS: Ergot Alkaloids Fungi/Metabolism
Kozikowski, Alan P.; Okita, Makoto; Kobayashi, Motomasa
Probing ergot alkaloid biosynthesis: synthesis and feeding of a proposed intermediate along the biosynthetic pathway. A new amidomalonate for tryptophan elaboration
The Journal of Organic Chemistry v53 p863-9 February 19 1988
SUBJECTS: Alkaloids/Synthesis Fungi/Metabolism Ergot Tryptophan
Kozikowski, Alan P.; Stein, Philip D.
Lewis acid assisted condensations between a 5-methoxyisoxazolidine and silicon-based nucleophiles: gamma-amino alcohol building block in the synthesis of agroclavine I
Journal of the American Chemical Society v107 p2569-71 April 17 1985
SUBJECTS: Condensation, Chemical Silicon compounds Isoxazolidines Ergot
Kozikowski, Alan P.; Wu, Jiang-Ping; Shibuya, Masaaki
Probing ergot alkaloid biosynthesis: identification of advanced intermediates along the biosynthetic pathway
Journal of the American Chemical Society v110 p1970-1 March 16 1988
SUBJECTS: Plants/Metabolism Alkaloids/Synthesis Ergot
Kren, Vladimir; Pazoutova, Sylva; Rylko, Viktor
Extracellular metabolism of sucrose in a submerged culture of Claviceps purpurea: formation of monosaccharides and clavine alkaloids
Applied and Environmental Microbiology v48 p826-9 October 1984
SUBJECTS: Ergot Metabolism/Carbohydrates Fungi/Metabolism Mycology/Cultures and culture media
KURIBARA H; ASAMI T; SAITO T; IDA I; TADOKORO S
Behavioral study on mergocriptine (CBM36-733) by ambulatory activity in mice: repeated administration and interaction with methamphetamine.
Jpn J Pharmacol. 1990 Oct; 54(2): 163-70
Effects of repeated administration of mergocriptine (CBM36-733: CBM), a long-acting ergot derivative with an agonistic action on both dopamine D1 and D2 receptors, as well as interaction between CBM and methamphetamine (MAP: 2 mg/kg, s.c.), were investigated by ambulatory activity in mice. CBM at 4 mg/kg significantly suppressed the ambulatory activity, but significantly increased it at 16 mg/kg in the drug-naive mice. However, 4 and 8 mg/kg of CBM were effective for increasing the ambulatory activity when these doses were repeatedly administered for 9 times at intervals of 7 days. The same treatment with 16 mg/kg of CBM produced a reverse tolerance to the ambulation-increasing effect. The mice that had received CBM at 1 and 2 mg/kg, but not 4-16 mg/kg, demonstrated a significantly lower sensitivity to MAP than the saline-experienced mice. On the other hand, the repeated MAP administration induced not only a reverse tolerance to itself, but also a cross reverse tolerance to 8 and 16 mg/kg of CBM. Furthermore, the established reverse tolerance to MAP was scarcely attenuated by the repeated treatment with any doses of CBM, but rather enhanced by 8 and 16 mg/kg of CBM. The present results indicate that, although the dose-effect relations are partially different, the behavioral characteristics of CBM were almost identical with those of bromocriptine, another long-acting ergot derivative having antagonistic and agonistic actions on dopamine D1 and D2 receptors, respectively.
LANG AE; RILEY DE; VACHON L; LATASTE X
CQA 206-291 in Parkinson's disease: an acute single escalating dosage study.
Can J Neurol Sci. 1990 Nov; 17(4): 416-9
CQA 206-291, a new ergot derivative with a 'biphasic' dopaminergic profile, was studied in 6 patients with longstanding Parkinson's disease suffering from pronounced fluctuations in hourly mobility. On alternate days, up to seven single doses, escalating from 0.2 to 20 mg, were given as replacement for the usual first morning dose of levodopa. At the most effective dosage, four of the six patients obtained as good a peak response to CQA (8-20 mg) as to L-dopa. Side effects were common and similar to other ergot derivatives, suggesting that the initial weak dopamine antagonist properties of the parent compound, documented in animals, may be of little clinical significance. However, comparative studies will be needed to confirm this suspicion. The addition of domperidone successfully reduced the incidence and severity of side effects. CQA 206-291 has potent anti-parkinsonian properties; further longer-term treatment trials are indicated.
Lyons, Philip C.; Plattner, Ronald D.; Bacon, Charles W.
Occurrence of peptide and clavine ergot alkaloids in tall fescue grass
Science v232 p487-9 April 25 1986
SUBJECTS: Ergotism Fescue Alkaloids Plants, Chemical analysis of
MACLENNAN SJ; MARTIN GR
Actions of non-peptide ergot alkaloids at 5-HT1-like and 5-HT2 receptors mediating vascular smooth muscle contraction.
Naunyn Schmiedebergs Arch Pharmacol. 1990 Aug; 342(2): 120-9
This report describes the actions of the non-peptide ergot alkaloids methysergide, methylergometrine and ergometrine at two types of 5-HT receptor mediating vascular contraction; the well established 5-HT2 receptor in rabbit aorta and a non-5-HT2 receptor in rabbit saphenous vein which resembles the 5-HT1-like receptor in dog saphenous vein. In the rabbit aorta ergometrine (1 mumol/l) and methylergometrine (0.3 mumol/l), but not methysergide, produced small contractions (14% and 7% respectively of the maximal response to 5-HT). This contraction was not related to activation of 5-HT2 receptors since it was resistant to blockade by ketanserin (0.3 mumol/l). When examined as antagonists of 5-HT-induced contractions of rabbit aorta, each ergot displayed nanomolar affinity at the 5-HT2 receptor but only methysergide behaved as a simple competitive antagonist (pKB = 8.25). Methylergometrine and ergometrine produced surmountable blockade which was accompanied by a non-parallel displacement of the 5-HT concentration-effect curves. The selective 5-HT1-like receptor agonist GR43175 (less than or equal to 30 mumol/l) was devoid of affinity at the 5-HT2 receptor in rabbit aorta. In the rabbit saphenous vein each of the ergots produced concentration-dependent contractions which resulted in overtly biphasic concentration-effect curves. Only the first phase of contraction mimicked the effects of 5-HT and GR43175 since contractions were not blocked by MDL 72222 (1 mumol/l), but were surmountably antagonised by methiothepin (10 nmol/l), ketanserin (0.3 mumol/l) and spiperone (0.3 mumol/l). ...
MAGEE R
Saint Anthony's fire revisited. Vascular problems associated with migraine medication.
Med J Aust. 1991 Jan 21; 154(2): 145-9
Ergotamine and related compounds have been used for many years in the management of migraine. This review highlights the potential for toxic effects upon the arterial system which may arise from the use of ergot medications. Data on four female patients aged from 30 to 49 years were collected retrospectively from in-patient records and out-patient follow-up between 1978 and 1990. All four patients presented with the symptoms and signs of arterial obstruction and all had been prescribed ergot preparations as treatment and prophylaxis of migraine, for periods ranging from three to 12 years. Two patients had an acute arterial obstruction that resolved completely when the migraine medication was withdrawn. Two had chronic obstructions and radiological and surgical examination gave evidence of arterial stenosis. These two patients were treated with bypass surgery. Review of the literature indicated that other authors had described similar cases but without specifying the methods of data collection. This report supports the findings of others regarding the toxic effects of ergot preparations upon the arterial system, which may take the form of chronic or acute obstruction. General practitioners and physicians should be aware of the possible complications arising from prolonged or excessive use of ergot medications.
MARTIGNONI E; PACCHETTI C; SIBILLA L; BRUGGI P; PEDEVILLA M; NAPPI G
Dihydroergocryptine in the treatment of Parkinson's disease: a six months' double-blind clinical trial.
Clin Neuropharmacol. 1991 Feb; 14(1): 78-83
The short-term efficacy of dihydro-alpha-ergocryptine (DEK), a hydrogenate ergot derivative with dopamine (DA) agonist properties was evaluated in 20 L-dopa (LD) stable responder parkinsonian patients by a 6-month double-blind randomized, placebo-controlled study. A motor improvement was found only in DEK-treated patients at mean daily doses of approximately 40 mg, ranging from 15 to 60 mg. The side effects never required the withdrawal of the drug or changes in its schedule. The authors demonstrate the efficacy and the good tolerability of DEK as a new DA agonist drug that can be added to LD in the treatment of parkinsonian patients.
Merhoff, G. Craig & Porter, John M.
Ergot Intoxication: Historical Review and Description of Unusual Clinical Manifestations.
Annals of Surgery 180:773-779. (1974)
MOHAMED, S N; KAZARIAN, S; MERSKEY, HAROLD; THOMPSON, M G
Treatment of tardive dyskinesia with dihydrogenated ergot alkaloids (Hydergine): A pilot study.
Canadian Journal of Psychiatry; 1980 Jun Vol 25(4) 325-328
Five 25-64 yr old patients with tardive dyskinesia were treated with dihydrogenated ergot alkaloids in doses of 3-4 mg/day for 6 wks. Blind ratings of standard videotape recordings indicated significant differences between Ss. Worsening occurred in 3 Ss during treatment and to a lesser extent after treatment; one S improved during treatment, and the 5th S demonstrated more sustained improvement. (French summary)
MOSKOWITZ MA
Basic mechanisms in vascular headache.
Neurol Clin. 1990 Nov; 8(4): 801-15
To better understand and treat painful conditions, one needs to identify the cause, discover the source, and develop knowledge of peripheral and central pain transmission; headaches are no exception. The development of appropriate animal models is important. Accordingly, we have reviewed the anatomy, neurochemistry, electrophysiology, and pharmacology of the trigeminovascular system in experimental animals and emphasized whenever possible the relevance of this final common pathway to migraine, cluster, and other headache syndromes in humans. For example, based on recent anatomic dissections, the pericarotid cavernous sinus plexus was suggested as an important focus to investigate cluster headache pathophysiology. This plexus is an anatomic point of convergence for the nerves giving rise to the signs of sympathetic and parasympathetic activity and sensory symptoms that develop in cluster patients. As in other nociceptive systems, trigeminovascular axons assume at least two important roles. One concerns the transmission of nociceptive information. Electrophysiologic evidence supports the trigeminal nucleus caudalis as an important site for the convergence of visceral (vessel) and somatic (forehead) inputs to mediate the referral of vascular pain to superficial tissues. A second important role concerns the initiation of local increases in blood flow and enhanced protein permeability (sterile inflammation) via the axonal release of vasoactive neuropeptides. Plasma extravasation develops within the dura mater following trigeminal stimulation. Extravasation can be blocked by the administration of ergot alkaloids or sumatriptan, a new serotonin-like agonist, and a prejunctional (neuronal) mechanism of action for these drugs (such as blockade of release) was suggested based on experimental evidence. Whether vasoconstriction also relates to the therapeutic efficacy remains to be determined. As in other organ systems, real or threatened tissue injury provides an important stimulus for depolarizing sensory fibers. The stimulus may come from external conditions such as reduced blood flow or hypoglycemia. The brain may also possess intrinsic neuronal mechanisms by which nociceptors may be synthesized (e.g., glutamate-induced neurotoxicity, seizures). Molecules of relevance include bradykinin, prostaglandins, leukotrienes, and potassium. Experimental evidence was presented demonstrating that the trigeminal nerve mediates hyperemia within cortical gray matter by axon-reflex like mechanisms. An important role for this nerve was established during the hyperemic period of recirculation after ischemia or during severe hypertension above the limits of autoregulation. ...
RICCI A; AMENTA D; CAVALLOTTI C; ROSSODIVITA I; AMENTA F
Autoradiographic localization of peripheral [3H]-hydergine binding sites.
Arch Int Pharmacodyn Ther. 1990 Mar Apr; 304: 75-92
The anatomical distribution of the ergot derivative [3H]-hydergine (co-dergocrine mesylate) was analyzed by the use of an in vitro autoradiographic technique on frozen sections of rat heart, mesenteric and renal arteries, adrenal gland and kidney. In the heart, [3H]-hydergine was bound by atria and by myocytes of ventricles. In the arterial wall, the drug was bound primarily by the adventitia, by the adventitia-media border and by the intimal layer. The density of adventitial and adventitial-medial binding sites has an inverse relation with the diameter of mesenteric or renal vessels. In the adrenal gland, [3H]-hydergine was bound primarily by the medulla and, in lesser amounts, by the zona glomerulosa. In the kidney, the drug was localized within the arterial tree as well as in cortical tubules and in medullary collecting tubules. The above findings suggest that [3H]-hydergine is bound by various structures involved in the regulation of cardiovascular homeostasis. Interaction with these sites probably accounts for the antihypertensive action of hydergine.
ROSEN, HERBERT J
Mental decline in the elderly: Pharmacotherapy (ergot alkaloids versus papaverine).
Journal of the American Geriatrics Society; 1975 Apr Vol 23(4) 169-174
Reports the 1st double-blind study in outpatients of the effectiveness of dihydrogenated ergot alkaloids (DEA; Hydergine) vs papaverine in the treatment of selected symptoms associated with mental aging. In addition, this study compared the 2 pharmacologic agents in relatively young geriatric patients, with a mean age of 66-67 yrs. After 12 wks of treatment, ratings of overall clinical condition and global change showed that the 26 Ss given DEA improved more than twice as much as the 27 given papaverine. Of the 14 individual symptoms rated, 13 improved significantly more in the DEA group than in the papaverine group. In view of its demonstrated beneficial clinical actions and of its notable scarcity of contraindications or side effects, DEA appears to represent a significant pharmacologic contribution to the care of elderly persons showing selected symptoms of mental and functional decline.
SAXENA PR; DEN BOER MO
Pharmacology of antimigraine drugs.
J Neurol. 1991; 238 Suppl 1: S28-35
The drugs used in migraine therapy can be divided into two groups: agents that abort an established migraine attack and agents used prophylactically to reduce the number of migraine attacks. Both groups have drugs that are specific for migrainous headaches and that are non-specific, and are used to treat the accompanying headache (analgesics), vomiting (anti-emetics), anxiety (sedatives and anxiolytics), or depression (antidepressants). The main drugs with specific action on migraine include ergot alkaloids (ergotamine, dihydroergotamine), agonists (sumatriptan) or partial agonists (methysergide) at a specific subtype of 5-HT1-like receptors, beta-adrenoceptor antagonists (propranolol, metoprolol), calcium antagonists (flunarizine) and anti-inflammatory agents (indomethacin). The pharmacological basis of therapeutic action of several of these drugs is not well understood. In the case of the ergot alkaloids and 5-HT1-like receptor agonists, however, it is likely that the antimigraine effect is related to the potent and rather selective constriction of the large arteries and arteriovenous anastomoses in the scalp and dural regions. In addition, these drugs inhibit plasma extravasation into the dura in response to trigeminal ganglion stimulation, but it is possible that this effect is related to the selective vasoconstriction in the extracerebral vascular bed. The selectivity of the pharmacological effects of these antimigraine drugs (constriction of the extracerebral arteries and arteriovenous anastomoses, poor penetration into the central nervous system and the absence of an antinociceptive effect even after intrathecal administration) strongly suggests that excessive dilatation in the extracerebral cranial vasculature, probably initiated by a neuronal event, is an integral part of the pathophysiology of migraine.
SCHULMAN EA; ROSENBERG SB
Claudication: an unusual side effect of DHE administration.
Headache. 1991 Apr; 31(4): 237-9
DHE is effective in the treatment of acute and chronic migraine. The side effects most commonly observed are abdominal discomfort, muscle pain, diarrhea and anxiety. DHE is a dehydrogenated amino acid ergot alkaloid and, as such, causes only limited vasoconstriction; indeed, its overall effects include peripheral vasodilation. The literature is replete with reports of clinical vasospasm and claudication occurring with therapeutic doses of ergotamine. There has not been any previous description of claudication caused by DHE. This paper describes pulselessness in two patients during relatively short courses of DHE. Treatment consisted of calcium channel blockers and discontinuation of DHE. Recovery was complete.
SCHULTES, RICHARD EVANS
The Botanical and Chemical Distribution of Hallucinogens.
Journal of Psychedelic Drugs Vol.9(No.3) Jul-Sep 1977
The main psychotomimetic constituent of the seeds of both species [Ipomoea tricolor & Rivea corymbosa] are ergine (d-delta-lysergic acid amide) and isoergine (d-delta-isolysergic acid amide) which occur together with minor alkaloids: chanoclavine, elymoclavine, and lysergol. Ergometrine appears to be present in the seeds of I. violacea, but absent in R. corymbosa. The total alkaloid content of R. corymbosa seed is 0.012% ; of I. violacea, 0.06% - and, indeed Indians use smaller quantities of the latter than of the former. I. violacea, often referred to by it's synonyms I. rubro-caerulea and I. tricolor, is represented in horticulture by a number of 'varieties,' such as: Heavenly Blue, Pearly Gates, Flying Saucers, Wedding Bells, Summer Skies, and Blue Stars - all of which contain the hallucinogenic ergot alkaloids.
SCHULTES, RICHARD EVANS
The Botanical and Chemical Distribution of Hallucinogens
Journal of Psychedelic Drugs Vol.9(No.3) Jul-Sep 1977
Ipomoea violacea, often referred to by it's synonyms I. rubro-caerulea and I. tricolor, is represented in horticulture by a number of 'varieties,' such as: Heavenly Blue, Pearly Gates, Flying Saucers, Wedding Bells, Summer Skies, and Blue Stars - all of which contain the hallucinogenic ergot alkaloids.
Shelley, William Scott.
The Elixir: An Alchemical Study of the Ergot Mushrooms.
Notre Dame, IN: Cross Cultural Publications, Inc. (1995)
Shibuya, M.; Chou, H.-M.; Fountoulakis, M.
Stereochemistry of the isoprenylation of tryptophan catalyzed by 4-(gamma, gamma-dimethylallyl)tryptophan synthase from Claviceps, the first pathway-specific enzyme in ergot alkaloid biosynthesis
Journal of the American Chemical Society v112 p297-304 January 3 1990
SUBJECTS: Ergot Tryptophan Isoprenoid compounds Alkaloids
SIEGEL RK
Intoxication
Intoxication. page 71 ISBN 0-525-24764-5
The first intentional use [of ergot] followed shorty after the first accidents when ancient Athenians conducted secret ceremonies in the temple at Eleusis. There, during these nocturnal 'mysteries,' individuals drank kykeon, a mixture of barley with ergot, water, and mint. For two millenia, until supression of these rites by Christianity in the fourth century A.D., thousands of people were annually given this unique experience. Participants included Aristotle, Sophocles, Plato, Aeschylus, Pindar, and several Roman emperors. It was a blissful experience, according to Homer, one that could lift men out of a gloomy darkness and give them what Cicero called a reason to live in joy. Confronted by a profoundly religious experience, the initiates surrendered to the visions with awe and wonderment.
Siegel, Ronald K.
LSD Hallucinations: From Ergot to Electric Kool-Aid.
Journal of Psychoactive Drugs 17(4):247-256. (1985)
SIEGEL, RONALD K
LSD hallucinations: From ergot to electric Kool-Aid.
Journal of Psychoactive Drugs; 1985 Oct-Dec Vol 17(4) 247-256
Presents the natural history of LSD-type hallucinations. It is indicated that not all human encounters with LSD-like hallucinations were accidental or unpleasant. Religious, magical, and medical uses were employed by numerous cultural groups. The experimental analysis of drug-induced hallucinations is also discussed. (29 ref)
SILBERGELD, ELLEN K; HRUSKA, ROBERT E
Lisuride and LSD: Dopaminergic and serotonergic interactions in the 'serotonin syndrome.'
Psychopharmacology; 1979 Nov Vol 65(3) 233-237
A characteristic behavioral syndrome has been associated with stimulation of central serotonin receptors in rats. This behavior can be produced by inhibition of MAO and administration of 5-hydroxytryptophan (5-HTP) as well as by direct acting serotonergic agonists. LSD and the novel ergot derivative lisuride produced this syndrome in male Sprague-Dawley rats. It was not clear how the 2 ergot drugs acted to produce this syndrome. The syndrome produced by pargyline and 5-HTP methyl ester was blocked by haloperidol, methysergide, parachlorophenylalanine, and alphamethylparatyrosine, but these treatments failed to block the effects of lisuride. Methysergide partially blocked the behavioral effects of LSD; pretreatment with either haloperidol or metoclopramide potentiated and prolonged the behavioral effects of LSD. The differences between LSD and lisuride may be relevant to their different psychopharmacological properties.
Soma: Divine Mushroom of Immortality. R. Gordon Wasson. Ethno-mychological Studies 1. Harcourt Brace Jovanovich, Inc. paper edition. no date of publication. 380 pages with color plates. paperback [box 3m]
hardcover-smells strongly of mold. ![[ZEFF LIBRARY]](zefftag.gif)
STOLL W A
Lysergsaure-diathyl-amid, ein Phantastikum aus der Mutterkorngruppe. (LSD, a hallucinatory agent from the ergot group)
Schweiz.Arch.Neur. 60 (1947).
A report is made of the mental effects of LSD. LSD was administered on 29 occasions to 16 normal subjects and on 20 occasions to 6 schizophrenics. LSD produced a state of intoxication of the acute exogenic reaction type. Stress is laid on the fact that LSD is active in very small amounts (20-30 mcg. orally).
STONE, T W
On the antagonism of ergot alkaloids and dopamine by phenothiazines.
Experientia; 1974 Vol 30(7) 827-829
Discusses the mechanism responsible for the antagonism of LSD by the phenothiazines. Molecular models were constructed of both D-LSD and several phenothiazine derivatives. The models indicate the overlap area of the 2 types of molecules to cause antagonism by enabling each to act at the same receptor site. Implications are drawn for the potential identification of the primary cause of psychotic disorders by the investigation of the dopamine antagonist's molecular site of action. (French summary)
USTIUZHANINA SV; SARKISOVA MA; GORIN SE
Konservatsiia produtsenta peptidnykh ergoalkaloidov Claviceps purpurea metodom L-vysushivaniia. [Preservation of Claviceps purpurea, the producer of peptide ergot alkaloids, by the method of freeze drying]
Antibiot Khimioter. 1991 Feb; 36(2): 6-8
A saprotrophic strain of Claviceps purpurea VNIIA 312A, an organism producing peptide +ergot alkaloids with prolactin inhibiting activity was shown to die under lyophilization conditions. To provide long-term storage of strain 312A, L-drying or drying under vacuum from liquid state was used with success. Three protective media were tested. Favourable results were obtained by using 25 per cent maltose solution as a protective medium. Preservation of the culture viability was accompanied by maintenance of the culture capacity for active formation of the biomass and production of +ergot alkaloids.
WASSON RG; HOFMANN A; RUCK CA
The road to Eleusis : unveiling the secret of the mysteries
The road to Eleusis : unveiling the secret of the mysteries. Harcourt, Brace, Jovanovich, 1978 BL795.E5
SUBJECTS: Eleusis, Eleusinian mysteries, Claviceps paspali, Ergot alkaloids
WHITE, FRANCIS J; APPEL, JAMES B
Lysergic acid diethylamide (LSD) and lisuride: Differentiation of their neuropharmacological actions.
Science; 1982 Apr Vol 216(4545) 535-537
The nonhallucinogenic ergot derivative lisuride exerts many pharmacological effects that are similar to those of its hallucinogenic congener, LSD. It was shown that 63 water-deprived rats trained to discriminate between the presence of one drug and the other (0.02, 0.08, or 0.32 mg/kg) can be used to differentiate the actions of these compounds on a neuronal level. The discriminative stimulus effect of LSD (the LSD cue) is similar to that of the serotonin agonist quipazine, whereas the lisuride cue is similar to that of the dopamine agonist apomorphine. Data support the hypothesis that serotonin is intricately involved in the hallucinogenic effects of LSD.
WILCOX, JAMES A
Psychoactive properties of methysergide.
Journal of Psychoactive Drugs; 1987 Oct-Dec Vol 19(4) 387-388
Presents the case of a 29-yr-old male who experienced hallucinations, anxiety, and feelings of depersonalization after taking the ergot alkaloid derivative methysergide, which had been prescribed as a prophylactic for the S's vascular headaches.
WILKINSON, ROBERT E; HARDCASTLE, WILLIS S; MCCORMICK, CYNTHIA S
Psychotomimetic ergot alkaloid contents of seed from Calonyction muricatum, Jacquemontia tamnifolia, Quamoclit lobata, and Q. sloteri
Botanical Gazette; March 1988 Vol 149 pg 107-109
Psychotomimetic substances in cultivated morning-glory seed have resulted in a prohibition of morning-glory seed in soybean sold internationally. Seeds of four native, wild morning glory species - purple moonflower (Calonyction muricatum), smallflower morning glory (Jacquemontia tamnifolia), cypressvine (Quamoclit lobata), and cardinal creeper (Q. sloteri) - were analysed for ergot alkaloid contents. Seed of a horticultural variety of Ipomoea violaceae 'Heavenly Blue' contained 0.052% total alkaloids. Total ergot alkaloids in the wild morning-glory species ranged from 0.0029% to 0.0059% (5.6%-11.4% of the total alkaloids in 'Heavenly Blue' seed). Major alkaloids were separated and characterized by two-dimensional thin-layer chromatography and co-chromatography with authenticated standards as chanoclavine, elymoclavine, penniclavine, ergonovinine, agroclavine, ergonovine, ergosine, and ergosinine. The types of alkaloids varied among morning-glory species, and the quantities were too small to be considered a psychotomimetic hazard in soybean utilized for human consumption.
WITTERS W L
Extraction and identification of clavine and lysergic acid alkaloids from morning glories
Ohio Journal of Science; Vol. 75 pp 198-201
[NO ABSTRACT] Morning glories. Ergot alkloid extraction.
Ergot-Related Patents: 1994 1995