Etilefrine

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Etilefrine
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Systematic (IUPAC) name
(RS)-3-[2-(ethylamino)-1-hydroxyethyl]phenol
Clinical data
AHFS/Drugs.com International Drug Names
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Identifiers
CAS number 709-55-7
ATC code C01CA01
PubChem CID 3306
ChemSpider 3190 7pxY
UNII ZB6F8MY53V 7pxY
KEGG D07931 7pxY
ChEMBL CHEMBL86882 7pxY
Synonyms (2-ethylamino-1-(3'-hydroxy-phenyl)ethanol
Chemical data
Formula C10H15NO2 
Mol. mass 181.232 g/mol
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Etilefrine is a cardiac stimulant used as an antihypotensive. It is a sympathomimetic amine of the 3-hydroxy-phenylethanolamine series used in treating orthostatic hypotension of neurological, cardiovascular, endocrine or metabolic origin. Intravenous infusion of this compound increases cardiac output, stroke volume, venous return and blood pressure in man and experimental animals, suggesting stimulation of both α and β adrenergic receptors.[1] However, in vitro studies indicate that etilefrine has a much higher affinity for β1 (cardiac) than for β2 adrenoreceptors.[2]

Intravenous etilefrine increases the pulse rate, cardiac output, stroke volume, central venous pressure and mean arterial pressure of healthy individuals. Peripheral vascular resistance falls during the infusion of 1–8 mg etilefrine but begins to rise at higher dosage. Marked falls in pulse rate, cardiac output, stroke volume and peripheral bloodflow, accompanied by rises in mean arterial pressure, occur when etilefrine is infused after administration of intravenous propranolol 2,5 mg. These findings indicate that etilefrine has both β1 and α1 adrenergic effects in man.

References

  1. Nusser, Donath and Russ, 1965; Mellander, 1966; Limbourg, Just and Lang, 1973; Tarnow et al.~1973; Carrera and Aguilera, 1973.
  2. Offermeier and Dreyer, 1971.

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