Abstract
A series of aroxyethylamines (1-10) was synthesized and evaluated for hypotensive activity in rats after intravenous and oral administration. The 4 compounds (4, 7, 8 and 10) containing a (2-methoxy)phenylpiperazine moiety displayed hypotensive activity and their affinities for alpha1-, alpha2- and beta1-adrenoreceptors were determined by radioligand binding assays. Compounds 4, 7, 8 and 10 were also tested for their effect on the pressor responses to epinephrine, norepinephrine, methoxamine, tyramine and DMPP. The results suggest that the hypotensive effect of these compounds is related to their alpha- and beta-adrenolytic properties.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Administration, Oral
-
Animals
-
Antihypertensive Agents / chemical synthesis*
-
Antihypertensive Agents / metabolism
-
Antihypertensive Agents / pharmacology*
-
Binding, Competitive / drug effects
-
Blood Pressure / drug effects
-
Chromatography, Thin Layer
-
Ethylamines / chemistry*
-
Ethylamines / pharmacology*
-
Indicators and Reagents
-
Injections, Intravenous
-
Kinetics
-
Lethal Dose 50
-
Magnetic Resonance Spectroscopy
-
Male
-
Mice
-
Radioligand Assay
-
Rats
-
Rats, Wistar
-
Receptors, Adrenergic / drug effects
-
Receptors, Adrenergic / metabolism*
-
Receptors, Adrenergic, alpha-1 / drug effects
-
Receptors, Adrenergic, alpha-1 / metabolism
-
Receptors, Adrenergic, alpha-2 / drug effects
-
Receptors, Adrenergic, alpha-2 / metabolism
-
Receptors, Adrenergic, beta-1 / drug effects
-
Receptors, Adrenergic, beta-1 / metabolism
-
Structure-Activity Relationship
-
Vasoconstrictor Agents / antagonists & inhibitors
-
Vasoconstrictor Agents / pharmacology
Substances
-
Antihypertensive Agents
-
Ethylamines
-
Indicators and Reagents
-
Receptors, Adrenergic
-
Receptors, Adrenergic, alpha-1
-
Receptors, Adrenergic, alpha-2
-
Receptors, Adrenergic, beta-1
-
Vasoconstrictor Agents