Novel GABA analogues as hypotensive agents

The actions of four analogues of gamma-aminobutyric acid (GABA) on blood pressure and heart rate were measured in the cat after intracerebroventricular administration. These compounds were previously found to inhibit binding to GABAA receptors of neuronal membranes from the CNS of the rat. Each of t...

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Bibliographic Details
Published inNeuropharmacology Vol. 25; no. 11; p. 1191
Main Authors Matheson, G K, Freed, E, Tunnicliff, G
Format Journal Article
LanguageEnglish
Published England 01.11.1986
Subjects
Aminobenzoates - pharmacology
Animals
Antihypertensive Agents
Blood Pressure - drug effects
Cats
Female
gamma-Aminobutyric Acid - analogs & derivatives
gamma-Aminobutyric Acid - pharmacology
Heart Rate - drug effects
Injections, Intraventricular
Male
meta-Aminobenzoates
Pyrroles - pharmacology
Receptors, GABA-A - drug effects
Taurine - analogs & derivatives
Taurine - pharmacology
Urocanic Acid - pharmacology
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Summary:The actions of four analogues of gamma-aminobutyric acid (GABA) on blood pressure and heart rate were measured in the cat after intracerebroventricular administration. These compounds were previously found to inhibit binding to GABAA receptors of neuronal membranes from the CNS of the rat. Each of the drugs, together with GABA, produced an average maximum reduction in blood pressure of 27.63% +/- 12.5. However, aminoethanethiosulfonic acid (AETS) was the most potent (ED50 = 2.24 X 10(-10) mol/kg) of the drugs, followed by 5-phenyl-2-pyrrole propionic acid (PPP), urocanic acid (UCA), m-aminobenzoic acid (MABA) and GABA. None of the compounds produced a significant effect on heart rate. The fact that these analogues mimicked the action of GABA on the cardiovascular system of the cat and that they were able to inhibit binding to GABAA receptors, indicates that they may be GABA agonists.
ISSN:0028-3908
DOI:10.1016/0028-3908(86)90135-8