GABAB receptor antagonist and GABAA receptor agonist properties of a delta-aminovaleric acid derivative, Z-5-aminopent-2-enoic acid.
The activity of Z-5-aminopent-2-enoic acid (A), a conformationally restricted analogue of delta-aminovaleric acid, was investigated in vitro in the guinea pig isolated ileum and vas deferens. A was found to be a relatively potent GABAB-receptor antagonist and a relatively weak GABAA-receptor agonist. The GABAB-receptor antagonist activity of A was at least 5 times greater than that of phaclofen, a selective GABAB-receptor antagonist. A may therefore be an important lead for the development of new potent and selective GABAB-antagonists.
Dickenson
H W
HW
Department of Pharmacology, University of Sydney, N.S.W., Australia.
Allan
R D
RD
Ong
J
J
Johnston
G A
GA
D000596:Amino Acids / Q000378:metabolism* / Q000494:pharmacology*; D021542:Amino Acids, Neutral; D000818:Animals; D001640:Bicuculline / Q000494:pharmacology; D006168:Guinea Pigs; D007082:Ileum / Q000294:innervation* / Q000502:physiology; D066298:In Vitro Techniques; D008297:Male; D009119:Muscle Contraction / Q000187:drug effects*; D011963:Receptors, GABA-A / Q000187:drug effects / Q000502:physiology*; D014649:Vas Deferens / Q000294:innervation / Q000502:physiology
D000596:Amino Acids; D021542:Amino Acids, Neutral; D011963:Receptors, GABA-A; C013809:5-aminovaleric acid; C056204:5-aminopent-2-enoic acid; D001640:Bicuculline