作者
Mary Chebib, Tina Hinton, Katrina L Schmid, Darren Brinkworth, Haohua Qian, Susana Matos, Hye-Lim Kim, Heba Abdel-Halim, Rohan J Kumar, Graham AR Johnston, Jane R Hanrahan
发表日期
2009/2/1
期刊
Journal of Pharmacology and Experimental Therapeutics
卷号
328
期号
2
页码范围
448-457
出版商
American Society for Pharmacology and Experimental Therapeutics
简介
This study reports pharmacological and physiological effects of cis- and trans-(3-aminocyclopentanyl)butylphosphinic acid (cis- and trans-3-ACPBPA). These compounds are conformationally restricted analogs of the orally active GABAB/C receptor antagonist (3-aminopropyl)-n-butylphosphinic acid (CGP36742 or SGS742). cis-[IC50(ρ1) = 5.06 μM and IC50(ρ2) = 11.08 μM; n = 4] and trans-3-ACPMPA [IC50(ρ1) = 72.58 μM and IC50(ρ2) = 189.7 μM; n = 4] seem competitive at GABAC receptors expressed in Xenopus laevis oocytes, having no effect as agonists (1 mM) but exerting weak antagonist (1 mM) effects on human GABAA and GABAB receptors. cis-3-ACPBPA was more potent and selective than the trans-compound, being more than 100 times more potent at GABAC than GABAA or GABAB receptors. cis-3-ACPBPA was further evaluated on dissociated rat retinal bipolar cells and dose-dependently inhibited …
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M Chebib, T Hinton, KL Schmid, D Brinkworth, H Qian… - Journal of Pharmacology and Experimental …, 2009