R-(-)-BETA-PHENYL-GABA IS A FULL AGONIST AT GABA(B) RECEPTORS IN BRAIN-SLICES BUT A PARTIAL AGONIST IN THE ILEUM

被引：24
|
作者：
ONG, J [1 ]
KERR, DIS [1 ]
DOOLETTE, DJ [1 ]
DUKE, RK [1 ]
MEWETT, KN [1 ]
ALLEN, RD [1 ]
JOHNSTON, GAR [1 ]
机构：
[1] UNIV SYDNEY,DEPT PHARMACOL,SYDNEY,NSW 2006,AUSTRALIA
来源：
EUROPEAN JOURNAL OF PHARMACOLOGY | 1993年 / 233卷 / 01期
关键词：
BACLOFEN; BETA-PHENYL-GABA; GABA(B) RECEPTORS; BRAIN SLICES (RAT); ILEUM (GUINEA-PIG); (AGONIST PARTIAL AGONIST);
D O I：
10.1016/0014-2999(93)90364-N
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
R-(-)-beta-phenyl-GABA has been compared at GABA(B) receptors using cortical and ileal preparations. R-(-)-beta-phenyl-GABA (EC50 = 25 muM) was a less potent full agonist than R,S-(+/-)-baclofen (EC50 = 2.5 muM), in depressing CA1 population spikes of rat hippocampal slices, and 5 times less potent in attenuating the spontaneous discharges of rat neocortex. However, R-(-)-beta-phenyl-GABA (100-400 muM) was only a weak partial agonist in the ileum. All these actions were sensitive to CGP 35348 (3-aminopropyl-(P-diethoxymethyl)-phosphinic acid) and therefore mediated by GABA(B) receptors.
引用
收藏
页码：169 / 172
页数：4
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