CGP 35348 - A CENTRALLY ACTIVE BLOCKER OF GABA-B RECEPTORS

被引：315

作者：

OLPE, HR ^{[1
]}

KARLSSON, G ^{[1
]}

POZZA, MF ^{[1
]}

BRUGGER, F ^{[1
]}

STEINMANN, M ^{[1
]}

VANRIEZEN, H ^{[1
]}

FAGG, G ^{[1
]}

HALL, RG ^{[1
]}

FROESTL, W ^{[1
]}

BITTIGER, H ^{[1
]}

机构：

[1] CIBA GEIGY LTD,CENT RES LABS,MANCHESTER M17 1WT,ENGLAND

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1990年 / 187卷 / 01期

关键词：

(Rat); Baclofen; CGP; 35348; GABA (γ-aminobutyric acid); GABA[!sub]B[!/sub] receptor antagonists; GABA[!sub]B[!/sub] receptors; Hippocampus; Spinal cord;

D O I：

10.1016/0014-2999(90)90337-6

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The biochemical, electrophysiological and pharmacological properties of the new GABAB receptor blocker CGP 35348 are described. In a variety of receptor binding assays CGP 35348 showed affinity for the GABAB receptor only. CGP 35348 had an IC50 of 34 μM at the GABAB receptor. The compound antagonized (100, 300, 1000 μM) the potentiating effect of L-baclofen on noradrenaline-induced stimulation of adenylate cyclase in rat cortex slices. In electrophysiological studies CGP 35348 (10, 100 μM) antagonized the effect of L-baclofen in the isolated rat spinal cord. In the hippocampal slice preparation CGP 35348 (10, 30, 100 μM) blocked the membrane hyperpolarization induced by D/L-baclofen (10 μM) and the late inhibitory postsynaptic potential. CGP 35348 appeared to be 10-30 times more potent than the GABAB receptor blocker phaclofen. Ionophoretic and behavioural experiments showed that GABAB receptors in the brain were blocked after i.p. administration of CGP 35348. This compound may be of considerable value in elucidating the roles of brain GABAB receptors. © 1990.

引用

页码：27 / 38

页数：12

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