CGP 35348 - A CENTRALLY ACTIVE BLOCKER OF GABA-B RECEPTORS
CGP 35348 - A CENTRALLY ACTIVE BLOCKER OF GABA-B RECEPTORS
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DOI：
10.1016/0014-2999(90)90337-6
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发表时间：
1990-10-02
影响因子：
5
通讯作者：
BITTIGER, H
中科院分区：
文献类型：
--
作者：
OLPE, HR;KARLSSON, G;BITTIGER, H
本文介绍了新型GABA受体阻滞剂CGP-35348的生化、电生理和药理性质。在各种受体结合分析中，CGP35348只与GAAB受体有亲和力。CgP 35348在GABAB受体上的IC_(50)为34微米。该化合物可拮抗L-巴氯芬对去甲肾上腺素引起的大鼠皮层脑片腺苷环化酶的增强作用。在电生理学研究中，CGP 35348(10,100微米)可拮抗L-巴氯芬对大鼠脊髓的作用。在海马片制备中，CGP 35348(10，30,100微米)阻断D/L-巴氯芬(10微米)诱发的膜超极化和晚期抑制性突触后电位。CGP 35348的效力似乎是GABA受体阻滞剂苯氯芬的10-30倍。离子导入和行为学实验表明，腹腔注射后，大脑中的GABAB受体被阻断。《中国政府采购协议35348》的管理。该化合物在阐明大脑GABAB受体的作用方面可能有相当大的价值。
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 has an IC50 of 34 .mu.M at the GABAB receptor. The compound antagonized (100, 300, 1000 .mu.M) the potentiating effect of L-baclofen on noradrenaline-induced stimulation of adenylate cyclase in rat cortex slices. In electrophysiological studies CGP 35348 (10, 100 .mu.M) antagonized the effect of L-baclofen in the isolated rat spinal cord. In the hippocampal slice preparation CGP 35348 (10, 30, 100 .mu.M) blocked the membrane hyperpolarization induced by D/L-baclofen (10 .mu.M) and the late inhibitory postsynaptic potential. CGP 35348 appeared to be 10-30 times more potent that the GABAB receptor blocker phaclofen. Ionophoretic and behavioural experiments showed that GABAB receptor 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.