Anderson R A, Mitchell R
Eur J Pharmacol. 1985 Dec 3;118(3):355-8. doi: 10.1016/0014-2999(85)90148-7.
The effect of the selective GABAB receptor agonist baclofen was examined on stimulus-induced release of [3H]GABA from crude synaptosomal preparations of median eminence (ME) and pituitary neurointermediate lobe (NI). Baclofen stereospecifically inhibited release of [3H]GABA in a concentration-dependent manner from ME but had no effect in NI. The effect of (+/-) baclofen was partly antagonized by the putative GABAB receptor antagonist delta-aminovaleric acid, but these experiments were complicated by a degree of heteroexchange. These results provide the first evidence for GABAB autoreceptors in the CNS.
研究了选择性γ-氨基丁酸B(GABAB)受体激动剂巴氯芬对来自正中隆起(ME)和垂体神经中间叶(NI)的粗制突触体制剂中刺激诱导的[3H]γ-氨基丁酸(GABA)释放的影响。巴氯芬以浓度依赖性方式立体特异性地抑制ME中[3H]GABA的释放,但对NI没有影响。消旋巴氯芬的作用部分被推定的GABAB受体拮抗剂δ-氨基戊酸拮抗,但这些实验因一定程度的异源交换而变得复杂。这些结果为中枢神经系统中GABAB自身受体提供了首个证据。