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CL 218872对苯二氮䓬受体的激动剂和反向激动剂作用。

Agonist and inverse agonist effects of CL 218872 on benzodiazepine receptors.

作者信息

Gardner C R

出版信息

Neurosci Lett. 1984 Sep 28;51(1):1-6. doi: 10.1016/0304-3940(84)90253-2.

Abstract

Extracellular action potentials were recorded from cerebellar Purkinje cells in urethane-anaesthetised rats. Synaptic inhibition was evoked by electrical stimulation of the nearby cortical surface and recorded using peristimulus-time histograms. A benzodiazepine agonist, RU 32007, decreased cell firing rate and increased the inhibitory response duration in parallel. beta-Carboline ethyl ester increased firing and decreased the inhibitory response. In some cases the inhibitory response was abolished, independent of the change in firing. CL 218872 decreased firing with the parallel increase in inhibitory response. However, in some cases the inhibitory response was abolished despite decreases in firing. All the effects of all three agents were blocked by Ro 15-1788.

摘要

在氨基甲酸乙酯麻醉的大鼠中,从小脑浦肯野细胞记录细胞外动作电位。通过电刺激附近的皮质表面诱发突触抑制,并使用刺激后时间直方图进行记录。一种苯二氮䓬激动剂RU 32007降低细胞放电率,并同时增加抑制反应持续时间。β-咔啉乙酯增加放电并减少抑制反应。在某些情况下,抑制反应被消除,与放电变化无关。CL 218872降低放电,同时抑制反应平行增加。然而,在某些情况下,尽管放电减少,抑制反应仍被消除。这三种药物的所有作用均被Ro 15-1788阻断。

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