GABA 激动剂 THIP（一种蝇蕈醇类似物）不干扰大鼠皮质膜上的苯二氮䓬结合位点。

The GABA agonist THIP a muscimol analogue, does not interfere with the benzodiazepine binding site on rats cortical membranes.

作者信息

Maurer R

出版信息

Neurosci Lett. 1979 Apr;12(1):65-8. doi: 10.1016/0304-3940(79)91481-2.

Abstract

THIP, a cyclic analogue of muscimol, is a powerful GABA agonist. It is as active as GABA in displacing [3H]muscimol from its binding site to cerebellar membranes (IC50 = 31.5 +/- 2.5 mM). However, unlike muscimol or GABA, it is devoid of any modulatory interaction with the benzodiazepine binding site on rat's cortical membranes. Homotaurine, isoguvacine and imidazole acetic acid are less active than muscimol and GABA for increasing the affinity of [3H]diazepam to cortical membrane preparations.

摘要

THIP是蝇蕈醇的环状类似物，是一种强效GABA激动剂。它在从小脑细胞膜的结合位点取代[3H]蝇蕈醇方面与GABA活性相当（IC50 = 31.5 +/- 2.5 mM）。然而，与蝇蕈醇或GABA不同，它与大鼠皮质膜上的苯二氮䓬结合位点没有任何调节性相互作用。高牛磺酸、异鹅膏蕈氨酸和咪唑乙酸在增加[3H]地西泮与皮质膜制剂的亲和力方面比蝇蕈醇和GABA活性低。