SQ 20009与类GABA药物作为苯二氮䓬受体结合调节剂的相互作用。

Interaction of SQ 20009 and GABA-like drugs as modulators of benzodiazepine receptor binding.

作者信息

Supavilai P, Karobath M

出版信息

Eur J Pharmacol. 1980 Mar 21;62(2-3):229-33. doi: 10.1016/0014-2999(80)90282-4.

Abstract

SQ 20009, a new anxiolytic drug structurally unrelated to GABA or benzodiazepines, has two modulatory effects on the binding of 3H-flunitrazepam to membranes from rat cerebellum. Thus, SQ 20009 has a direct and chloride ion dependent stimulatory effect on benzodiazepine receptor binding which in turn appears to be modulated by the associated GABA receptor. In addition SQ 20009 has indirect effects on benzodiazepine receptor binding since it enhances the potency of GABA and muscimol to stimulate 3H-flunitrazepam binding.

摘要

SQ 20009是一种结构上与γ-氨基丁酸（GABA）或苯二氮䓬无关的新型抗焦虑药物，它对3H-氟硝西泮与大鼠小脑细胞膜的结合有两种调节作用。因此，SQ 20009对苯二氮䓬受体结合具有直接的、氯离子依赖性的刺激作用，而这种作用似乎又受到相关GABA受体的调节。此外，SQ 20009对苯二氮䓬受体结合有间接作用，因为它增强了GABA和蝇蕈醇刺激3H-氟硝西泮结合的效力。