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首页> 外文期刊>Life sciences >BIOCHEMICAL AND PHARMACOLOGICAL CHARACTERISATION OF SR141716A, THE FIRST POTENT AND SELECTIVE BRAIN CANNABINOID RECEPTOR ANTAGONIST
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BIOCHEMICAL AND PHARMACOLOGICAL CHARACTERISATION OF SR141716A, THE FIRST POTENT AND SELECTIVE BRAIN CANNABINOID RECEPTOR ANTAGONIST

机译：SR141716A，第一种强效和选择性脑大麻素受体拮抗剂的生物化学和药理特性

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摘要

SR141716A is a selective, potent and orally active antagonist of the brain cannabinoid receptor with a long duration of action. This compound shows high affinity for the central cannabinoid receptor (K-i=2 nM), displays low affinity for the peripheral cannabinoid receptor (K-i>1000 nM). In vitro, SR141716A antagonizes the inhibitory effects of cannabinoid receptor agonists on both mouse vas deferens contractions and dopamine-stimulated adenylyl cyclase activities in rat brain membranes. After oral administration SR141716A totally inhibited the ex vivo [H-3]-CP55,940 binding to cerebral membranes with a ED(50) value of 3.5 mg/kg. Furthermore SR141716A antagonizes the classical pharmacological responses elicited by cannabinoid receptor agonists. In addition, SR141716A reverses the inhibitory effect of WIN55212-2 on isoniazid-induced elevation of cGMP in rat cerebellum. This compound will provide a powerful tool for studying the in vivo functions of the anandamide/cannabinoid system. [References: 18]
机译：SR141716A是脑大麻素受体的选择性，有效和口服活性拮抗剂，具有长效作用。该化合物对中央大麻素受体表现出高亲和力（K-1 = 2 nM），对周围大麻素受体表现出低亲和力（K-i> 1000 nM）。在体外，SR141716A拮抗大麻素受体激动剂对小鼠输精管收缩和大鼠脑膜中多巴胺刺激的腺苷酸环化酶活性的抑制作用。口服后，SR141716A完全抑制离体[H-3] -CP55,940与脑膜的结合，ED（50）值为3.5 mg / kg。此外，SR141716A拮抗大麻素受体激动剂引起的经典药理反应。另外，SR141716A逆转了WIN55212-2对异烟肼诱导的大鼠小脑cGMP升高的抑制作用。该化合物将为研究anandamide / cannabinoid系统的体内功能提供强大的工具。 [参考：18]

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