Howlett A C
Department of Pharmacological and Physiological Science, Saint Louis University School of Medicine, Missouri 63104, USA.
Annu Rev Pharmacol Toxicol. 1995;35:607-34. doi: 10.1146/annurev.pa.35.040195.003135.
Two subtypes of cannabinoid receptors, CB1 and CB2, have been described to date, although future investigations may elucidate other receptors. The actions of cannabimimetic agents via CB1 receptors in brain are mediated by GI/O to inhibit adenylate cyclase and Ca2+ channels. Little is known about signal transduction mechanisms utilized by CB2 receptors. Three classes of agonist ligands regulate cannabinoid receptors: cannabinoid, aminoalkyl-indole, and eicosanoid derivatives. Cannabinoid receptors produce analgesia and modify cognition, memory, locomotor activity, and endocrine functions in mammals.
迄今为止,已发现两种大麻素受体亚型,即CB1和CB2,不过未来的研究可能会阐明其他受体。大麻素模拟剂通过脑中CB1受体产生的作用由G蛋白偶联内向整流钾通道(GIRK)/G蛋白α亚基(Gi/o)介导,从而抑制腺苷酸环化酶和钙通道。关于CB2受体所利用的信号转导机制,人们了解甚少。三类激动剂配体可调节大麻素受体:大麻素、氨基烷基吲哚和类花生酸衍生物。大麻素受体可产生镇痛作用,并改变哺乳动物的认知、记忆、运动活性及内分泌功能。