Demuth Dirk G, Molleman Areles
School of Life Sciences, University of Hertfordshire, CP Snow Building, Hatfield, Herts, UK.
Life Sci. 2006 Jan 2;78(6):549-63. doi: 10.1016/j.lfs.2005.05.055. Epub 2005 Aug 18.
After their discovery, the two known cannabinoid receptors, CB(1) and CB(2), have been the focus of research into the cellular signalling mechanisms of cannabinoids. The initial assessment, mainly derived from expression studies, was that cannabinoids, via G(i/o) proteins, negatively modulate cyclic AMP levels, and activate inward rectifying K(+) channels. Recent findings have complicated this assessment on different levels: (1) cannabinoids include a wide range of compounds with varying profiles of affinity and efficacy at the known CB receptors, and these profiles do not necessarily match their biological activity; (2) CB receptors appear to be intrinsically active and possibly coupled to more than one type of G protein; (3) CB receptor signalling mechanisms are diverse and dependent on the system studied; (4) cannabinoids have other targets than CB receptors. The aim of this mini review is to discuss the current literature regarding CB receptor signalling pathways. These include regulation of adenylyl cyclase, MAP kinase, intracellular Ca(2+), and ion channels. In addition, actions of cannabinoids that are not mediated by CB(1) or CB(2) receptors are discussed.
在这两种已知的大麻素受体CB(1)和CB(2)被发现之后,它们一直是大麻素细胞信号传导机制研究的焦点。最初的评估主要来自表达研究,认为大麻素通过G(i/o)蛋白负向调节环磷酸腺苷水平,并激活内向整流钾通道。最近的研究结果在不同层面使这一评估变得复杂:(1)大麻素包括多种化合物,它们对已知CB受体的亲和力和效力各不相同,而且这些特性不一定与其生物活性相匹配;(2)CB受体似乎具有内在活性,并且可能与不止一种类型的G蛋白偶联;(3)CB受体信号传导机制多种多样,且取决于所研究的系统;(4)大麻素除了CB受体外还有其他靶点。本综述的目的是讨论当前关于CB受体信号通路的文献。这些包括腺苷酸环化酶、丝裂原活化蛋白激酶、细胞内Ca(2+)和离子通道的调节。此外,还讨论了不由CB(1)或CB(2)受体介导的大麻素作用。