GPR55 is a cannabinoid receptor that increases intracellular calcium and inhibits M current |
| |
Authors: | Lauckner Jane E Jensen Jill B Chen Huei-Ying Lu Hui-Chen Hille Bertil Mackie Ken |
| |
Institution: | Departments of *Physiology and Biophysics and ;¶Anesthesiology and ;†Neurobiology and Behavior Graduate Program, University of Washington, Seattle, WA 98195; and ;‡Department of Pediatrics, Baylor College of Medicine, Houston, TX 77030 |
| |
Abstract: | The CB(1) cannabinoid receptor mediates many of the psychoactive effects of Delta(9)THC, the principal active component of cannabis. However, ample evidence suggests that additional non-CB(1)/CB(2) receptors may contribute to the behavioral, vascular, and immunological actions of Delta(9)THC and endogenous cannabinoids. Here, we provide further evidence that GPR55, a G protein-coupled receptor, is a cannabinoid receptor. GPR55 is highly expressed in large dorsal root ganglion neurons and, upon activation by various cannabinoids (Delta(9)THC, the anandamide analog methanandamide, and JWH015) increases intracellular calcium in these neurons. Examination of its signaling pathway in HEK293 cells transiently expressing GPR55 found the calcium increase to involve G(q), G(12), RhoA, actin, phospholipase C, and calcium release from IP(3)R-gated stores. GPR55 activation also inhibits M current. These results establish GPR55 as a cannabinoid receptor with signaling distinct from CB(1) and CB(2). |
| |
Keywords: | orphan pain CB3 G protein-coupled receptor |
本文献已被 PubMed 等数据库收录! |
|