Sim L J, Xiao R, Childers S R
Department of Physiology and Pharmacology, Bowman Gray School of Medicine, Wake Forest University, Winston-Salem, NC 27157, USA.
Neuroreport. 1996 Feb 29;7(3):729-33. doi: 10.1097/00001756-199602290-00012.
Recent reports have identified an endogenous peptide ligand for the opioid receptor-like (ORL1) receptor. In the present study, ORL1 peptide-stimulated [35>]GTP gamma S binding was assessed in rat cortical membranes and brain sections to localize ORL1 receptor-activated G-proteins. In membrane assays, with 20 microM GDP, ORL1 peptide stimulated [35S]GTP gamma S binding by approximately two-fold with an ED50 value of 20 nM. ORL1 peptide-stimulated [35S]GTP gamma S binding was unaffected by opioid or other G-protein-coupled receptor antagonists. In brain sections, ORL1 peptide-stimulated [35S]GTP gamma S binding was identified in regions including cortex, amygdala, hypothalamus, thalamus and brain stem. The anatomical distribution of ORL1 peptide-stimulated [35S]GTP gamma S binding suggests its involvement in cognition, emotion and homeostasis.
最近的报道已鉴定出一种阿片样物质受体样（ORL1）受体的内源性肽配体。在本研究中，在大鼠皮质膜和脑切片中评估了ORL1肽刺激的[35S]GTPγS结合，以定位ORL1受体激活的G蛋白。在膜试验中，使用20μM GDP时，ORL1肽刺激的[35S]GTPγS结合增加了约两倍，ED50值为20 nM。ORL1肽刺激的[35S]GTPγS结合不受阿片类药物或其他G蛋白偶联受体拮抗剂的影响。在脑切片中，在包括皮质、杏仁核、下丘脑、丘脑和脑干在内的区域中鉴定出ORL1肽刺激的[35S]GTPγS结合。ORL1肽刺激的[35S]GTPγS结合的解剖学分布表明其参与认知、情绪和体内平衡。
