Connor M, Yeo A, Henderson G
Department of Pharmacology, University of Bristol.
Br J Pharmacol. 1996 May;118(2):205-7. doi: 10.1111/j.1476-5381.1996.tb15387.x.
The human neuroblastoma cell line SH-SY5Y expresses the 'orphan' opioid receptor (ORL1). We have demonstrated that nociceptin, the putative endogenous ligand for ORL1, produces a concentration-dependent inhibition of the N-type calcium channel current in these cells (IC50 42 nM). In addition, in the presence of carbachol, nociceptin increased the intracellular concentration of Ca2+ (EC50 60 nM). Both effects of nociceptin were blocked by pertussis toxin pretreatment but not by the opioid antagonists CTAP (1 microM), naltrindole (1 microM) and naloxone (10 microM).
人神经母细胞瘤细胞系SH-SY5Y表达“孤儿”阿片受体(ORL1)。我们已经证明,伤害感受肽(ORL1的假定内源性配体)对这些细胞中的N型钙通道电流产生浓度依赖性抑制作用(IC50为42 nM)。此外,在卡巴胆碱存在的情况下,伤害感受肽增加了细胞内Ca2+的浓度(EC50为60 nM)。伤害感受肽的这两种作用均被百日咳毒素预处理所阻断,但未被阿片拮抗剂CTAP(1 microM)、纳曲吲哚(1 microM)和纳洛酮(10 microM)阻断。