Mima H, Morikawa H, Fukuda K, Kato S, Shoda T, Mori K
Department of Anesthesia, Kyoto University Hospital, Japan.
Eur J Pharmacol. 1997 Dec 11;340(2-3):R1-2.
Endomorphin-1 and -2, recently isolated endogenous peptides specific for the mu-opioid receptor, inhibited Ca2+ channel currents with EC50 of 6 and 9 nM, respectively, in NG108-15 cells transformed to express the cloned rat mu-opioid receptor. On the other hand, they elicited no response in nontransfected NG108-15 cells. It is concluded that endomorphin-1 and -2 induce Ca2+ channel inhibition by selectively activating the mu-opioid receptor.
内吗啡肽-1和-2是最近分离出的对μ-阿片受体具有特异性的内源性肽，在转染以表达克隆的大鼠μ-阿片受体的NG108-15细胞中，它们分别以6 nM和9 nM的半数有效浓度（EC50）抑制Ca2+通道电流。另一方面，它们在未转染的NG108-15细胞中未引起反应。结论是，内吗啡肽-1和-2通过选择性激活μ-阿片受体诱导Ca2+通道抑制。
