Nociceptin receptor-mediated Ca2+ channel inhibition and its desensitization in NG108-15 cells

被引：27

作者：

Morikawa, H ^{[1
]}

Fukuda, K ^{[1
]}

Mima, H ^{[1
]}

Shoda, T ^{[1
]}

Kato, S ^{[1
]}

Mori, K ^{[1
]}

机构：

[1] Kyoto Univ Hosp, Dept Anesthesia, Sakyo Ku, Kyoto 6068507, Japan

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1998年 / 351卷 / 02期

关键词：

nociceptin receptor; Ca2+; channel; N-type; desensitization; NG108-15; cells; patch damp;

D O I：

10.1016/S0014-2999(98)00306-9

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

It has been shown that the membrane of hybrid NG108-15 neuroblastoma X glioma cells contains a high-affinity binding site for nociceptin. In the present study, we first demonstrated the expression of nociceptin receptor mRNA in NG108-15 cells. Application of nociceptin to NG108-15 cells produced a concentration-dependent (EC50 = 29 nM) inhibition of Ca2+ channel currents in a pertussis toxin-sensitive fashion. This nociceptin-induced inhibition of Ca2+ channel currents was prevented in the presence of omega-conotoxin GVIA, a blocker of the N-type Ca2+ channel, and had both voltage-dependent and -independent components. Prolonged application of nociceptin elicited homologous desensitization of the inhibition with a time constant of 5.3 min. These results indicate that the nociceptin receptor is coupled to the N-type Ca2+ channel via pertussis toxin-sensitive G proteins in NG108-15 cells and that this coupling is associated with rapid and homologous desensitization. (C) 1998 Elsevier Science B.V. All rights reserved.

引用

页码：247 / 252

页数：6

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