Functional coupling of μ-receptor-Gαi-tethered proteins in AtT20 cells

被引：2

作者：

Chieng, Billy C. ^{[1
]}

Lee, David J. ^{[1
]}

Du, Yan P. ^{[1
]}

Osborne, Peregrine B. ^{[1
]}

Christie, MacDonald J. ^{[1
,2
]}

Massotte, Dominique ^{[3
]}

机构：

[1] Univ Sydney, Royal N Shore Hosp, Kolling Inst, Pain Management Res Inst, St Leonards, NSW 2065, Australia

[2] Univ Sydney, Royal N Shore Hosp, Brain & Mind Res Inst, St Leonards, NSW 2065, Australia

[3] ULP, INSERM, CNRS,UMR 7104, Inst Genet & Mol & Cellular Biol,Dept Mol Neurobi, Illkirch Graffenstaden, France

来源：

NEUROREPORT | 2008年 / 19卷 / 18期

关键词：

AtT20; calcium current; G-protein; opioid; pertussis toxin; potassium current; mu-receptor; tethered protein;

D O I：

10.1097/WNR.0b013e3283196b55

中图分类号：

Q189 [神经科学];

学科分类号：

071006 ;

摘要：

Opioid efficacy on p-receptor may be influenced by various G(i/o)-G-protein subunits interacting with intracellular face of receptor. Pertussis toxin-insensitive G alpha(i1) and G alpha(i2) subunits tethered with p-receptor were stably transfected into AtT20 cells to (i) determine coupling of different alpha-subunits on opioid efficacy, and (ii) determine coupling to downstream effectors, for example, calcium and potassium channels. After pertussis toxin, stimulation of [(35)S]GTP-gamma-S incorporation persisted. Both constructs were able to couple to native calcium and potassium channels, with endomorphins 1 and 2 equally effective. However, pertussis toxin abolished opioid actions on calcium and potassium channels suggesting strong coupling to endogenous G-proteins, and that differences in coupling efficacy to G alpha(i1) and G alpha(i2) previously observed are restricted to initial step of signaling cascade. NeuroReport 19:1793-1796 (C) 2008 Wolters Kluwer Health vertical bar Lippincott Williams & Wilkins.

引用

页码：1793 / 1796

页数：4

共 13 条

[1] Opioid agonists have different efficacy profiles for G protein activation, rapid desensitization, and endocytosis of mu-opioid receptors [J].