Gi1 and GoA differentially determine kinetic efficacies of agonists for κ‐opioid receptor

FEBS Letters

Fukushima, Nobuyuki¹  Ueda, Hiroshi¹  Kohno, Masayuki¹  Yoshida, Akira¹ 

[1] Department of Molecular Pharmacology and Neuroscience, Nagasaki University School of Pharmaceutical Sciences, 1-14 Bunkyo-machi, Nagasaki 852-8521, Japan

关键词: κ-Opioid receptor;    G protein;    Reconstitution;   

DOI  :  10.1016/S0014-5793(00)01495-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

We examined the diversity of single receptor function by measuring receptor–G protein coupling in the baculovirus–Sf21 expression system. In comparative studies using Sf21 cell membranes expressing κ-opioid receptor (KOR) plus Gα_i1β₁γ₂ or KOR plus Gα_oAβ₁γ₂, there was no significant difference between both preparations in the K _i values of various κ-opioid ligands for the displacement of [³H]U69593 binding. However, a marked difference in the rank order of agonists to stimulate [³⁵S]GTPγS binding was observed between both preparations. These findings suggest that agonist efficacy is dependent on the population of different G proteins expressed in various tissues.

【 授权许可】

Unknown