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G i1 and G oA differentially determine kinetic efficacies of agonists for κ‐opioid receptor
Author(s) -
Kohno Masayuki,
Fukushima Nobuyuki,
Yoshida Akira,
Ueda Hiroshi
Publication year - 2000
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/s0014-5793(00)01495-2
Subject(s) - gtpgammas , receptor , opioid receptor , agonist , chemistry , pharmacology , opioid , population , μ opioid receptor , g protein , g protein coupled receptor , medicine , endocrinology , biology , biochemistry , environmental health
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 i1 β 1 γ 2 or KOR plus Gα oA β 1 γ 2 , there was no significant difference between both preparations in the K i values of various κ‐opioid ligands for the displacement of [ 3 H]U69593 binding. However, a marked difference in the rank order of agonists to stimulate [ 35 S]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.