Gi1 and GoA differentially determine kinetic efficacies of agonists for κ‐opioid receptor
- 4 May 2000
- journal article
- Published by Wiley in FEBS Letters
- Vol. 473 (1) , 101-105
- https://doi.org/10.1016/s0014-5793(00)01495-2
Abstract
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 Gαi1β1γ2 or KOR plus GαoAβ1γ2, there was no significant difference between both preparations in the Ki 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 tissuesKeywords
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