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

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Opioid efficacy on μ-receptor may be influenced by various Gi/o-G-protein subunits interacting with intracellular face of receptor. Pertussis toxin-insensitive Gαi1 and Gαi2 subunits tethered with μ-receptor were stably transfected into AtT20 cells to (i) determine coupling of different α-subunits on opioid efficacy, and (ii) determine coupling to downstream effectors, for example, calcium and potassium channels. After pertussis toxin, stimulation of [35S]GTP-γ-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 Gαi1 and Gαi2 previously observed are restricted to initial step of signaling cascade.

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