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Functional coupling of mu-receptor-Galphai-tethered proteins in AtT20 cells.

Abstract : Opioid efficacy on mu-receptor may be influenced by various Gi/o-G-protein subunits interacting with intracellular face of receptor. Pertussis toxin-insensitive Galphai1 and Galphai2 subunits tethered with mu-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 [35S]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 Galphai1 and Galphai2 previously observed are restricted to initial step of signaling cascade.
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Contributor : Maité Peney <>
Submitted on : Tuesday, May 26, 2009 - 4:56:44 PM
Last modification on : Thursday, June 17, 2021 - 3:16:03 PM




Billy Chieng, David Lee, Yan Du, Peregrine Osborne, Macdonald Christie, et al.. Functional coupling of mu-receptor-Galphai-tethered proteins in AtT20 cells.. NeuroReport, Lippincott, Williams & Wilkins, 2008, 19 (18), pp.1793-6. ⟨10.1097/WNR.0b013e3283196b55⟩. ⟨inserm-00384590⟩



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