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Differential coupling of the human cannabinoid receptors hCB1R and hCB2R to the G-protein Galpha i2beta 1gamma 2

Nickl, Kathrin ; Gardner, Eric E. ; Geiger, Sarah ; Heilmann, Jörg ; Seifert, Roland



Abstract

Human cannabinoid receptors 1 (hCB1R) and 2 (hCB2R) are expressed in the CNS and couple to Gi/Go-proteins. The aim of this study was to compare coupling of hCB1R and hCB2R to Galpha i2beta 1gamma 2 in Sf9 insect cells. High-affinity agonist binding at hCB1R, but not at hCB2R, was resistant to guanine nucleotides. HCB1R activated Galpha i2beta 1gamma 2 much more rapidly than hCB2R in the ...

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