Article
Tight association of the human Mel(1a)-melatonin receptor and G(i): precoupling and constitutive activity.
Molecular pharmacology - 1 Nov 1999
Roka F, Brydon L, Waldhoer M, Strosberg A D, Freissmuth M, Jockers R, Nanoff C
Abstract excerpt
If stably expressed in human embryonic kidney (HEK)293 cells, the human Mel(1a)-melatonin receptor activates G(i)-dependent, pertussis toxin-sensitive signaling pathways, i.e., inhibition of adenylyl cyclase and stimulation of phospholipase Cbeta; the latter on condition that G(q) is coactivated. The antagonist luzindole blocks the effects of melatonin and acts as an inverse agonist at the Mel(1a) receptor in...
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