The human muscarinic M1 acetylcholine receptor, when express in CHO cells, activates and downregulates both Gq alpha and G11 alpha equally and non-selectively.
CHO cells express both of the phosphoinositidase C-linked G-proteins Gq and G11. G11 alpha is some 2.5-fold more highly expressed than Gq alpha in membranes of these cells. Following transfection and stable expression of CHO cells with DNA encoding the human muscarinic M1 acetylcholine (HM1) receptor, chronic treatment of the cells with the cholinergic agonist carbachol resulted in down-regulation of membrane levels of both Gq alpha and G11 alpha. Dose-response curves to carbachol produced identical EC50 values for agonist-induced down-regulation of the two G-proteins and both were down-regulated with the same time course. These data indicate that the HM1 receptor interacts with the activates both Gq alpha and G11 alpha equivalently and non-selectively in a whole cell system in which the receptor has access to both G-proteins.
Department of Biochemistry, University of Glasgow, Scotland, UK.
I
I
Mullaney
F M
FM
Mitchell
J F
JF
McCallum
N J
NJ
Buckley
G
G
Milligan
D000818:Animals; D016466:CHO Cells; D002217:Carbachol / Q000494:pharmacology; D006224:Cricetinae; D004305:Dose-Response Relationship, Drug; D015536:Down-Regulation; D019204:GTP-Binding Proteins / Q000145:classification / Q000235:genetics / Q000378:metabolism*; D006801:Humans; D011976:Receptors, Muscarinic / Q000235:genetics / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism
D011976:Receptors, Muscarinic; D011994:Recombinant Proteins; D002217:Carbachol; D019204:GTP-Binding Proteins