Gz coupling to the rat kappa-opioid receptor.
We have expressed the cloned rat kappa-opioid receptor in human embryonic kidney 293 cells and studied the ability of kappa-selective ligands to inhibit adenylyl cyclase. In transfected 293 cells, activation of the kappa-opioid receptor by U50,488 and the dynorphins resulted in the inhibition of cAMP accumulation. The inhibitory response was sensitive to pertussis toxin and highly selective for kappa-agonists; neither mu- nor delta-opioids were able to activate the kappa-opioid receptor. Upon co-transfection with the alpha subunit of Gz, inhibition of cAMP accumulation by kappa-agonist became refractory to pertussis toxin, indicating that the kappa-opioid receptor can couple to both G(i) and Gz proteins.
Lai
H W
HW
Department of Biology, Hong Kong University of Science and Technology, Clear Water Bay, Kowloon.
Minami
M
M
Satoh
M
M
Wong
Y H
YH
D037361:Adenylate Cyclase Toxin; D000067956:Adenylyl Cyclase Inhibitors; D000818:Animals; D002478:Cells, Cultured; D003001:Cloning, Molecular; D019204:GTP-Binding Proteins / Q000378:metabolism*; D006801:Humans; D037342:Pertussis Toxin; D051381:Rats; D017473:Receptors, Opioid, kappa / Q000235:genetics / Q000378:metabolism*; D010566:Virulence Factors, Bordetella / Q000494:pharmacology; D014981:Xenopus
D037361:Adenylate Cyclase Toxin; D000067956:Adenylyl Cyclase Inhibitors; D017473:Receptors, Opioid, kappa; D010566:Virulence Factors, Bordetella; D037342:Pertussis Toxin; D019204:GTP-Binding Proteins