Ca2+ channel inhibition by endomorphins via the cloned mu-opioid receptor expressed in NG108-15 cells.
Endomorphin-1 and -2, recently isolated endogenous peptides specific for the mu-opioid receptor, inhibited Ca2+ channel currents with EC50 of 6 and 9 nM, respectively, in NG108-15 cells transformed to express the cloned rat mu-opioid receptor. On the other hand, they elicited no response in nontransfected NG108-15 cells. It is concluded that endomorphin-1 and -2 induce Ca2+ channel inhibition by selectively activating the mu-opioid receptor.
Mima
H
H
Department of Anesthesia, Kyoto University Hospital, Japan.
Morikawa
H
H
Fukuda
K
K
Kato
S
S
Shoda
T
T
Mori
K
K
D000701:Analgesics, Opioid / Q000494:pharmacology*; D000818:Animals; D001932:Brain Neoplasms / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000494:pharmacology*; D005910:Glioma / Q000378:metabolism; D009447:Neuroblastoma / Q000378:metabolism; D009842:Oligopeptides / Q000494:pharmacology*; D051381:Rats; D017450:Receptors, Opioid, mu / Q000819:agonists / Q000096:biosynthesis / Q000378:metabolism*; D011994:Recombinant Proteins / Q000378:metabolism; D014407:Tumor Cells, Cultured
D000701:Analgesics, Opioid; D002121:Calcium Channel Blockers; D009842:Oligopeptides; D017450:Receptors, Opioid, mu; D011994:Recombinant Proteins; C105293:endomorphin 1; C105294:endomorphin 2