Partial agonistic action of endomorphins in the mouse spinal cord.
The partial agonistic properties of endogenous mu-opioid peptides endomorphin-1 and endomorphin-2 for G-protein activation were determined in the mouse spinal cord, monitoring the increases in guanosine-5'-o-(3-[35S]thio)triphosphate binding. The G-protein activation induced by endogenous opioid peptide beta-endorphin in the spinal cord was significantly, but partially, attenuated by co-incubation with endomorphin-1 or endomorphin-2. The data indicates that endomorphin-1 and endomorphin-2 are endogenous partial agonists for mu-opioid receptor in the mouse spinal cord.
Mizoguchi
H
H
Department of Anesthesiology, Medical College of Wisconsin, 8701 Watertown Plank Road, Milwaukee, WI 53226, USA. toyama@mcw.edu
Wu
H E
HE
Narita
M
M
D000701:Analgesics, Opioid / Q000494:pharmacology*; D000818:Animals; D019204:GTP-Binding Proteins / Q000187:drug effects / Q000378:metabolism; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000494:pharmacology; D008297:Male; D051379:Mice; D009842:Oligopeptides / Q000494:pharmacology*; D011957:Receptors, Opioid / Q000819:agonists*; D017450:Receptors, Opioid, mu / Q000819:agonists; D013116:Spinal Cord / Q000187:drug effects*
D000701:Analgesics, Opioid; D009842:Oligopeptides; D011957:Receptors, Opioid; D017450:Receptors, Opioid, mu; C105293:endomorphin 1; D016244:Guanosine 5'-O-(3-Thiotriphosphate); C105294:endomorphin 2; D019204:GTP-Binding Proteins