Antinociceptive effects of SC-39566, an opioid dipeptide arylalkylamide, in the Rhesus monkey.
This study evaluated the antinociceptive activity of an opioid dipeptide arylalkylamide, SC-39566 (2,6-dimethyl-L-tyrosinyl-D-alanyl-(3-phenyl-l-propyl)- amide), in the Rhesus monkey using the discrete trial, intermittent shock titration paradigm. I.m. administration of doses ranging from 12 to 24 mg/kg produced a dose-dependent increase in escape threshold and a dose-dependent rightward shift in the frequency distribution of responses to suprathreshold electrocutaneous stimuli. Although equivalent with respect to efficacy, SC-39566 was only one-fourth to one-sixth as potent as morphine in this paradigm. This study is the first report of the antinociceptive activity of an opioid dipeptide arylalkylamide after systemic administration in the primate.
Hammond
D L
DL
Department of Anesthesia and Critical Care, University of Chicago, IL 60637.
Bloss
J L
JL
D000701:Analgesics, Opioid / Q000008:administration & dosage / Q000494:pharmacology*; D000818:Animals; D004151:Dipeptides / Q000008:administration & dosage / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004558:Electric Stimulation; D004924:Escape Reaction / Q000187:drug effects; D007273:Injections, Intramuscular; D008253:Macaca mulatta; D008297:Male; D012879:Skin Physiological Phenomena
D000701:Analgesics, Opioid; D004151:Dipeptides; C072400:2,6-dimethyltyrosyl-N-(3-phenylpropyl)alaninamide