Antinociceptive effects of SC-39566, an opioid dipeptide arylalkylamide, in the Rhesus monkey.

Abstract

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.

• Authors: D L Hammond, J L Bloss
• Journal: European journal of pharmacology (Eur J Pharmacol) Vol. 231 Issue 2 Pg. 281-5 (Feb 09 1993) ISSN: 0014-2999 [Print] Netherlands
• PMID: 8095901 (Publication Type: Journal Article)

Chemical References

• Analgesics, Opioid
• Dipeptides
• 2,6-dimethyltyrosyl-N-(3-phenylpropyl)alaninamide

Topics

• Analgesics, Opioid (administration & dosage, pharmacology)
• Animals
• Dipeptides (administration & dosage, pharmacology)
• Dose-Response Relationship, Drug
• Electric Stimulation
• Escape Reaction (drug effects)
• Injections, Intramuscular
• Macaca mulatta
• Male
• Skin Physiological Phenomena