Kinetic studies in isolated organs: tools to design analgesic peptides and to analyze their receptor effects.
The opioid activities of peptide and non-peptide narcotics were studied in longitudinal muscle strip of guinea pig ileum (GPI) and in mouse vas deferens (MVD). The comparison of agonist activities of peptides found in GPI and MVD offered the opportunity to predict the presence but not the magnitude of potential analgesic activity. The kinetics of the antagonism between naltrexone and different types of agonists were also determined in these systems. Using C-6 epimers of naltrexone, it was found that the site of opiate receptors recognizing the information provided by the C-6 substituent of naltrexone are different in GPI and MVD.
D000701:Analgesics, Opioid / Q000378:metabolism* / Q000494:pharmacology; D000818:Animals; D005260:Female; D006168:Guinea Pigs; D007082:Ileum / Q000378:metabolism*; D008297:Male; D051379:Mice; D009271:Naltrexone / Q000378:metabolism; D010455:Peptides / Q000378:metabolism* / Q000494:pharmacology; D011957:Receptors, Opioid / Q000187:drug effects*; D014649:Vas Deferens / Q000378:metabolism*
D000701:Analgesics, Opioid; D010455:Peptides; D011957:Receptors, Opioid; D009271:Naltrexone