A dose-ratio comparison of mu and kappa agonists in formalin and thermal pain.
The effects of putative mu and kappa agonists, with and without naloxone, were compared in the formalin and tail flick tests in rats. The mu agonist sufentanil was more potent in the tail flick test than the formalin test while the opposite was true for the kappa agonist ethylketocyclazocine (EKC). MR2034 was equipotent in the two tests and in the tail flick test, analgesia decreased at high doses. The naloxone (0.1 mg/kg) dose-ratios (DR) for sufentanil and EKC were 3 to 7 times larger for the tail flick test than the formalin test. From this and other DR studies it is argued that in thermal pain tests, opioid analgesia is mediated primarily by mu receptors while in non thermal tests kappa effects predominate.
D000698:Analgesia; D000818:Animals; D001575:Benzomorphans / Q000494:pharmacology; D003496:Cyclazocine / Q000031:analogs & derivatives / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D016314:Ethylketocyclazocine; D005283:Fentanyl / Q000031:analogs & derivatives / Q000494:pharmacology; D005557:Formaldehyde; D006358:Hot Temperature; D008297:Male; D009270:Naloxone / Q000494:pharmacology; D010146:Pain; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects / Q000502:physiology*; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D017409:Sufentanil
D001575:Benzomorphans; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D005557:Formaldehyde; D009270:Naloxone; C032478:MR 2034; D016314:Ethylketocyclazocine; D017409:Sufentanil; D003496:Cyclazocine; D005283:Fentanyl