beta-Funaltrexamine antagonizes the analgesic effects of mu and kappa agonists in the formalin test.
The formalin test assesses the behavioral response of an animal to minor tissue injury-induced pain. Opioid antinociception in this test has been suggested to depend largely on activation of kappa receptors but mu agonists are also potent in reducing pain behavior. The present study used the irreversible mu antagonist, beta-funaltrexamine (beta-FNA), to examine the role of mu receptor activation in this test. beta-FNA given intracranially 4 h before testing fully blocked the effects of morphine and attenuated the effects of ethylketocyclazocine and U50,488H. The results do not support a role for kappa receptors in antinociception in the formalin test. Instead, mu and, possibly, delta receptors are involved.
Abbott
F V
FV
Department of Psychiatry, McGill University, Montreal, Quebec, Canada.
D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D000818:Animals; D004305:Dose-Response Relationship, Drug; D016314:Ethylketocyclazocine / Q000494:pharmacology; D005557:Formaldehyde; D008297:Male; D009020:Morphine / Q000494:pharmacology; D009271:Naltrexone / Q000031:analogs & derivatives* / Q000494:pharmacology; D009292:Narcotic Antagonists; D010146:Pain / Q000188:drug therapy / Q000503:physiopathology; D011759:Pyrrolidines / Q000494:pharmacology; D051381:Rats; D011957:Receptors, Opioid / Q000187:drug effects*; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D014554:Urination / Q000187:drug effects
D009292:Narcotic Antagonists; D011759:Pyrrolidines; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D017450:Receptors, Opioid, mu; D005557:Formaldehyde; D016314:Ethylketocyclazocine; D009271:Naltrexone; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; C024524:beta-funaltrexamine; D009020:Morphine