An analysis of naltrexone and naloxone's possible agonistic actions in the dog.
Naltrexone (0.01-2.0 mg/kg, i.v.) produced dose-dependent EEG slowing in the conscious dog as did morphine (0.5-8 mg/kg, i.v.) and fentanyl (5-20 micrograms/kg, i.v.). However, the dose-response curve for naltrexone was not parallel to the morphine or fentanyl dose-response curves. Morphine and fentanyl but not naltrexone also produced dose-dependent miosis and increased the skin twitch reflex latency. When administered into the fourth cerebral ventricle naltrexone (60 micrograms), morphine (80 micrograms) and ethylketazocine (30 micrograms) produced EEG slowing. Again, naltrexone did not alter the skin twitch latency whereas morphine lengthened it and ethylketazocine reduced it. The pharmacological profiles obtained from different routes of administration indicate that naltrexone is clearly different from morphine, fentanyl and ethylketazocine. However, naltrexone may act as a partial agonist in the production of EEG slowing at a previously unidentified opioid receptor.
Wettstein
J G
JG
Martin
W R
WR
D000701:Analgesics, Opioid / Q000494:pharmacology; D000818:Animals; D003496:Cyclazocine / Q000031:analogs & derivatives / Q000494:pharmacology; D004285:Dogs; D004357:Drug Synergism; D004569:Electroencephalography; D016314:Ethylketocyclazocine; D005071:Evoked Potentials / Q000187:drug effects; D005260:Female; D005283:Fentanyl / Q000494:pharmacology; D009020:Morphine / Q000494:pharmacology; D009270:Naloxone / Q000494:pharmacology*; D009271:Naltrexone / Q000494:pharmacology*; D011930:Reaction Time / Q000187:drug effects; D012018:Reflex / Q000187:drug effects*; D012025:Reflex, Pupillary / Q000187:drug effects*
D000701:Analgesics, Opioid; D009270:Naloxone; D016314:Ethylketocyclazocine; D009271:Naltrexone; D009020:Morphine; D003496:Cyclazocine; D005283:Fentanyl