In vivo studies with ICI 154,129, a putative delta receptor antagonist.
We studied the in vivo pharmacology of ICI 154,129, a new antagonist that is claimed to show selectivity for delta opiate receptors. At s.c. doses of 30 and 100 mg/kg, ICI 154,129 had no marked effect on the gastrointestinal transit of a charcoal meal in mice. In this test, ICI 154,129 reversed the inhibitory action of metkephamid (a proposed delta receptor agonist) but not that of levorphanol. ICI 154,129 was proconvulsant in the mouse picrotoxin potentiation test; the dose-response curve had a low ceiling and was biphasic. Naloxone (1 mg/kg, s.c.) enhanced the proconvulsant action of ICI 154,129 (40 mg/kg, s.c.) by an unknown mechanism.
D000818:Animals; D003292:Convulsants; D004357:Drug Synergism; D004743:Enkephalin, Leucine / Q000031:analogs & derivatives* / Q000494:pharmacology; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives / Q000494:pharmacology; D005769:Gastrointestinal Motility / Q000187:drug effects; D007981:Levorphanol / Q000494:pharmacology; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D009294:Narcotics / Q000494:pharmacology*; D010852:Picrotoxin / Q000494:pharmacology; D051381:Rats; D011919:Rats, Inbred Strains; D011957:Receptors, Opioid / Q000187:drug effects*; D017465:Receptors, Opioid, delta; D012640:Seizures / Q000503:physiopathology
D003292:Convulsants; D004743:Enkephalin, Leucine; D004744:Enkephalin, Methionine; D007981:Levorphanol; D009294:Narcotics; D010852:Picrotoxin; D011957:Receptors, Opioid; D017465:Receptors, Opioid, delta; C036405:ICI 154129; C028208:metkephamid