A comparison of the anticonvulsant effects of two systemically active enkephalin analogues in rats.
FK-33,824 (Tyr-D-Ala-Gly-MePhe-Met(O)-ol) and metkephamid (Tyr-D-Ala-Gly-Phe-N(Me)Met-CONH2; LY 127623) are two parenterally active synthetic analogues of the endogenous morphinomimetic pentapeptide, [Met5]-enkephalin. Acute s.c. administration of each analogue raised the seizure threshold in a dose-related manner in rats challenged with flurothyl, a volatile convulsant. The anticonvulsant action was antagonized by a low dose of naloxone (0.10 mg/kg s.c.). FK-33,824 and metkephamid can therefore be classified with typical mu-receptor agonists such as morphine and etorphine in this procedure.
D000818:Animals; D000927:Anticonvulsants; D005405:D-Ala(2),MePhe(4),Met(0)-ol-enkephalin; D004305:Dose-Response Relationship, Drug; D004723:Endorphins / Q000494:pharmacology*; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives*; D004745:Enkephalins / Q000494:pharmacology*; D005481:Flurothyl / Q000494:pharmacology; D008297:Male; D009270:Naloxone / Q000494:pharmacology; D051381:Rats; D012640:Seizures / Q000139:chemically induced
D000927:Anticonvulsants; D004723:Endorphins; D004745:Enkephalins; D009270:Naloxone; D004744:Enkephalin, Methionine; D005405:D-Ala(2),MePhe(4),Met(0)-ol-enkephalin; D005481:Flurothyl; C028208:metkephamid