Opiate-like peptides. Part XII. Synthesis and some biological properties of Met-enkephalin analogues modified in position 2 by D-alanyl residue in positions 2 and 4 by 3-(2-naphthyl)-D-alanyl residue.
Nine Met-enkephalin analogues containing D-alanyl residue in position 2 and/or 3-(2-naphthyl)-D-alanyl residue in positions 2 and 4 have been obtained. Their biological activity has been determined after intracerebroventricular administration to rats. Almost all compounds appeared strongly toxic causing the death of the animals. Only [D-2-Nal2,4, Met5-OMe]--enkephalin exerted an analgesic effect after the administration in the form of fine suspension.
Rolka
K
K
Institute of Chemistry, University of Gdańsk, Kotowice, Poland.
Obuchowicz
E
E
Kupryszewski
G
G
Gołba
K
K
Herman
Z S
ZS
D000700:Analgesics; D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D055598:Chemical Phenomena; D002621:Chemistry; D004744:Enkephalin, Methionine / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology* / Q000633:toxicity; D007202:Indicators and Reagents; D007276:Injections, Intraventricular; D008297:Male; D009043:Motor Activity / Q000187:drug effects; D051381:Rats; D011919:Rats, Inbred Strains
D000700:Analgesics; D007202:Indicators and Reagents; D004744:Enkephalin, Methionine