Opiate-like peptides. Part XI. 2-[2-phenyl-1,3-indandionyl]--amides of enkephalin analogs. Synthesis and analgesic activity.
Four enkephalin analogs containing C-terminal 2-amino-2-phenyl-1,3-indandione residue were prepared: [Met-NHPID5]--enkephalin (E3), [D-Ala2,Met-NHPID5]--enkephalin (E4), [Leu-NHPID5]--enkephalin (E5), [D-Ala2,Leu-NHPID5]--enkephalin (E6). Their analgesic activities were assayed by three in vivo tests: the "hot plate" method, the reaction to electric painful stimulus and the writhing syndrome test. Neurotoxicity effects were determined by the rota-rod test. The most pronounced analgesic effect was induced by compounds with D-Ala in position 2, particularly in the "hot plate" test.
Nedev
H
H
Pedagogical Institute, Shoumen, Bulgaria.
Rolka
K
K
Minchev
S
S
Kupryszewski
G
G
Kolasa
K
K
Kleinrok
Z
Z
D000818:Animals; D004558:Electric Stimulation; D004723:Endorphins / Q000138:chemical synthesis* / Q000494:pharmacology; D004745:Enkephalins / Q000031:analogs & derivatives*; D006358:Hot Temperature; D051379:Mice; D010146:Pain / Q000517:prevention & control; D010147:Pain Measurement; D011930:Reaction Time
D004723:Endorphins; D004745:Enkephalins