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Opiate-like peptides. Part XI. 2-[2-phenyl-1,3-indandionyl]--amides of enkephalin analogs. Synthesis and analgesic activity

Nedev, H.; Rolka, K.; Minchev, S.; Kupryszewski, G.; Kolasa, K.; Kleinrok, Z.

Polish Journal of Pharmacology and Pharmacy 40(3): 303-311

1988

ISSN/ISBN: 0301-0244
PMID: 3241770
Document Number: 307798
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.

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