Studies on Analgesic Oligopeptides. IV. Synthesis and Analgesic Activity of N-Terminal Shorter Analogs of [D-Arg^2] Dermorphin and Des-Tyr^1-Dermorphin Analogs

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Des-Tyr^1-dermorphin, des-Tyr^1-[D-Arg^2] dermorphin, and the N-terminal di-, tri-, tetra- and hexapeptide amides of [D-Arg^2] dermorphin were synthesized by a conventional solution method and their analgesic activities were assayed by means of the tail pressure test after subcutaneous administration (s. c.) to mice. The des-Tyr^1 analogs of both dermorphin and [D-Arg^2] dermorphin did not show analgesic activity even at a dose of up to 50 mg/kg, s. c. The N-terminal tetrapeptide amide, H-Tyr-D-Arg-Phe-Gly-NH_2,showed extremely potent activity, being 31 times more active than morphine on a molar basis, whereas the N-terminal tri- and dipeptide amides showed no activity even at a dose of up to 40 mg/kg, s. c.
社団法人日本薬学会の論文
1985-11-25