Synthetic Studies on Enkephalin Analogs. I. Potent Analgesic Activity of H-Tyr-D-Ala-Gly-Phe-NHNH-CO-R (R=Lower Alkyl)
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概要
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Thirty tetrapeptide hydrazide analogs of enkephalin, H-Tyr-D-Ala-Gly-Phe-NHN-(R_1)-R_2 (R_1,R_2=H, alkyl or acyl), were synthesized. The analgesic activities of these peptides were tested in mice after intravenous or subcutaneous injection, and compared with that of morphine. Among the analogs synthesized, the tetrapeptide acyl-hydrazide analog, H-Tyr-D-Ala-Gly-Phe-NHNH-CO-R (R=lower alkyl), was the most active and showed analgesic activity ten times more potent than that of the tetrapeptide amide analog, H-Tyr-D-Ala-Gly-Phe-NH_2 and half as potent as that of morphine. On the basis of these results, structure-activity relations in the hydrazide part of enkephalin analogs of this new type are discussed.
- 公益社団法人日本薬学会の論文
- 1981-12-25
著者
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藤野 政彦
Chemistry Laboratories Central Research Division Takeda Chemical Industries Ltd.
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藤野 政彦
Central Research Division, Takeda Chemical Industries Ltd.
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品川 進
Central Research Division, Takeda Chemical Industries, Ltd.
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石井 治光
Central Research Division, Takeda Chemical Industries, Ltd.
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石井 治光
武田薬品工業株式会社中央研究所
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川井 清尚
Central Research Division Takeda Chemical Industries Ltd.
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