Design and synthesis of a metabolically stable and potent antitussive agent, a novel δ opioid receptor antagonist, TRK-851

…, A Saitoh, K Nakao, N Izumimoto, H Matsuura…

Index: Sakami, Satoshi; Kawai, Koji; Maeda, Masayuki; Aoki, Takumi; Fujii, Hideaki; Ohno, Hiroshi; Ito, Tsuyoshi; Saitoh, Akiyoshi; Nakao, Kaoru; Izumimoto, Naoki; Matsuura, Hirotoshi; Endo, Takashi; Ueno, Shinya; Natsume, Kazuto; Nagase, Hiroshi Bioorganic and Medicinal Chemistry, 2008 , vol. 16, # 17 p. 7956 - 7967

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Citation Number: 21

Abstract

We have previously reported on antitussive effect of (5R, 9R, 13S, 14S)-17- cyclopropylmethyl-6, 7-didehydro-4, 5-epoxy-5′, 6′-dihydro-3-methoxy-4′ H-pyrrolo [3, 2, 1-ij] quinolino [2′, 1′: 6, 7] morphinan-14-ol (1b) methanesulfonate (TRK-850), a selective δ opioid receptor antagonist which markedly reduced the number of coughs in a rat cough model. We designed TRK-850 based on naltrindole (NTI), a typical δ opioid ...