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Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics

…, V Parnet, JM Teulon, F Camborde, F Caussade…

文献索引:Potin, Dominique; Parnet, Veronique; Teulon, Jean-Marie; Camborde, Francoise; Caussade, Francois; Meignen, Joelle; Provost, Daniel; Cloarec, Alix Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 8 p. 805 - 809

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被引用次数: 12

摘要

A series of 3-(4-piperidinylthio)-1H-indoles was synthesized and evaluated in mice in the phenylbenzoquinone (PBQ)-induced writhing and hot plate tests. Most of these compounds are good analgesics with activities comparable to that of morphine. Among them compound 1i (UP 237-61), which has a strong serotonin binding profile, has an interesting antinociceptive activity which is not reversed by naloxone.