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Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics
D Potin1, V Parnet, J M Teulon
1Laboratoires UPSA, Rueil Malmaison, France. d.potin@cerep.fr
Bioorganic & Medicinal Chemistry Letters
|April 27, 2000
Abstract:
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.