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

Authors
Potin, D Parnet, V Teulon, JM Camborde, F Caussade, F Meignen, J Provost, D Cloarec, A
Citation
D. Potin et al., Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics, BIOORG MED, 10(8), 2000, pp. 805-809
Citations number
19
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
8
Year of publication
2000
Pages
805 - 809
Database
ISI
SICI code
0960-894X(20000417)10:8<805:N3APNO>2.0.ZU;2-F
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 s erotonin binding profile, has an interesting antinociceptive activity which is not reversed by naloxone. (C) 2000 Elsevier Science Ltd. All rights res erved.