Novel 3-(4-piperidinylthio)-1H-indoles as potent nonopioid orally active central analgesics.
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.
Potin
D
D
Laboratoires UPSA, Rueil Malmaison, France. d.potin@cerep.fr
Parnet
V
V
Teulon
J M
JM
Camborde
F
F
Caussade
F
F
Meignen
J
J
Provost
D
D
Cloarec
A
A
D000284:Administration, Oral; D018712:Analgesics, Non-Narcotic / Q000008:administration & dosage / Q000494:pharmacology*; D000818:Animals; D007211:Indoles / Q000008:administration & dosage / Q000494:pharmacology*; D051379:Mice
D018712:Analgesics, Non-Narcotic; D007211:Indoles