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

Bioorg Med Chem Lett. 2000 Apr 17;10(8):805-9. doi: 10.1016/s0960-894x(00)00102-5.

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.

MeSH terms

  • Administration, Oral
  • Analgesics, Non-Narcotic / administration & dosage
  • Analgesics, Non-Narcotic / pharmacology*
  • Animals
  • Indoles / administration & dosage
  • Indoles / pharmacology*
  • Mice

Substances

  • Analgesics, Non-Narcotic
  • Indoles