Analgesic and Psychotropic Effects of a New Bradykinin Antagonist

Bull Exp Biol Med. 2024 Mar;176(5):581-584. doi: 10.1007/s10517-024-06071-6. Epub 2024 May 9.

Abstract

A bradykinin B1 receptors antagonist PAV-0056, an 1,4-benzodiazepin-2-one derivative, intragastrically administrated to mice at doses of 0.1 and 1 mg/kg causes analgesia in the "formalin test" not inferior to that of diclofenac sodium (10 mg/kg) and tramadol (20 mg/kg). PAV-0056 at doses of 0.1 and 10 mg/kg has no anxiolytic and central muscle relaxant effects in mice and does not damage the gastric mucosa in rats. Based on the results of the conditioned place preference test, PAV-0056 also does not induce addiction in mice.

Keywords: 1,4-benzodiazepin-2-one; analgesic effect; potential neuropsychotropic effects; risk of ulcerogenic effect.

MeSH terms

  • Analgesics* / pharmacology
  • Animals
  • Anti-Anxiety Agents / pharmacology
  • Bradykinin / analogs & derivatives
  • Bradykinin / pharmacology
  • Bradykinin B1 Receptor Antagonists / pharmacology
  • Diclofenac / pharmacology
  • Gastric Mucosa / drug effects
  • Gastric Mucosa / metabolism
  • Male
  • Mice
  • Pain Measurement / drug effects
  • Pain Measurement / methods
  • Psychotropic Drugs / pharmacology
  • Rats
  • Rats, Wistar
  • Tramadol / pharmacology