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

Analgesic and Psychotropic Effects of a New Bradykinin Antagonist

A E Aliforenko  1   2 , V S Motov  1 , V V Bykov  3   4 , A V Bykova  1 , V I Pavlovsky  1 , V V Larchenko  1   2 , V A Khazanov  1 , A I Vengerovskii  2
Affiliations

Analgesic and Psychotropic Effects of a New Bradykinin Antagonist

A E Aliforenko et al. Bull Exp Biol Med. 2024 Mar.

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.

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