Analgesic effect of a bradykinin antagonist – a 1,4-benzodiazepine-2-one derivative

Aim . To study the analgesic effect of a new 1,4-benzodiazepine-2-one derivative (codenamed PAV-0056) in pain models mice, its anti-inflammatory experimental exudative inflammation rats, and potential ulcerogenic effect. Materials methods A was orally administered polyvinylpyrrolidone (PVP) solution to 192 CD-1 mice weighing 20–25 g 140 Sprague – Dawley rats 250–300 g. The PAV-0056 compound at dose 0.01, 0.1, 1 mg / kg studied murine acute thermal (hot plate test, hot water immersion tail-flick test), chemogenic (formalin visceral spasticity-related (acetic acid-induced writhing test). doses an rat model induced by subplantar administration bradykinin histamine. intact who were injected with 50 four times. compared that diclofenac sodium 10 tramadol 20 kg. Its effects those Results In 0.1 increased response latency 36%, kg, it 46% (p < 0.05). heat stimulation After formalin, 0.01–1 had pronounced effect, as shown decrease number responses 39–55% When intraperitoneally acetic acid solution, reduced frequency writhings 46 57%, respectively; delayed onset first 21% experiments on prevented development did not have histamine-induced inflammation. cause formation gastric ulcers mucosal bleeding. Conclusion derivative, PAV-0056, has thermal, chemogenic, somatic, wide range (0.01–1 kg). are same is selective, depends little suppression inflammatory exudation, caused antagonism. This substance low toxicity does damage mucosa.