Pharmacological studies of 2-(5H-(1)benzopyrano(2, 3-b)pyridin-7-yl) propionic acid (Y-8004) (1) Anti-inflammatory, analgesic and antipyretic activities

Abstract

A newly synthesized anti-inflammatory agent, Y-8004 [2-(5H-[1]benzopyrano[2,3-b]pyridin-7-yl) propionic acid] possessed greater antiinflammatory activity than did indomethacin (IM) on inflammatory response such as UV erythema in guinea pigs, carrageenin edema, evans blue and carrageenin-induced pleuritis and acetic acid-induced peritonitis in rats. The action of Y-8004 was to equal that of IM in cases of granuloma formation around a cotton pellet and the development of adjuvant arthritis in rats, but Y-8004 was only half as effective as IM regarding exudation in the granuloma pouch. The agent was effective in alleviating established adjuvant arthritis. The anti-inflammatory activity was not mediated by stimulation of the adrenals, and glucocorticoid-like activity could not be demonstrated. Analgesic and antipyretic activities were to the same degree as seen with IM, and the analgesic property of Y-8004 was considered to be peripheral, as is the case with IM. The ulcerogenic activity of Y-8004 was observed mainly in the jejunum andileum of therat, but compared to IM, there were considerable differences between the ulcerogenic and the effective doses. As Y-8004 has a wider therapeutic margin than IM, this non-steroidal anti-inflammatory agent should be quite useful for clinical purposes.