| abstract |
The application relates to the use of 5-HT2Breceptor antagonists and more particularly benzylideneaminoguanidines of formula (I) or salts thereof for the treatment of inflammation and pain. R1and R2are chloro, methoxy or hydrogen; R3is chloro or methoxy and R4is chloro, hydrogen or nitro; and at least one of R1-R3is chloro and another of R1-R3is methoxy. The examples relate to N-(2-chloro-3,4-dimethoxybenzylideneamino)guanidine acetate for the treatment of inflammation, in particular rheumatoid arthritis, and pain. Further 5-HT antagonists tested include 4-(4-fluoro-l-naphthyl)-6-isopropylpyrimidin-2-alpine (RS 127445) or 6-chloro-5-methyl-N-[6-[(2-methylpyridin-3-yl)oxy]pyridin-3-yl]indoline-1-carboxamide (SB 242084). Also outlined is a method of identifying test compounds having an anti-inflammatory effect, comprising the steps of (i) contacting a test compound with a 5-HT2Breceptor in vitro, and (ii) determining the binding capacity of the test compound with a Kiof less than 1μm or preferably equal to/less than 0.5µm is identified as a compound having an anti-inflammatory effect. |