Pharmacology of 4-benzyol-1-indancarboxylic acid (TAI-901) and 4-(4-methylbenzoyl)-1-indancarboxylic acid (TAI-908).
Pharmacological studies on the derivatives of 1-indancarboxylic acid yielded 4-benzoyl-1-indancarboxylic acid (TAI-901) and 4-(4-methylbenzoyl)-1-indancarboxylic acid (TAI-908). The relative potency (R.P.) of TAI-901 and TAI-908 assessed in parallel line assays (indomethacin - 1) demonstrated that both compounds were highly analgesic against various noxious stimuli induced in experimental animals. R.P. values of TAI-901 were 1.0, 1.7, 4.4 and 2.8 in the phenylquinone writhing, acetic acid writhing, adjuvant arthritic pain and urate arthritic pain tests, respectively. R.P. values of TAI-908 were 1.6, 2.0, 4.7 and 7.0, respectively, in these tests. Both compounds were more inhibitory than indomethacin against acute inflammation, but less inhibitory against chronic inflammation. The inhibitory activities of TAI-901 and TAI-908 on the prostaglandin biosynthesis by microsomes of rabbit renal medulla were 2.2 and 2.6 times that of indomethacin. TAI-901 was 1/3.8 1/7.1, and TAI-908 was 1/16.7 and 1/12.5 as toxic as indomethacin in male rats and mice, respectively.
D000700:Analgesics / Q000494:pharmacology*; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal; D004285:Dogs; D005260:Female; D005767:Gastrointestinal Diseases / Q000139:chemically induced; D006168:Guinea Pigs; D007189:Indans / Q000494:pharmacology*; D007192:Indenes / Q000494:pharmacology*; D007213:Indomethacin / Q000494:pharmacology; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D011453:Prostaglandins / Q000096:biosynthesis; D011817:Rabbits; D051381:Rats; D014456:Ulcer / Q000139:chemically induced
D000700:Analgesics; D000894:Anti-Inflammatory Agents, Non-Steroidal; D007189:Indans; D007192:Indenes; D011453:Prostaglandins; C033924:4-benzoyl-1-indancarboxylic acid; C033925:4-(4-methylbenzoyl)-1-indancarboxylic acid; D007213:Indomethacin