Paper
Resolution of etodolac and antiinflammatory and prostaglandin synthetase inhibiting properties of the enantiomers.
Published Dec 1, 1983 · C. Demerson, L. Humber, N. Abraham
Journal of medicinal chemistry
78
Citations
0
Influential Citations
Abstract
Etodolac, 1,8-diethyl-1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid, a clinically effective analgesic and antiinflammatory agent, has been resolved via a chromatographic separation of its diastereoisomeric esters with (-)-borneol. The effects of the enantiomers were studied in vitro on prostaglandin synthetase and on adjuvant-induced arthritis in rats. The biochemical and pharmacological results show that virtually all of the effects of etodolac are due to the (+) enantiomer.
Etodolac's analgesic and antiinflammatory effects are mainly due to the (+) enantiomer, which inhibits prostaglandin synthetase and is effective in treating arthritis in rats.
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