<I>CS-600, a new anti-inflammatory agent. Inhibitory activity on prostaglandin biosynthesis</I>
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概要
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CS-600, sodium 2- (4- (2-oxocyclopentan-l-yl methyl) phenyl) propionate, which has potent anti-inflammatory and analgesic activities, showed a weak inhibitory activity to the<I>in vitro</I>PG synthesis with bovine seminal vesicle microsomes (IC<SUB>50</SUB>: 760μM) . Its main metabolite, which was produced by stereospecific reduction of the cyclopentanone moiety to hydroxy cyclopentane, exhibited a potent inhibitory activity (IC<SUB>50</SUB>: 9 μM) to the enzyme. The stereospecific configuration (trans-OH, SRS) was essential for the inhibitory activity. Oral administration of CS-600 to rats markedly decreased the urinary PGE<SUB>2</SUB>and F<SUB>2</SUB>α levels, suggesting that the active metabolite was produced and inhibited PG synthesis<I>in vivo</I>. In a culture system of 3T6 fibroblasts, CS-600 was effectively converted to the active metabolite and inhibited the PGE<SUB>2</SUB>production of the fibroblasts.
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