Abstract
The inhibition of prostaglandin biosynthesis by SL-573 (1-cyclopropylmethyl-4-phenyl-6-methoxy -2-(1H)-quinazolinone), indomethacin. and aspirin was determined by the selective extraction method of prostaglandins. using bovine seminal vesicle microsomes as enzyme sources and arachidonic acid-1-[ 14C] as a substrate. SL-573 was found to inhibit the prostaglandin biosynthesis. The relative inhibitory potencies of indomethacin. SL-573. and aspirin were 1000. 227, and 1.0, respectively. SL-573. however, differed from other drugs in the nature of the inhibition. The inhibition of SL-573 was reversible, while that of indomethacin and aspirin was irreversible and progressed time-dependently. Furthermore. SL-573 was found to prevent the progressive increase of the irreversible inhibition of indomethacin and aspirin. On the basis of such findings, the lack of the gastrointestinal side-effect of SL-573 was discussed.
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