Effect of 4'-chloro-5-methoxy-3-biphenylylacetic acid (DKA-9) on prostaglandin synthetase.
4'-Chloro-5-methoxy-3-biphenylylacetic acid (DKA-9) was evaluated for its ability to inhibit the conversion of arachidonic acid into prostaglandin E2 and the oxygen uptake on arachidonic acid by sheep seminal vesicle microsomes. DKA-9 inhibited equally the formation of prostaglandin E2 and oxygen uptake at 20 mumol/l or more in a concentration-dependent manner, which suggests a blockade of prostaglandin endoperoxide formation. DKA-9 did not promote time-dependent inactivation of the enzyme and inhibited the enzyme competitively with respect to substrate. Thus, it behaved as a reversible and competitive inhibitor.
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000494:pharmacology; D016861:Cyclooxygenase Inhibitors; D066298:In Vitro Techniques; D008297:Male; D008861:Microsomes / Q000378:metabolism; D010101:Oxygen Consumption / Q000187:drug effects; D010648:Phenylacetates / Q000494:pharmacology*; D011458:Prostaglandins E / Q000378:metabolism; D012669:Seminal Vesicles / Q000378:metabolism; D012756:Sheep; D013997:Time Factors
D000893:Anti-Inflammatory Agents; D001713:Biphenyl Compounds; D016861:Cyclooxygenase Inhibitors; D010648:Phenylacetates; D011458:Prostaglandins E; C006015:DKA 9