[Nature of the interaction of voltaren and other pyrazolone and aniline derivatives with prostaglandin endoperoxide synthetase].
A study was made of the nature and mechanism of interaction of voltaren, butadion, analgin, phenacetin and paracetamol with endoperoxide prostaglandin synthetase (PGH-synthetase) of sheep vesicular glands. Activity of the enzyme was measured by polarography with the aid of a Clark's electrode. Butadion and analgin reversibly inhibited PGH-synthetase at concentrations of the order of 10(-4) M, whereas voltaren at those of the order of 10(-6) M. As regards the mechanism of action, butadion and analgin are competitive inhibitors of PGH-synthetase in respect to arachidonic acid and uncompetitive inhibitors in respect to the electron donor adrenaline. Phenacetin administered at concentrations up to 4 X 10(-2) M did not inhibit PGH-synthetase, whereas paracetamol (10(-3)-10(-2) M) increased its catalytic activity, apparently due to the electron donor properties.
D000082:Acetaminophen / Q000494:pharmacology; D000814:Aniline Compounds / Q000494:pharmacology*; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D016861:Cyclooxygenase Inhibitors; D004008:Diclofenac / Q000494:pharmacology*; D004177:Dipyrone / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D066298:In Vitro Techniques; D007700:Kinetics; D008297:Male; D008861:Microsomes / Q000201:enzymology; D010615:Phenacetin / Q000494:pharmacology; D010648:Phenylacetates / Q000494:pharmacology*; D010653:Phenylbutazone / Q000494:pharmacology; D011720:Pyrazoles / Q000494:pharmacology*; D012669:Seminal Vesicles / Q000201:enzymology; D012756:Sheep
D000814:Aniline Compounds; D000893:Anti-Inflammatory Agents; D016861:Cyclooxygenase Inhibitors; D010648:Phenylacetates; D011720:Pyrazoles; D004008:Diclofenac; D000082:Acetaminophen; D004177:Dipyrone; D010615:Phenacetin; D010653:Phenylbutazone
O kharaktere vzaimodeĭstviia vol'tarena i nekotorykh proizvodnykh pirazolona i anilina s éndoperoksiprostaglandinsintetazoĭ.