Biomaterial Database

Inhibition of prostaglandin synthase by pirprofen. Studies with sheep seminal vesicle enzyme. 1975

E C Ku, and J M Wasvary

1. Pirprofen, racemic 2-[3-chloro-4(3-pyrrolinyl) phenyl] propionic acid, was evaluated for its ability to inhibit the conversion of arachidonic acid into prostaglandin E2 by sheep seminal vesicle prostaglandin synthase in vitro. 2. The compound proved to be a potent inhibitor with a Ki value of about 1.2 muM. Like indomethacin, aspirin and certain other non-steroidal anti-inflammatory drugs, pirprofen inhibited the enzyme competively with respect to substrate. Unlike most non-steroidal anti-inflammatory drugs, however, pirprofen did not promote time-dependent inactivation of the enzyme. It behaved as a competitive, reversible inhibitor, whereas most of the other agents acted as competitive, irreversible inhibitors. 3. The results suggest that inhibition of prostaglandin synthesis accounts in large part for the pharmacological effects of pirprofen.

UI	MeSH Term	Description	Entries
D007213	Indomethacin	A non-steroidal anti-inflammatory agent (NSAID) that inhibits CYCLOOXYGENASE, which is necessary for the formation of PROSTAGLANDINS and other AUTACOIDS. It also inhibits the motility of POLYMORPHONUCLEAR LEUKOCYTES.	Amuno,Indocid,Indocin,Indomet 140,Indometacin,Indomethacin Hydrochloride,Metindol,Osmosin
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D008297	Male		Males
D008861	Microsomes	Artifactual vesicles formed from the endoplasmic reticulum when cells are disrupted. They are isolated by differential centrifugation and are composed of three structural features: rough vesicles, smooth vesicles, and ribosomes. Numerous enzyme activities are associated with the microsomal fraction. (Glick, Glossary of Biochemistry and Molecular Biology, 1990; from Rieger et al., Glossary of Genetics: Classical and Molecular, 5th ed)	Microsome
D010666	Phenylpropionates	Derivatives of 3-phenylpropionic acid, including its salts and esters.
D011758	Pyrroles	Azoles of one NITROGEN and two double bonds that have aromatic chemical properties.	Pyrrole
D006899	Mixed Function Oxygenases	Widely distributed enzymes that carry out oxidation-reduction reactions in which one atom of the oxygen molecule is incorporated into the organic substrate; the other oxygen atom is reduced and combined with hydrogen ions to form water. They are also known as monooxygenases or hydroxylases. These reactions require two substrates as reductants for each of the two oxygen atoms. There are different classes of monooxygenases depending on the type of hydrogen-providing cosubstrate (COENZYMES) required in the mixed-function oxidation.	Hydroxylase,Hydroxylases,Mixed Function Oxidase,Mixed Function Oxygenase,Monooxygenase,Monooxygenases,Mixed Function Oxidases,Function Oxidase, Mixed,Function Oxygenase, Mixed,Oxidase, Mixed Function,Oxidases, Mixed Function,Oxygenase, Mixed Function,Oxygenases, Mixed Function
D000818	Animals	Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA.	Animal,Metazoa,Animalia
D000963	Antimetabolites	Drugs that are chemically similar to naturally occurring metabolites, but differ enough to interfere with normal metabolic pathways. (From AMA Drug Evaluations Annual, 1994, p2033)	Antimetabolite
D001095	Arachidonic Acids		Eicosatetraenoic Acids,Acids, Arachidonic,Acids, Eicosatetraenoic