The influence of some 3-amino-2-pyrazoline derivatives on cyclooxygenase and lipoxidase activities. 1982

J Robak, and Z Duniec

The influence of 3-amino-1-[m-(trifluoromethyl)-phenyl]-2-pyrazoline (BW 755C), 1-(3,3-diphenylpropyl)-3-amino-5-methyl-2-pyrazoline (KD 785) and 1-(3,3-diphenylpropyl)-3-amino-2-pyrazoline (KD 679) on cyclooxygenase and lipoxidase activities has been studied. All three compounds inhibited soybean and platelet lipoxidase activity. BW 755C was a much stronger inhibitor than KD compounds. The tested compounds stimulated oxygen consumption by cyclooxygenase from ram seminal vesicle microsomes in the presence of 100 microM of arachidonic acid in the range of concentrations between 30 and 300 microM and increased PGE2 generation in these experimental conditions. Radiochemical studies showed that BW 755C had been a stimulator of cyclooxygenase in higher (100 microM) substrate concentrations but, in agreement with a previous report it acted as an inhibitor of this enzyme when substrate concentration was 1.6 microM. Probably this component acted as a free radical scavenger.

UI MeSH Term Description Entries
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
D010101 Oxygen Consumption The rate at which oxygen is used by a tissue; microliters of oxygen STPD used per milligram of tissue per hour; the rate at which oxygen enters the blood from alveolar gas, equal in the steady state to the consumption of oxygen by tissue metabolism throughout the body. (Stedman, 25th ed, p346) Consumption, Oxygen,Consumptions, Oxygen,Oxygen Consumptions
D011453 Prostaglandins A group of compounds derived from unsaturated 20-carbon fatty acids, primarily arachidonic acid, via the cyclooxygenase pathway. They are extremely potent mediators of a diverse group of physiological processes. Prostaglandin,Prostanoid,Prostanoids
D011720 Pyrazoles Azoles of two nitrogens at the 1,2 positions, next to each other, in contrast with IMIDAZOLES in which they are at the 1,3 positions.
D001792 Blood Platelets Non-nucleated disk-shaped cells formed in the megakaryocyte and found in the blood of all mammals. They are mainly involved in blood coagulation. Platelets,Thrombocytes,Blood Platelet,Platelet,Platelet, Blood,Platelets, Blood,Thrombocyte
D006736 Horses Large, hoofed mammals of the family EQUIDAE. Horses are active day and night with most of the day spent seeking and consuming food. Feeding peaks occur in the early morning and late afternoon, and there are several daily periods of rest. Equus caballus,Equus przewalskii,Horse, Domestic,Domestic Horse,Domestic Horses,Horse,Horses, Domestic
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
D001091 Arachidonate Lipoxygenases Enzymes catalyzing the oxidation of arachidonic acid to hydroperoxyarachidonates. These products are then rapidly converted by a peroxidase to hydroxyeicosatetraenoic acids. The positional specificity of the enzyme reaction varies from tissue to tissue. The final lipoxygenase pathway leads to the leukotrienes. EC 1.13.11.- . Arachidonic Acid Lipoxygenase,Lipoxygenase, Arachidonic Acid,Lipoxygenases, Arachidonate
D001095 Arachidonic Acids Eicosatetraenoic Acids,Acids, Arachidonic,Acids, Eicosatetraenoic

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