Pham Huu Chanh , B. Lasserre , V. Dossou-Gbete , J. Couquelet , P. Tronche
{"title":"An inhibitor of prostacyclin biosynthesis derived from aminopyridazine","authors":"Pham Huu Chanh , B. Lasserre , V. Dossou-Gbete , J. Couquelet , P. Tronche","doi":"10.1016/0262-1746(87)90019-9","DOIUrl":null,"url":null,"abstract":"<div><p>The effects of 3-dimethylamino 5-(3′ trifluoromethylbenzylidene) 6-methyl (4H)-pyridazine (PC88) on the biosynthesis of PGI<sub>2</sub>, using horse aorta microsomes as a source of enzyme and arachidonic acid as a substrate, were investigated. Under the experimental conditions adopted, PC88 was shown to dosedependently inhibit PGI<sub>2</sub> biosynthesis (ID50 = 6.9×10<sup>−4</sup> M ± 1.87 × 10<sup>−7</sup> M). This inhbitory effect of PC88 was complex: it was of neither competitive nor non-competitive type. 3-dimethylamino 5-(2′,6′-dichlorobenzylidene 6-methyl-(4H)-pyridazine (PC89) enhanced the biosynthesis of PGI<sub>2</sub>. It is worth noticing the replacement of the 2 Cl at carbon atoms 1 and 4 by a CF<sub>3</sub> at carbon atom 2 of the phenol ring. This appears to reverse the activity of the molecule on the synthesis of PGI<sub>2</sub>. PC88 and PC89 were both inhibitors of TXA<sub>2</sub> synthetase.</p></div>","PeriodicalId":20720,"journal":{"name":"Prostaglandins, leukotrienes, and medicine","volume":null,"pages":null},"PeriodicalIF":0.0000,"publicationDate":"1987-11-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/0262-1746(87)90019-9","citationCount":"3","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Prostaglandins, leukotrienes, and medicine","FirstCategoryId":"1085","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/0262174687900199","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 3
Abstract
The effects of 3-dimethylamino 5-(3′ trifluoromethylbenzylidene) 6-methyl (4H)-pyridazine (PC88) on the biosynthesis of PGI2, using horse aorta microsomes as a source of enzyme and arachidonic acid as a substrate, were investigated. Under the experimental conditions adopted, PC88 was shown to dosedependently inhibit PGI2 biosynthesis (ID50 = 6.9×10−4 M ± 1.87 × 10−7 M). This inhbitory effect of PC88 was complex: it was of neither competitive nor non-competitive type. 3-dimethylamino 5-(2′,6′-dichlorobenzylidene 6-methyl-(4H)-pyridazine (PC89) enhanced the biosynthesis of PGI2. It is worth noticing the replacement of the 2 Cl at carbon atoms 1 and 4 by a CF3 at carbon atom 2 of the phenol ring. This appears to reverse the activity of the molecule on the synthesis of PGI2. PC88 and PC89 were both inhibitors of TXA2 synthetase.
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