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Discovery of new phthalazinones as vasodilator agents and novel pharmacological tools to study calcium channels

dc.contributor.authorMunin J.
dc.contributor.authorQuezada E.
dc.contributor.authorViña D.
dc.contributor.authorUriarte E.
dc.contributor.authorDelogu G.L.
dc.contributor.authorGil-Longo J.
dc.date.accessioned2020-09-02T22:23:45Z
dc.date.available2020-09-02T22:23:45Z
dc.date.issued2019
dc.identifier10.4155/fmc-2018-0250
dc.identifier.citation11, 3, 179-191
dc.identifier.issn17568919
dc.identifier.urihttps://hdl.handle.net/20.500.12728/5469
dc.descriptionAim: Hydralazine has led to the synthesis of phthalazinone derivatives which induce vasorelaxation. Methods: A new series of 2-(aminoalkyl)-4-benzyl-2H-phthalazin-1-one derivatives has been synthesized to study their vasorelaxant activity. Results: At the highest-studied concentration, most of the new compounds relaxed the denuded aortic rings precontracted with phenylephrine by 72.9-85.7. Compound 25 (C25) suppressed almost totally the contractile effects of phenylephrine, high KCl concentration, ionomycin and caffeine related to the activation of Ca channels, whereas its inhibitory effect was reversed with high CaCl2 concentrations. Conclusion: Vasodilator effects of C25 appear to be due exclusively to the reversible blockage of different calcium channels. As broad range calcium channel blocker, C25 seems to be suitable as a pharmacological tool for calcium channel research. © 2019 2019 Newlands Press.
dc.language.isoen
dc.publisherFuture Medicine Ltd.
dc.subjectcalcium channel blockers
dc.subjectendothelium
dc.subjectphthalazinone derivatives
dc.subjectrat aortic rings
dc.subjectsynthesis
dc.subjectvasorelaxant activity
dc.subject2 (2 aminoethyl) 4 (3',5' dimethoxybenzyl) 2h phthalazin 1 one
dc.subject2 (aminoalkyl) 4 benzyl 2h phthalazin 1 one derivative
dc.subjectcaffeine
dc.subjectcalcium channel
dc.subjectcalcium chloride
dc.subjecthydralazine
dc.subjectionomycin
dc.subjectphenylephrine
dc.subjectphthalazinone derivative
dc.subjectpotassium chloride
dc.subjectunclassified drug
dc.subjectvasodilator agent
dc.subjectaorta
dc.subjectArticle
dc.subjectconcentration response
dc.subjectcontrolled study
dc.subjectdrug activity
dc.subjectdrug development
dc.subjectdrug synthesis
dc.subjectpriority journal
dc.subjectvasodilatation
dc.titleDiscovery of new phthalazinones as vasodilator agents and novel pharmacological tools to study calcium channels
dc.typeArticle


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