当前位置： SCI文献检索 > EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > Opposite vascular activity of (R)-apomorphine and its oxidised derivatives. Endothelium-dependent vasoconstriction induced by the auto-oxidation metabolite.

Opposite vascular activity of (R)-apomorphine and its oxidised derivatives. Endothelium-dependent vasoconstriction induced by the auto-oxidation metabolite.

Abstract：

:We have synthetised a series of oxidised apomorphine derivatives (orto and para quinones 2-5), in order to analyse their vascular activity. We have performed radioligand binding assays on rat cortical membranes and functional studies on rat aortic rings. Instead the relaxant activity exhibited by (R)-apomorphine, o-quinones 2, 4, show contractile activity dependent on endothelium in rat aortic rings. Compound 2, the main metabolite of (R)-apomorphine auto-oxidation, was the product which showed enhanced contractile activity by a complex mechanism related to activation of Ca(2+) channels through release and/or inhibition of endothelial factors. Moreover, this compound disrupts the endothelial function as shows the lack of response to acetylcholine observed in vessels pretreated with it.

journal_name

Eur J Med Chem

journal_title

European journal of medicinal chemistry

authors

Abarca B,Ballesteros R,Bielsa P,Moragues J,D'Ocon P,García-Zaragozá E,Noguera MA

doi

10.1016/s0223-5234(03)00057-6

subject

Has Abstract

pub_date

2003-05-01 00:00:00

pages

501-11

issue

5

eissn

0223-5234

issn

1768-3254

pii

S0223523403000576

journal_volume

38

pub_type

杂志文章

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