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

Authors
  • Abarca, Belén
  • Ballesteros, Rafael
  • Bielsa, Patricia
  • Moragues, Juan
  • D'Ocon, Pilar
  • García-Zaragozá, Eugenia
  • Noguera, M Antonia
Type
Published Article
Journal
European Journal of Medicinal Chemistry
Publisher
Elsevier
Publication Date
May 01, 2003
Volume
38
Issue
5
Pages
501–511
Identifiers
PMID: 12767600
Source
Medline
License
Unknown

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.

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