About this Biochemistry, Genetics and Molecular Biology article
1,4-Dihydropyridine derivatives as calcium channel modulators: the role of 3-methoxy-flavone moiety by Roberta Budriesi; Alessandra Bisi; Pierfranco Ioan; Angela Rampa; Silvia Gobbi; Federica Belluti; Lorna Piazzi; Piero Valenti; Alberto Chiarini is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
It was earlier recognized that calcium antagonists, and in particular 1,4-dihydropyridines, exhibited distinct cardiovascular profiles. In addition two different splice variants of the L-type calcium channel were found in vascular and cardiac tissues. In this study, novel substituted 1,4-dihydropyridines with a 3-methoxy-flavone moiety were synthesized and structural modifications of the substituents in the dihydropyridine ring of nifedipine were carried out in order to find tissue specific compounds. The negative inotropic, chronotropic and vasorelaxant effects were investigated on guinea-pig left, right atria and aortic strips, respectively. The introduction of an heteroaromatic ring in 4-position of the 1,4-dihydropyridine nucleus led to compounds selective for cardiac tissues. Moreover, different residues in the 1,4-dihydropyridine ring could modulate the chronotropic versus inotropic activity.
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- Author
- Roberta Budriesi; Alessandra Bisi; Pierfranco Ioan; Angela Rampa; Silvia Gobbi; Federica Belluti; Lorna Piazzi; Piero Valenti; Alberto Chiarini
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2005
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)