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1,4-Dihydropyridines: The Multiple Personalities of a Blockbuster Drug Family

More than 40 years after their introduction in therapy, 1,4-dihydropyridines (DHPs) are still amongst the most prescribed drugs in the world. Though they all share a similar mechanism of action blocking L-type voltage-gated Ca(2+) channels, DHPs differ in crucial pharmacological properties like tiss...

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Detalles Bibliográficos
Autores principales: Cataldi, Mauro, Bruno, Fiorentina
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Università di Salerno 2012
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3728803/
https://www.ncbi.nlm.nih.gov/pubmed/23905059
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author Cataldi, Mauro
Bruno, Fiorentina
author_facet Cataldi, Mauro
Bruno, Fiorentina
author_sort Cataldi, Mauro
collection PubMed
description More than 40 years after their introduction in therapy, 1,4-dihydropyridines (DHPs) are still amongst the most prescribed drugs in the world. Though they all share a similar mechanism of action blocking L-type voltage-gated Ca(2+) channels, DHPs differ in crucial pharmacological properties like tissue selectivity and cardiodepressant activity. This review examines how changes in the DHP structure can modify the pharmacological properties of these drugs and how some of these chemical manipulations have been exploited to obtain clinically more effective molecules. Special emphasis is given to the evidence that L-type Ca(2+) channels are an heterogeneous family and that DHPs with different pharmacological properties differ in their affinity for the different isoforms of this class of channels. Data showing that DHP pharmacological heterogeneity could be in part dependent on the interaction of some of these molecules with ion channels different from the L-type Ca(2+) channels is reviewed as well.
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spelling pubmed-37288032013-07-31 1,4-Dihydropyridines: The Multiple Personalities of a Blockbuster Drug Family Cataldi, Mauro Bruno, Fiorentina Transl Med UniSa Review More than 40 years after their introduction in therapy, 1,4-dihydropyridines (DHPs) are still amongst the most prescribed drugs in the world. Though they all share a similar mechanism of action blocking L-type voltage-gated Ca(2+) channels, DHPs differ in crucial pharmacological properties like tissue selectivity and cardiodepressant activity. This review examines how changes in the DHP structure can modify the pharmacological properties of these drugs and how some of these chemical manipulations have been exploited to obtain clinically more effective molecules. Special emphasis is given to the evidence that L-type Ca(2+) channels are an heterogeneous family and that DHPs with different pharmacological properties differ in their affinity for the different isoforms of this class of channels. Data showing that DHP pharmacological heterogeneity could be in part dependent on the interaction of some of these molecules with ion channels different from the L-type Ca(2+) channels is reviewed as well. Università di Salerno 2012-10-11 /pmc/articles/PMC3728803/ /pubmed/23905059 Text en http://creativecommons.org/licenses/by/2.5/ This is an open-access article distributed under the terms of the Creative Commons Attribution License, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Review
Cataldi, Mauro
Bruno, Fiorentina
1,4-Dihydropyridines: The Multiple Personalities of a Blockbuster Drug Family
title 1,4-Dihydropyridines: The Multiple Personalities of a Blockbuster Drug Family
title_full 1,4-Dihydropyridines: The Multiple Personalities of a Blockbuster Drug Family
title_fullStr 1,4-Dihydropyridines: The Multiple Personalities of a Blockbuster Drug Family
title_full_unstemmed 1,4-Dihydropyridines: The Multiple Personalities of a Blockbuster Drug Family
title_short 1,4-Dihydropyridines: The Multiple Personalities of a Blockbuster Drug Family
title_sort 1,4-dihydropyridines: the multiple personalities of a blockbuster drug family
topic Review
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3728803/
https://www.ncbi.nlm.nih.gov/pubmed/23905059
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