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Title: Inhibitory effect of carvedilol in the high-conductance state of the mitochondrial permeability transition pore
Authors: Oliveira, Paulo J. 
Coxito, Pedro M. 
Rolo, Anabela P. 
Santos, Dario L. 
Palmeira, Carlos M. 
Moreno, António J. M. 
Issue Date: 2001
Citation: European Journal of Pharmacology. 412:3 (2001) 231-237
Abstract: The mitochondrial permeability transition is a widely studied, but poorly understood, phenomenon in mitochondrial bioenergetics. It has been recognised that this phenomenon is related to the opening of a protein pore in the inner mitochondrial membrane, and that opening of this pore is the cause of some forms of mitochondrial dysfunction. In this work, we propose that carvedilol, a multi-role cardioprotective compound, may act as an inhibitor of the high-conductance state of the mitochondrial permeability transition pore, a conclusion supported by the finding that carvedilol provides differential protection against mitochondrial swelling in sucrose and KCl-based media, and that it is unable to protect against calcium-induced depolarisation of the mitochondrial membrane. We also show that carvedilol inhibits the oxidation of mitochondrial thiol groups and that, beyond causing a slight depression of the membrane potential, it has no inhibitory effect on mitochondrial calcium uptake.
DOI: 10.1016/S0014-2999(01)00745-2
Rights: openAccess
Appears in Collections:FCTUC Ciências da Vida - Artigos em Revistas Internacionais

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