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Article

A Prospective Repurposing of Dantrolene as a Multitarget Agent for Alzheimer’s Disease

1
Department of Pharmacy-Drug Sciences, University of Bari Aldo Moro, Via E. Orabona 4, 70125 Bari, Italy
2
Institute of Biomembranes, Bioenergetics and Molecular Biotechnologies (IBIOM), National Research Council (CNR), via Amendola 122/O, 70126 Bari, Italy
*
Author to whom correspondence should be addressed.
These authors contributed equally to this work.
Academic Editors: Diego Muñoz-Torrero, F. Javier Luque and Marçal Pastor-Anglada
Molecules 2019, 24(23), 4298; https://doi.org/10.3390/molecules24234298
Received: 23 October 2019 / Revised: 20 November 2019 / Accepted: 21 November 2019 / Published: 25 November 2019
(This article belongs to the Special Issue Facing Novel Challenges in Drug Discovery)
The orphan drug dantrolene (DAN) is the only therapeutic treatment for malignant hyperthermia (MH), a pharmacogenetic pathology affecting 0.2 over 10,000 people in the EU. It acts by inhibiting ryanodine receptors, which are responsible for calcium recruitment in striatal muscles and brain. Because of its involvement in calcium homeostasis, DAN has been successfully investigated for its potential as neuroprotecting small molecule in several animal models of Alzheimer’s disease (AD). Nevertheless, its effects at a molecular level, namely on putative targets involved in neurodegeneration, are still scarcely known. Herein, we present a prospective study on repurposing of DAN involving, besides the well-known calcium antagonism, inhibition of monoamine oxidase B and acetylcholinesterase, cytoprotection from oxidative insult, and activation of carnitine/acylcarnitine carrier, as concurring biological activities responsible for neuroprotection. View Full-Text
Keywords: dantrolene; drug repurposing; multitarget activity; neuroprotection; carnitine/acylcarnitine carrier; Alzheimer’s disease dantrolene; drug repurposing; multitarget activity; neuroprotection; carnitine/acylcarnitine carrier; Alzheimer’s disease
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MDPI and ACS Style

Bolognino, I.; Giangregorio, N.; Pisani, L.; de Candia, M.; Purgatorio, R.; Tonazzi, A.; Altomare, C.D.; Cellamare, S.; Catto, M. A Prospective Repurposing of Dantrolene as a Multitarget Agent for Alzheimer’s Disease. Molecules 2019, 24, 4298. https://doi.org/10.3390/molecules24234298

AMA Style

Bolognino I, Giangregorio N, Pisani L, de Candia M, Purgatorio R, Tonazzi A, Altomare CD, Cellamare S, Catto M. A Prospective Repurposing of Dantrolene as a Multitarget Agent for Alzheimer’s Disease. Molecules. 2019; 24(23):4298. https://doi.org/10.3390/molecules24234298

Chicago/Turabian Style

Bolognino, Isabella, Nicola Giangregorio, Leonardo Pisani, Modesto de Candia, Rosa Purgatorio, Annamaria Tonazzi, Cosimo D. Altomare, Saverio Cellamare, and Marco Catto. 2019. "A Prospective Repurposing of Dantrolene as a Multitarget Agent for Alzheimer’s Disease" Molecules 24, no. 23: 4298. https://doi.org/10.3390/molecules24234298

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