Journal
MOLECULES
Volume 24, Issue 23, Pages -Publisher
MDPI
DOI: 10.3390/molecules24234298
Keywords
dantrolene; drug repurposing; multitarget activity; neuroprotection; carnitine/acylcarnitine carrier; Alzheimer's disease
Funding
- Italian Ministry for Education and Research (Fondo di Finanziamento per le Attivita Base di Ricerca FFABR 2017)
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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.
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