Safinamide's potential in treating nondystrophic myotonias: Inhibition of skeletal muscle voltage-gated sodium channels and skeletal muscle hyperexcitability in vitro and in vivo.
Current-clamp
In vivo model
Muscle excitability
Myotonia
Patch-clamp
Safinamide
Voltage-gated sodium channels
Journal
Experimental neurology
ISSN: 1090-2430
Titre abrégé: Exp Neurol
Pays: United States
ID NLM: 0370712
Informations de publication
Date de publication:
06 2020
06 2020
Historique:
received:
29
10
2019
revised:
14
03
2020
accepted:
19
03
2020
pubmed:
25
3
2020
medline:
31
12
2020
entrez:
25
3
2020
Statut:
ppublish
Résumé
The antiarrhythmic sodium-channel blocker mexiletine is used to treat patients with myotonia. However, around 30% of patients do not benefit from mexiletine due to poor tolerability or suboptimal response. Safinamide is an add-on therapy to levodopa for Parkinson's disease. In addition to MAOB inhibition, safinamide inhibits neuronal sodium channels, conferring anticonvulsant activity in models of epilepsy. Here, we investigated the effects of safinamide on skeletal muscle hNa
Identifiants
pubmed: 32205118
pii: S0014-4886(20)30118-7
doi: 10.1016/j.expneurol.2020.113287
pii:
doi:
Substances chimiques
Benzylamines
0
NAV1.4 Voltage-Gated Sodium Channel
0
safinamide
90ENL74SIG
Alanine
OF5P57N2ZX
Types de publication
Journal Article
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
113287Informations de copyright
Copyright © 2020 Elsevier Inc. All rights reserved.
Déclaration de conflit d'intérêts
Declaration of Competing Interest Charlotte Keywood, Elsa Melloni, Gloria Padoani, Silvia Vailati are employees of Zambon S.p.A. and Carla Caccia is a consultant of Zambon S.p.A. The International patent application PCT/EP2019/063733 entitled “Safinamide for treating myotonia” was filed on May 28, 2019 in the name of Zambon S.p.A. Designated inventors are Desaphy J.F., Pierno S., Conte D., Melloni E., Vailati S., Padoani G., and Caccia C.