ML 218 hydrochloride |
Catalog No.GC15386 |
Le chlorhydrate de ML 218 est un inhibiteur puissant, sélectif et oralement actif des canaux Ca2+ de type T (Cav3.1, Cav3.2, Cav3.3) avec des CI50 de 310 nM et 270 nM pour Cav3.2 et Cav3.3, respectivement.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1346233-68-8
Sample solution is provided at 25 µL, 10mM.
ML218 is a selective T-type calcium channel inhibitor with IC50s of 270 and 310 nM for Cav3.3 and Cav3.2 in electrophysiology assay, respectively.
ML218 (CID 45115620) inhibits Cav3.1, Cav3.2, Cav3.3[1].
Electrophysiology studies in STN neurons demonstrate robust effects of ML218 on the inhibition of T-type calcium current, inhibition of low threshold spike, and rebound burst activity. ML218 was found to be orally efficacious in a dose-dependent manner in a preclinical Parkinson’s disease model, haloperidol-induced catalepsy, and comparable to clinically validated A2A antagonism[1]. ML218 reaches a peak cerebrospinal fluid concentration 1-2 hrs after s.c. administration. No effects of ML218 on cardiac rhythmicity is found in electrocardiographic studies. ML218 does not have antiparkinsonian effects in MPTP-treated parkinsonian monkeys, due at least in part, to the agent’s sedative effects[2].
References:
[1]. Xiang Z, et al. The Discovery and Characterization of ML218: A Novel, Centrally Active T-Type Calcium Channel Inhibitor with Robust Effects in STN Neurons and in a Rodent Model of Parkinson's Disease. ACS Chem Neurosci. 2011 Dec 21;2(12):730-742.
[2]. https://www.ncbi.nlm.nih.gov/pubmed/22368764
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