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ML 218 hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML 218 hydrochloride图片
CAS NO:1346233-68-8
规格:98%
分子量:405.79
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
T-type calcium channels inhibitor
CAS:1346233-68-8
分子式:C19H26Cl2N2O.HCl
分子量:405.79
纯度:98%
存储:Store at -20°C

Background:

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].


参考文献:
[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