| CAS NO: | 1346233-68-8 |
| 规格: | 98% |
| 分子量: | 405.79 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
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
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