ML 218 hydrochloride |
رقم الكتالوجGC15386 |
هيدروكلوريد ML 218 هو مثبط فعال وانتقائي وفعال عن طريق الفم من النوع T Ca2+ (Cav3.1 ، Cav3.2 ، Cav3.3) مع IC50s من 310 نانومتر و 270 نانومتر لـ Cav3.2 و Cav3.3 ، على التوالي.
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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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