质量水平
检测方案
≥98% (HPLC)
形式
powder
旋光性
[α]/D -150 to -175, c = 0.5 in chloroform-d
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
2-8°C
生化/生理作用
ML375 is an orally active, brain-penetrant, potent and M5 subtype-selective muscarinic acetylcholine receptor (mAChR) negative allosteric modulator (NAM) (IC50 = 300/790 nM against 10 μM NMS-induced Ca2+ mobilization in h/r M5-transfected CHO cells; h/r M1-M4 IC50 >30 μM) that reduces N-methylscopolamine (NMS) ML5 dissociation rate without competing against NMS for receptor binding. M375 shows in vivo efficacy in rat models of substances addiction (cocaine, ethanol, oxycodone) with excellent multispecies pharmacokinetic properties.
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Patrick R Gentry et al.
Journal of medicinal chemistry, 56(22), 9351-9355 (2013-10-30)
A functional high throughput screen and subsequent multidimensional, iterative parallel synthesis effort identified the first muscarinic acetylcholine receptor (mAChR) negative allosteric modulator (NAM) selective for the M5 subtype. ML375 is a highly selective M5 NAM with submicromolar potency (human M5
Alice E Berizzi et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 43(7), 1510-1517 (2018-02-28)
Despite the cost to both individual and society, alcohol use disorders (AUDs) remain a major health risk within society, and both relapse and heavy drinking are still poorly controlled with current medications. Here we demonstrate for the first time that
Robert W Gould et al.
ACS chemical neuroscience, 10(8), 3740-3750 (2019-07-04)
Opioid use disorder (OUD) is a debilitating neuropsychiatric condition characterized by compulsive opioid use, dependence, and repeated relapse after periods of abstinence. Given the high risk of developing OUD following prescription opioid use, the continued need for opioid-induced analgesia, and
Barak W Gunter et al.
Addiction biology, 23(5), 1106-1116 (2017-10-19)
Cocaine use disorder (CUD) remains a debilitating health problem in the United States for which there are no Food and Drug Administration-approved treatment options. Accumulating anatomical and electrophysiological evidence indicates that the muscarinic acetylcholine receptor (mAChR) subtype 5 (M5 )
Alice E Berizzi et al.
Molecular pharmacology, 90(4), 427-436 (2016-07-28)
Recently, the first subtype-selective allosteric modulators of the M5 muscarinic acetylcholine receptor (mAChR) have been described, but their molecular mechanisms of action remain unknown. Using radioligand-binding and functional assays of inositol phosphate (IP) accumulation and Ca(2+) mobilization in a recombinant
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