产品
编 号:F043337
分子式:C18H28ClN3O3
分子量:369.89
产品类型
结构图
CAS No: 1135242-13-5
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产品详情
生物活性:
VU0357017 hydrochloride (CID-25010775) is a potent, selective and brain-penetrant allosteric agonist of M1 muscarinic acetylcholine receptor, with an EC50 of 477 nM. VU0357017 hydrochloride is highly selective for M1 and has no activity at M2-M5 up to the highest concentrations tested (30 μM). VU0357017 hydrochloride can be used for the research of Alzheimer’s disease and schizophrenia.
体内研究:
VU0357017 hydrochloride (1-10 mg/kg,腹腔注射) 逆转东莨菪碱引起的情境恐惧条件反射的破坏。Animal Model:Male Sprague?Dawley rats (380-420 g) were pretreated with scopolamine
Dosage:1, 3, 10 mg/kg
Administration:A single i.p.
Result:Produced a significant reversal of the scopolamine-induced deficits at a dose of 10 mg/kg.
体外研究:
VU0357017 hydrochloride 在 CHO 细胞中对 M1 (Ki=9.91 μM) 的选择性高于 M2-M5 mAChRs (K i=21.4,55.3,35.0,and 50.0 μM,respectively)。 VU0357017 hydrochloride (1 nM-100 μM) 在 CHO 细胞中呈浓度依赖性诱导钙释放和 ERK 磷酸化。