产品说明书

Roluperidone

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Chemical Structure| 359625-79-9 同义名 : MIN-101;MT-210;CYR-101
CAS号 : 359625-79-9
货号 : A709477
分子式 : C22H23FN2O2
纯度 : 98%
分子量 : 366.429
MDL号 : MFCD28502826
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 35 mg/mL(95.52 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Roluperidone (CYR-101), a novel cyclic amide compound, exhibits high and equal potency for 5-HT2A and sigma-2 receptors, with binding constants (Ki) of 7.53 nM for 5-HT2A and 8.19 nM for sigma-2 receptors[1]. Roluperidone (CYR-101) demonstrates affinity to α1-adrenergic receptors, showing minimal to negligible binding to muscarinic, cholinergic, and histaminergic receptors. Despite lacking affinity for both pre- and postsynaptic dopaminergic receptors, Roluperidone (CYR-101) is likely involved in the regulation of dopamine and glutamatergic signaling pathways through sigma-2 receptor interaction, also affecting neuronal calcium modulation[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.73mL

0.55mL

0.27mL

13.65mL

2.73mL

1.36mL

27.29mL

5.46mL

2.73mL
参考文献

[1]Davidson M, et al. Efficacy and Safety of MIN-101: A 12-Week Randomized, Double-Blind, Placebo-Controlled Trial of a New Drug in Development for the Treatment of Negative Symptoms in Schizophrenia. Am J Psychiatry. 2017 Jul 28:appiajp201717010122.