Roluperidone 是一种新型环酰胺衍生物,对5-HT2A和sigma-2受体具有高亲和力,Ki分别为 7.53 和 8.19 nM。
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Roluperidone is a novel cyclic amide derivative. It has high equipotent affinities for 5-HT2A and σ2 receptors (Ki of 7.53 nM and 8.19 nM for 5-HT2A and σ2).
体外活性
Roluperidone shows binding affinity for α1-adrenergic receptors. Which low or no affinity for muscarinic, cholinergic, and histaminergic receptors. Although Roluperidone (CYR-101) has no affinities for pre- or postsynaptic dopaminergic receptors, it is probable that sigma-2 receptors are implicated in the modulation of dopamine and glutamatergic pathways and in calcium neuronal modulation[1].
Cas No.
359625-79-9
分子式
C22H23FN2O2
分子量
366.43
别名
MIN-101;CYR-101;MT-210
储存和溶解度
H2O:< 0.1 mg/mL (insoluble)
DMSO:33.33 mg/mL (90.96 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years