NS9283 是有效的(α4)3(β2)2烟碱型ACh受体的正向变构调节剂。NS9283在一系列神经系统疾病中有研究价值,如注意力缺陷多动障碍、精神分裂症、帕金森病和阿尔茨海默病。
产品描述
NS9283, a positive allosteric modulator selective for the α4β2 form, reduces ethanol consumption.
体外活性
NS9283 increased the potency of varenicline to activate and desensitize α4β2?nAChRs in vitro without affecting other known targets of varenicline[2].
体内活性
In male and female C57BL/6J mice, NS9283 (10 mg/kg) reduced ethanol intake in a two-bottle choice, intermittent drinking procedure without affecting saccharin intake, ethanol-induced incoordination or ethanol-induced loss of the righting reflex. Subthreshold doses of NS9283 (2.5 mg/kg) plus varenicline (0.1 mg/kg) synergistically reduced ethanol intake in both sexes. Finally, despite having no aversive valence of its own, NS9283 enhanced ethanol-conditioned place aversion[2].
Cas No.
913830-15-6
分子式
C14H8N4O
分子量
248.24
别名
NS-9283;NS 9283;NS9283
储存和溶解度
DMSO:3.06 mg/ml (12.31 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years