产品信息
抗原名称
5-HT2A Receptor
商品描述
Lumateperone tosylate (ITI-007 tosylate) is a 5-HT2A receptor antagonist (Ki = 0.54 nM), a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM), and a SERT blocker (Ki = 61 nM).
分子量
565.7
纯度
98%
可溶性
DMSO : 100 mg/mL (176.77 mM; Need ultrasonic)
外观
off-white solid
In vitro(体外研究)
Lumateperone also possesses an affinity for the D1 receptor (Ki: 52 nM) and weak affinity for the α1A- and α1B-adrenergic receptors (Ki: 173 nM at α1) and D4 receptor. Lumateperone does not significantly bind to the 5-HT2B, 5-HT2C, H1, or mACh receptors. Lumateperone shows a 60-fold difference in its affinities for the 5-HT2A and D2 receptors, which is far greater than that of most or all existing atypical antipsychotics, such as risperidone (12-fold), olanzapine (12.4-fold), and aripiprazole (0.18-fold).
In vivo(体内研究)
It is thought that this property may improve the effectiveness and reduce the side effect profile of Lumateperone relative to currently-available antipsychotics, a hypothesis which is supported by the observation of minimal catalepsy in mice treated with Lumateperone.
背景
别名
卢美哌隆对甲苯磺酸盐
分子式
C31H36FN3O4S
CAS号
1187020-80-9
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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