SB 243213

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SB 243213 是一种口服有效的，选择性的，高亲和力的 5-HT2C 受体拮抗剂，对人 5-HT2C 受体的 pKi 为 9.37，pKb 为 9.8。SB 243213 对多种神经递质受体、酶和离子通道具有超过 100 倍的选择性。SB 243213 具有改善的抗焦虑特性，有用于精神分裂症和运动障碍的潜力。

SB 243213 is an orally active, selective and high-affinity 5-HT2C receptor antagonist with a pKi of 9.37 and a pKb of 9.8 for human 5-HT2C receptor. SB 243213 shows greater than a 100-fold selectivity over a wide range of neurotransmitter receptors, enzymes and ion channels. SB 243213 has improved anxiolytic profile and has the potential for schizophrenia and motor disorders.

SB 243213 shows little affinity (pKi<6) for cloned human 5-HT1A, 5-HT1B, 5-HT1E, 5- HT1F and 5-HT7 receptors. It shows weak affinity (pKi<6.5) for the cloned human 5-HT1D and D3 receptors and moderate affinity (pKi=6.7) for the cloned human D2 receptor.

SB 243213 (0.1-10 mg/kg, p.o. 1 h pre-test) dose-dependently and significantly increases the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box. SB 243213 (0.3 mg/kg; p.o.; 1 h pre-test) significantly increases time spent in social interaction. Animal Model:Male Sprague-Dawley experimentally naive rats (220-300 g) Dosage:0.1, 0.3, 1, 3, 10 mg/kg Administration:PO; 1 hour pre-test Result:Dose-dependently and significantly increased the amount of time rats spent in social interaction over 15 min under brightly lit conditions and in an unfamiliar test box.

——

GPCR/G Protein

5-HT Receptor

5-HT Receptor

——

——

200940-22-3

428.41

C22H19F3N4O2

>98% (HPLC)

In Vitro:?DMSO 中的溶解度 : 125 mg/mL (291.78 mM; 超声助溶 )

Cc1cc2CCN(C(=O)Nc3ccc(Oc4cccnc4C)nc3)c2cc1C(F)(F)F

——

(-20℃)

With Ice Pack

≥ 2 years