Lurasidone (SM-13496) is an antagonist of bothdopamine D₂and5-HT₇withIC₅₀s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of5-HT_1Areceptor with anIC₅₀of 6.75 nM.

Lurasidone (SM-13496) is an antagonist of dopamine D₂and 5-HT₇with IC₅₀s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT_1Areceptor with an IC₅₀of 6.75±0.97 nM.In vitroreceptor binding experiments reveal that Lurasidone (SM-13496) demonstrates affinity for dopamine D₂and 5-HT_2Areceptors higher than other tested antipsychotics. Lurasidone (SM-13496) does not increase [³⁵S]GTPγS binding to the membrane preparations for dopamine D₂receptors by itself, but it antagonizes dopamine-stimulated [³⁵S]GTPγS binding in a concentration-dependent manner with a K_Bvalue of 2.8±1.1 nM^[1].

Lurasidone (SM-13496) dose-dependently increases the ratio of DOPAC/dopamine in frontal cortex and striatum, but it shows a preferential effect on the frontal cortex compare with the striatum, especially at higher doses. Lurasidone (SM-13496) (ED₅₀values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED₅₀values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED₅₀9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED₅₀values 0.44 to 1.7 mg/kg). Lurasidone (SM-13496) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED₅₀values are 6.3 mg/kg. Lurasidone (SM-13496) dose-dependently inhibits tryptamine (TRY)-induced forepaw clonic seizure and p-chloroamphetamine (p-CAMP)-induced hyperthermia with ED₅₀values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (SM-13496) (0.3 to 30 mg/kg) dose-dependently and significantly increases the number of shocks received by rats in the conflict test with MED of 10 mg/kg (p<0.01)^[1].

492.68

Solid

C₂₈H₃₆N₄O₂S

367514-87-2

鲁拉西酮；卢拉西酮

Room temperature in continental US; may vary elsewhere.

4°C, protect from light

*该产品在溶液状态不稳定，建议您现用现配，即刻使用。

DMSO : 20.83 mg/mL(42.28 mM;Need ultrasonic)

Ethanol : 3.33 mg/mL(6.76 mM;ultrasonic and warming and heat to 60℃)

请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液；该产品在溶液状态不稳定，建议您现用现配，即刻使用。

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

• 1.

  请依序添加每种溶剂： 10% DMSO    90%corn oil

  Solubility: ≥ 2.08 mg/mL (4.22 mM); Clear solution

  此方案可获得 ≥ 2.08 mg/mL (4.22 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

  以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。