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

Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of dopamine D₂and 5-HT₇with IC₅₀s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT_1Areceptor with an IC₅₀of 6.75±0.97 nM.In vitroreceptor binding experiments reveal that Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) demonstrates affinity for dopamine D₂and 5-HT_2Areceptors higher than other tested antipsychotics. Lurasidone 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 (Hydrochloride) (SM-13496 (Hydrochloride)) dose-dependently increases the ratio of DOPAC/dopamine in both regions, but it shows a preferential effect on the frontal cortex compare with the striatum, especially at higher doses. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) (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 (Hydrochloride) (SM-13496 (Hydrochloride)) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED₅₀values are 6.3 mg/kg. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) dose-dependently inhibits TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia with ED₅₀values of 5.6 and 3.0 mg/kg, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) (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].

529.14

Solid

C₂₈H₃₇ClN₄O₂S

367514-88-3

盐酸鲁拉西酮

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

DMSO : 6.67 mg/mL(12.61 mM;ultrasonic and warming and adjust pH to 3 with HCl and heat to)

Ethanol : 2 mg/mL(3.78 mM;Need ultrasonic)

H₂O :< 0.1 mg/mL(insoluble)

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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

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    40%PEG300   5%Tween-80   45% saline

  Solubility: ≥ 0.67 mg/mL (1.27 mM); Clear solution

  此方案可获得 ≥ 0.67 mg/mL (1.27 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

  将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液
• 2.

  请依序添加每种溶剂： 10% DMSO    90% (20%SBE-β-CDin saline)

  Solubility: ≥ 0.67 mg/mL (1.27 mM); Clear solution

  此方案可获得 ≥ 0.67 mg/mL (1.27 mM，饱和度未知) 的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

  将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明