CAS NO: | 367514-88-3 |
包装 | 价格(元) |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
200mg | 电议 |
500mg | 电议 |
1 g | 电议 |
5 g | 电议 |
生物活性 | 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-HT1Areceptor with anIC50of 6.75 nM. | ||||||||||||||||
IC50& Target |
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体外研究 (In Vitro) | 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-HT1Areceptor 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-HT2Areceptors 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 KBvalue of 2.8±1.1 nM[1]. | ||||||||||||||||
体内研究 (In Vivo) | 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]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 529.14 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C28H37ClN4O2S | ||||||||||||||||
CAS 号 | 367514-88-3 | ||||||||||||||||
中文名称 | 盐酸鲁拉西酮 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 | 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) | ||||||||||||||||
溶解性数据 | In Vitro: 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) 配制储备液
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