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Lurasidone

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	同义名 :	SM-13496
	CAS号 :	367514-87-2
	货号 :	A418721
	分子式 :	C₂₈H₃₆N₄O₂S
	纯度 :	98%
	分子量 :	492.676
	MDL号 :	MFCD14635357
	存储条件：	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6个月-80°C:12个月
	溶解度 :	DMSO: 20 mg/mL(40.59 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO 无水乙醇: 3 mg/mL(6.09 mM)，配合低频超声，并水浴加热至45℃助溶，注意：无水乙醇开封后，易挥发，也会吸收空气中的水分，导致溶解能力下降，请避免使用开封较久的乙醇
	动物实验配方：

生物活性
靶点	D2 receptor D2 receptor, IC50:1.68 nM D2 receptor D2 receptor, Ki:1 nM
描述	Lurasidone (SM-13496) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (SM-13496) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM. In vitro receptor binding experiments reveal that Lurasidone (SM-13496) demonstrates affinity for dopamine D2 and 5-HT2A receptors higher than other tested antipsychotics. 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) (ED50 values 2.3 to 5.0 mg/kg) shows a comparable potency with olanzapine (ED50 values 1.1 to 5.1 mg/kg), higher potency than clozapine (ED50 9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED50 values 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 ED50 values 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 ED50 values 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^[1]. 80 mg/d lurasidone, an effective and tolerable dose for non-TRS (treatment-resistant schizophrenia) patients, was also effective in TRS patients but required longer duration of treatment^[2]. In the ITT (intention-to-treat) (but not the mITT) population, treatment with lurasidone was associated with significant improvement in the PANSS (Positive and Negative Syndrome Scale) total score in patients with schizophrenia. Lurasidone was generally well tolerated with minimal impact on weight and metabolic parameters^[3].

临床研究
NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02181803	Schizophrenia	Phase 1	Completed	-	-
NCT01431326	-		Recruiting	February 2020	-
NCT01364818	-		Completed	-	United States, North Carolina ... 展开 >> University of North Carolina Chapel Hill Chapel Hill, North Carolina, United States, 27599 收起 <<

实验方案

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.03mL

0.41mL

0.20mL

10.15mL

2.03mL

1.01mL

20.30mL

4.06mL

2.03mL

参考文献

[1]Ishibashi T, Horisawa T, Tokuda K, Ishiyama T, Ogasa M, Tagashira R, Matsumoto K, Nishikawa H, Ueda Y, Toma S, Oki H, Tanno N, Saji I, Ito A, Ohno Y, Nakamura M. Pharmacological profile of lurasidone, a novel antipsychotic agent with potent 5-hydroxytryptamine 7 (5-HT7) and 5-HT1A receptor activity. J Pharmacol Exp Ther. 2010 Jul;334(1):171-81

[2]Meltzer HY, Share DB, Jayathilake K, Salomon RM, Lee MA. Lurasidone Improves Psychopathology and Cognition in Treatment-Resistant Schizophrenia. J Clin Psychopharmacol. 2020 May/Jun;40(3):240-249

[3]Higuchi T, Ishigooka J, Iyo M, Yeh CB, Ebenezer EG, Liang KY, Lee JS, Lee SY, Lin SK, Yoon BH, Nakamura M, Hagi K, Sato T. Lurasidone in the treatment of schizophrenia: Results of a double-blind, placebo-controlled trial in Asian patients. Asia Pac Psychiatry. 2019 Jun;11(2):e12352

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靶点

靶点	数值

D2 receptor	D2 receptor, IC50:1.68 nM
D2 receptor	D2 receptor, Ki:1 nM