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• 产品描述： Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is an antagonist of both dopamine D2 and 5-HT7 with IC50s of 1.68 and 0.495 nM, respectively. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75 nM.

• 靶点： 5-HT7 Receptor：0.495 nM (IC50)；5-HT1A Receptor：6.75 nM (IC50)；D2 Receptor：1.68 nM (IC50);DopamineReceptor;5-HTReceptor;Norepinephrine

• 体内研究：
  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)) (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 (Hydrochloride) (SM-13496 (Hydrochloride)) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in rats, and the ED50 values are 6.3 mg/kg. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) dose-dependently inhibits TRY-induced forepaw clonic seizure and p-CAMP-induced hyperthermia with ED50 values 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)

• 参考文献：
  1. Ishibashi T, et al. 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. Sakine Atila Karaca, et al. Development of a validated high-performance liquid chromatographic method for the determination of Lurasidone in pharmaceuticals. Marmara Pharm J. 2017;21 (4): 931-937.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： RT

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	1.89 ml	9.449 ml	18.899 ml
  5 mM	0.378 ml	1.89 ml	3.78 ml
  10 mM	0.189 ml	0.945 ml	1.89 ml
  50 mM	0.038 ml	0.189 ml	0.378 ml

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *