1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELurasidone HydrochlorideCat. No.: HY-B0032CAS No.: 367514-88-3Synonyms: SM-13496 (Hydrochloride)分式: CHClNOS分量: 529.14作靶點: 5-HT Receptor; Dopamine Receptor作通路: GPCR/G Protein; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsI

2、n solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 1 mg/mL (1.89 mM; Need ultrasonic and warming)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.8899 mL 9.4493 mL 18.8986 mL5 mM - - -10 mM - - -請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 Stock solution of LUR at

3、 1 mg/mL is prepared in methanol using LUR hydrochloride. Stock solutions of LURtablets at 1 mg/mL are prepared in methanol2.BIOLOGICAL ACTIVITY物活性Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)是dopamine D2 和 5-HT7 的拮抗劑，IC50 值分別1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE為 1.68 和 0.495 nM。

4、 Lurasidone 也是5-HT1A 受體的部分激動劑，IC50 值為 6.75 nM。IC50 & Target IC50: 1.68 nM (dopamine D2), 0.495 nM (5-HT7), 6.75 nM (5-HT1A) 1體外研究 Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride) is an antagonist of dopamine D2 and 5-HT7 withIC50s of 1.680.09 and 0.4950.090 nM, respectively. Lurasidone (Hydrochl

5、oride) (SM-13496(Hydrochloride) is also a partial agonist of 5-HT1A receptor with an IC50 of 6.750.97 nM. In vitro receptorbinding experiments reveal that Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride) demonstratesaffinity for dopamine D2 and 5-HT2A receptors higher than other tested antipsych

6、otics. Lurasidone does notincrease 35SGTPS binding to the membrane preparations for dopamine D2 receptors by itself, but itantagonizes dopamine-stimulated 35SGTPS binding in a concentration-dependent manner with a KBvalue of 2.81.1 nM 1.體內(nèi)研究 Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride) dose-

7、dependently increases the ratio ofDOPAC/dopamine in both regions, but it shows a preferential effect on the frontal cortex compare with thestriatum, especially at higher doses. Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride) (ED50 values2.3 to 5.0 mg/kg) shows a comparable potency with olanzapi

8、ne (ED50 values 1.1 to 5.1 mg/kg), higherpotency than clozapine (ED50 9.5 to 290 mg/kg), and slightly lower potency than haloperidol (ED50 values0.44 to 1.7 mg/kg). Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride) (1 to 10 mg/kg) dose-dependently inhibits conditioned avoidance response (CAR) in

9、rats, and the ED50 values are 6.3 mg/kg.Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride) dose-dependently inhibits TRY-induced forepawclonic 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

10、 mg/kg) dose-dependently and significantlyincreases the number of shocks received by rats in the conflict test with MED of 10 mg/kg (p 1.PROTOCOLAnimal SD rats are individually isolated in clear plastic cages and injected with methamphetamine (MAP) (1 mg/kgAdministration 1 i.p.) 1 h after the admini

11、stration of drugs or vehicle. In the test of persistence of the effect, Lurasidone(Hydrochloride) (SM-13496 (Hydrochloride) is administered 1, 2, 4, and 8 h before the MAP injection.Locomotor activity is measured for 80 min from 10 min after MAP injection. Four or five groups of 6 to 13 ratsare used

12、 to calculate the ED50 value that inhibits MAP-induced hyperactivity by 50% of the animals tested1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Marmara Pharm J. 2017;21 (4): 931-937. Marmara Pharm J. 2017;21 (4): 931-937.See more customer

13、 validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. 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 ofLurasidone in pharmaceuticals. Marmara Pharm J. 2017;21 (4): 931-9