| 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 |
|
| 注意: |
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