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CAS No. : 367514-88-3
MCE 国际站:Lurasidone Hydrochloride
产品活性:Lurasidone (Hydrochloride) (SM-13496 (Hydrochloride)) 是 dopamine D2 和 5-HT7 的拮抗剂,IC50 值分别为 1.68 和 0.495 nM。 Lurasidone 也是 5-HT1A 受体的部分激动剂,IC50 值为 6.75 nM。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:5-HT Receptor | Dopamine Receptor
In Vitro: Lurasidone (SM-13496) Hydrochloride is an antagonist of dopamine D2 and 5-HT7 with IC50s of 1.68±0.09 and 0.495±0.090 nM, respectively. Lurasidone (SM-13496) Hydrochloride is also a partial agonist of 5-HT1A receptor with an IC50 of 6.75±0.97 nM. In vitro receptor binding experiments reveal that Lurasidone (SM-13496) Hydrochloride demonstrates affinity for dopamine D2 and 5-HT2A receptors higher than other tested antipsychotics. Lurasidone does not increase [35S]GTPγS binding to the membrane preparations for dopamine D2 receptors by itself, but it antagonizes dopamine-stimulated [35S]GTPγS binding in a concentration-dependent manner with a KB value of 2.8±1.1 nM.
In Vivo: Lurasidone (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 (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 (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 (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 (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).
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