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Lurasidone

CAS No. : 367514-87-2

MCE 站：Lurasidone

产品活性：Lurasidone (SM-13496) 是 dopamine D₂ 和 5-HT₇ 的拮抗剂，IC₅₀ 值分别为 1.68 和 0.495 nM。 Lurasidone (SM-13496) 也是 5-HT_1A 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) 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) is also a partial agonist of 5-HT_1A receptor with an IC₅₀ of 6.75±0.97 nM. In vitro receptor binding experiments reveal that Lurasidone (SM-13496) demonstrates affinity for dopamine D₂ and 5-HT_2A receptors higher than other tested antipsychotics. Lurasidone (SM-13496) 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 K_B value of 2.8±1.1 nM.

In Vivo: 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 (p<0.01).

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