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MAO-B-IN-6

CAS No. : 2376198-66-0

MCE 站：MAO-B-IN-6

产品活性：MAO-B-IN-6 是一种有效的、选择性和具有口服活性的 MAO-B 抑制剂，IC₅₀ 值为 0.019 M。MAO-B-IN-6 在体外和体内均显示比 Safinamide 更有效。MAO-B-IN-6 具有研究帕金森病 (PD) 的潜力。

研究领域：Neuronal Signaling

作用靶点：Monoamine Oxidase

In Vitro: MAO-B-IN-6 (compound D5) (Sf9 cells) shows inhibitory activities towards monoamine oxidase (MAO) with the IC₅₀s of 46.365 M ａnd 0.019 M for MAO-A ａnd MAO-B, respectively.
MAO-B-IN-6 shows no inhibition potential towards cytochrome P450 (IC₅₀=>29 M for 1A2, 2B6, 2C8, 2C9, 2C19, 2D6 ａnd 3A4/5 enzymes).
MAO-B-IN-6 (10 M) shows high permeability through MDR1-MDCK II cell monolayers.

In Vivo: MAO-B-IN-6 (1 mg/kg, i.v.; 5 mg/kg, p.o.) shows oral bioavailability in rats (F=55.2%) ａnd monkeys (F=107.1%).
MAO-B-IN-6 (0.08, 0.4, 2 mg/kg; i.p.) diaplays stronger MAO-B inhibitory activity.
MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) increases the rearing activity in a dose-dependent manner.
MAO-B-IN-6 (0.625, 1.25, 2.5 mg/kg; i.p.) shows a potential efficacy for alleviating dopamine (DA) deficits in the MPTP-induced Parkinson＇s disease (PD) mouse model.
MAO-B-IN-6 (0.156, 0.312, 0.625, 1.25 mg/kg; i.p.) increases the effect of levodopa on dopamine concentration in the striatum.
MAO-B-IN-6 (0.156, 0.312, 0.625, 1.25 mg/kg; i.p.) shows a significant reduction in galantamine-induced tremulous jaw movements.
Pharmacokinetic Parameters of MAO-B-IN-6 in SD rats ａnd cynomolgus monkeys.

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