Dipraglurant,872363-17-2

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Dipraglurant

CAS No. : 872363-17-2

MCE 国际站：Dipraglurant

产品活性：Dipraglurant (ADX48621) 是一种有效的，选择性的，具有口服活性和可透过血脑屏障的 mGluR5 的负变构调节剂 (NAM)，IC₅₀ 值为 21 nM。Dipraglurant 可以减少左旋多巴诱发的运动障碍 (LID)。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：mGluR

In Vitro: Dipraglurant (1-10 μM; 15 min) counteracts the abnormal membrane responses and calcium rise induced either by the D2R agonist quinpirole or by caged dopamine (NPEC-Dopamine).

In Vivo: Dipraglurant (3-30 mg/kg; a single p.o.) reduces L-dopa-induced chorea and dystonia and does not interfere with the efficacy of L-dopa in treating parkinsonian disability macaque.
Dipraglurant exhibits C_max (1.040, 1.380, 5.310 ng/mL) T_max (1.0, 0.5, 1.0 h) and AUC_inf (2.230, 2.860, 15.700) following p.o. administration (3, 10, 30 mg/kg) in macaque.

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