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AMG 579
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
AMG 579图片

AMG579是有效,选择性的磷酸二酯酶10A(PDE10A)抑制剂,IC50值为0.1nM。

Animal experiment:

Rats[1]Adult male Sprague–Dawley rats (250–280 g) are dosed at 0.1, 0.3, 1, and 3 mg/kg PO 1 h prior to administration of PCP. The magnitude of rat locomotor activity is quantified as number of beam breaks over a 2 h period[1].

产品描述

AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM.

AMG 579 shows statistically significant reduction of PCP induced behavior in rats over the 2 h period. Minimum effective doses for efficacy in PCP-LMA model is determined to be 0.3 mg/kg for AMG 579. In dog, 5 exhibits superior oral bioavailability of 72%[1].

[1]. Hu E,et al. Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A). J Med Chem. 2014 Aug 14;57(15):6632-41.

 
 
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