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排名前五的药物类型	数量

小分子化药	1

排名前五的靶点	数量

P2Y6 receptor(嘌呤受体P2Y6)	1

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1

项与 Glaucopharm Ltd. 相关的药物

TG-46

靶点

P2Y6 receptor

作用机制

P2Y6 receptor激动剂

在研机构

Glaucopharm Ltd.

原研机构

Glaucopharm Ltd.

在研适应症

青光眼

非在研适应症-

最高研发阶段临床前

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首次获批日期-

100 项与 Glaucopharm Ltd. 相关的临床结果

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0 项与 Glaucopharm Ltd. 相关的专利（医药）

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1

项与 Glaucopharm Ltd. 相关的文献（医药）

2018-09-01·Purinergic Signalling3区 · 医学

A promising drug candidate for the treatment of glaucoma based on a P2Y6-receptor agonist

3区 · 医学

Article

作者: Dixit, Mudit ; Ginsburg-Shmuel, Tamar ; Singh, Vijay ; Youdim, Moussa B H ; Pintor, Jesus ; Major, Dan T ; Fonseca, Begoña ; Weinreb, Orly ; Jacob, Tali Fishman ; Fischer, Bilha

Extracellular nucleotides can regulate the production/drainage of the aqueous humor via activation of P2 receptors, thus affecting the intraocular pressure (IOP). We evaluated 5-OMe-UDP(α-B), 1A, a potent P2Y6-receptor agonist, for reducing IOP and treating glaucoma. Cell viability in the presence of 1A was measured using [3-(4, 5-dimethyl-thiazol-2-yl) 2, 5-diphenyl-tetrazolium bromide] (MTT) assay in rabbit NPE ciliary non-pigmented and corneal epithelial cells, human retinoblastoma, and liver Huh7 cells. The effect of 1A on IOP was determined in acute glaucomatous rabbit hyaluronate model and phenol-induced chronic glaucomatous rabbit model. The origin of activity of 1A was investigated by generation of a homology model of hP2Y6-R and docking studies. 1A did not exert cytotoxic effects up to 100 mM vs. trusopt and timolol in MTT assay in ocular and liver cells. In normotensive rabbits, 100 μM 1A vs. xalatan, trusopt, and pilocarpine reduced IOP by 45 vs. 20-30%, respectively. In the phenol animal model, 1A (100 μM) showed reduction of IOP by 40 and 20%, following early and late administration, respectively. Docking results suggest that the high activity and selectivity of 1A is due to intramolecular interaction between Pα-BH³ and C5-OMe which positions 1A in a most favorable site inside the receptor. P2Y6-receptor agonist 1A effectively and safely reduces IOP in normotense, acute, and chronic glaucomatous rabbits, and hence may be suggested as a novel approach for the treatment of glaucoma.

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100 项与 Glaucopharm Ltd. 相关的转化医学

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