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Danegaptide

Danegaptide用途

Danegaptide (GAP-134) 是修饰的二肽,是第二代口服生物相容性的间隙连接调节剂。

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Danegaptide名称

[ CAS 号 ]:
943134-39-2

[ 中文名 ]:
Danegaptide

[ 英文名 ]:
GAP-134

[英文别名 ]:

zp1609
danegaptide
gap-134
unii-pa0y7735at

Danegaptide生物活性

[ 描述 ]:

Danegaptide (GAP-134) 是修饰的二肽,是第二代口服生物相容性的间隙连接调节剂。

[ 相关类别 ]:

信号通路 >> 细胞骨架 >> 间隙连接蛋白

研究领域 >> 心血管疾病

[ 靶点 ]

Gap junction.

[体外研究]

间隙连接解偶联可改变传导途径并促进心脏再入机制,其加强许多室上性心律失常,例如心房颤动(AF)和心房扑动(AFL)。间隙连接修饰物Danegaptide(GAP-134)在犬无菌性心包炎模型中对传导和AF/AFL诱导能力的测量显示出一致的功效。 Danegaptide(GAP-134)是一种药物制剂,具有良好的临床安全性和潜在的抗心律失常功效,已在I期临床试验中得到证实。

[参考文献]

[1]. De Vuyst E, Boengler K, Antoons G, et al. Pharmacological modulation of connexin-formed channels in cardiac pathophysiology. Br J Pharmacol. 2011 Jun;163(3):469-83.

[2]. Laurent G, Leong-Poi H, Mangat I, et al. Effects of chronic gap junction conduction-enhancing antiarrhythmic peptide GAP-134 administration on experimental atrial fibrillation in dogs. Circ Arrhythm Electrophysiol. 2009 Apr;2(2):171-8.

[3]. Hennan JK, Swillo RE, Morgan GA, et al. GAP-134 ([2S,4R]-1-[2-aminoacetyl]4-benzamidopyrrolidine-2-carboxylic acid) prevents spontaneous ventricular arrhythmias and reduces infarct size during myocardial ischemia/reperfusion injury in open-chest dogs. J Cardiovasc Pharmacol Ther. 2009 Sep;14(3):207-14.

[4]. Rossman EI, Liu K, Morgan GA, et al. The gap junction modifier, GAP-134 [(2S,4R)-1-(2-aminoacetyl)-4-benzamido-pyrrolidine-2-carboxylic acid], improves conduction and reduces atrial fibrillation/flutter in the canine sterile pericarditis model. J Pharmacol Exp Ther. 2009 Jun;329(3):1127-33.

[5]. Eugene L. Piatnitski Cheklera, John A. Buterab, Li Dib, Discovery of a class of potent gap-junction modifiers as novel antiarrhythmic agents. Bioorganic & Medicinal Chemistry Letters. 2009,19(16): 4551-4554

[相关活性小分子]

托那博沙 | GAP-134 Hydrochloride | Gap 27 | GAP26