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抑制剂描述:

产品名称:Pergolide mesylate

产品别名:见爱必信官网

英文别名:Pergolide mesylate

靶点:Dopamine Receptor

CAS:66104-23-2

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

Pergolide mesylate(商品名为Permax)是多巴胺受体激动剂,在一些国家用于治疗帕金森病。Pergolide mesylate 作为多巴胺D2,D1,和五羟色胺5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2B, 和5-HT_2C受体的激动剂。与Cabergoline类似,Pergolide mesylate在其他多巴胺受体亚型中可能也具有激动活性。

溶解性:DMSO :10 mg/mL

体外研究:

Pergolide mesylate (trade name Permax) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Pergolide mesylate functions as an agonist at the dopamine D2, D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline.

体内研究:Pergolide mesylate decreases plasma prolactin concentrations. The weak agonist activity of pergolide at D1 receptors somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease. The drug is in decreasing use, as it is reported to be associated with a form of heart disease called cardiac fibrosis. The use of pergolide or cabergoline is associated with a significantly increased risk of newly diagnosed cardiac-valve regurgitation.

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