标签归档：tetrahydroisoquinoline

7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物，专注于信号通路和疾病研究领域。
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 

7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (compound 11)，四氢异喹啉 (THIQ) 衍生物，是一种选择性的苯乙醇胺 N-甲基转移酶 (PNMT) 抑制剂，其 Ki 值为 0.3 μM。7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 可用于阿尔茨海默病和帕金森病等相关精神疾病的研究。

7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline

7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline Chemical Structure

CAS No. : 61563-24-4

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生物活性

7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (compound 11), a tetrahydroisoquinoline (THIQ) derivative, is a selective phenylethanolamine N-methyltransferase (PNMT) inhibitor with a Ki value of 0.3 μM. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline can be used in research on psychiatric disorders related to Alzheimer’s disease and Parkinson’s disease[1].

体内研究
(In Vivo)

7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (SKF-64139) (i.p., 40 mg/kg, once daily, 3 days) has an important role in the regulation of blood pressure and changes in adrenal catecholamine levels in rats[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male spontaneously hypertensive (SHR) and their age-paired normotensive Wistar-Kyoto (WKY) rats[2]
Dosage: 40 mg/kg
Administration: i.p.; once daily; 3 days
Result: Caused a decrease in blood pressure in SHR rats but no effect on blood pressure in WKY rats.
Caused a decrease in hypothalamic epinephrine (Epi) levels, norepinephrine (NE) levels and raised dopamine (DA) levels in both SHR and WKY rats.

分子量

202.08

Formula

C9H9Cl2N
CAS 号

61563-24-4
结构分类
  • Alkaloids
  • Isoquinoline Alkaloids
初始来源
  • 内源性代谢物
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (532 KB) 产品使用指南 (1538 KB)

参考文献

  • [1]. Pramod C Nair, et al. Using Theory to Reconcile Experiment: The Structural and Thermodynamic Basis of Ligand Recognition by Phenylethanolamine N-Methyltransferase (PNMT). J Chem Theory Comput. 2011 May 10;7(5):1458-68.  [Content Brief]

    [2]. N Y Liang, et al. Inhibitors of phenylethanolamine-N-methyltransferase. 2. Comparison of nonaromatic analogs of phenylethanolamines, 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline (SKF-64139) and 2,3-dichloro-alpha-methylbenzylamine: effects on rat brain and adrenal catecholamine content and blood pressure. J Pharmacol Exp Ther. 1982 Nov;223(2):382-7.  [Content Brief]

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