Isoquinoline, 7,9-dichloro-1,2,3,4-tetrahydro-

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].

Research Areas >> Neurological Disease

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]. 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.

[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.

[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.