Time-dependent inactivation of human phenylethanolamine N-methyltransferase by 7-isothiocyanatotetrahydroisoquinoline.

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Wu Q, Caine JM, Thomson SA, Slavica M, Grunewald GL, McLeish MJ

Time-dependent inactivation of human phenylethanolamine N-methyltransferase by 7-isothiocyanatotetrahydroisoquinoline.

Bioorg Med Chem Lett. 2009 Feb 15;19(4):1071-4. doi: 10.1016/j.bmcl.2009.01.014. Epub 2009 Jan 10.

PubMed ID

19171483 [ View in PubMed

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Abstract

Inhibitors of phenylethanolamine N-methyltransferase [PNMT, the enzyme that catalyzes the final step in the biosynthesis of epinephrine (Epi)] may be of use in determining the role of Epi in the central nervous system. Here we describe the synthesis and characterization of 7-SCN tetrahydroisoquinoline as an affinity label for human PNMT.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
1,2,3,4-Tetrahydro-Isoquinoline-7-Sulfonic Acid Amide	Phenylethanolamine N-methyltransferase	Ki (nM)	120	N/A	N/A	Details