Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.

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Grunewald GL, Lu J, Criscione KR, Okoro CO

Inhibitors of phenylethanolamine N-methyltransferase devoid of alpha2-adrenoceptor affinity.

Bioorg Med Chem Lett. 2005 Dec 1;15(23):5319-23. Epub 2005 Sep 19.

PubMed ID

16169723 [ View in PubMed

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Abstract

A series of 3-trifluoromethyl-1,2,3,4-tetrahydroisoquinolines was synthesized and evaluated for their phenylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the alpha(2)-adrenoceptor. Although their PNMT inhibitory potency decreased compared with corresponding 3-methyl-, 3-hydroxymethyl- or 3-unsubstituted-THIQs, some of them showed good selectivity due to their extremely low alpha(2)-adrenoceptor affinity.

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)	280	N/A	N/A	Details
7-Iodo-1,2,3,4-Tetrahydro-Isoquinoline	Phenylethanolamine N-methyltransferase	Ki (nM)	93	N/A	N/A	Details
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline	Phenylethanolamine N-methyltransferase	Ki (nM)	3.1	N/A	N/A	Details