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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, U.S. Gov't, Non-P.H.S.
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Enzyme Inhibitors / chemical synthesis
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / pharmacology*
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Humans
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Molecular Structure
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Phenylethanolamine N-Methyltransferase / antagonists & inhibitors*
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Receptors, Adrenergic, alpha-2 / drug effects
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Tetrahydroisoquinolines / chemical synthesis
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Tetrahydroisoquinolines / chemistry*
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Tetrahydroisoquinolines / pharmacology*
Substances
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Enzyme Inhibitors
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Receptors, Adrenergic, alpha-2
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Tetrahydroisoquinolines
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Phenylethanolamine N-Methyltransferase