Abstract
3-Hydroxyethyl- and 3-hydroxypropyl-7-substituted-tetrahydroisoquinolines (9, 10, 16, and 17) were synthesized and evaluated for their phenylethanolamine N-methyltransferase (PNMT) inhibitory potency and affinity for the alpha(2)-adrenoceptor. Although alpha(2)-adrenoceptor affinity decreased for these compounds, selectivity was not gained over the parent 3-hydroxymethyl compounds (1, 2) due to a loss in PNMT inhibitory potency.
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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Animals
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Binding Sites
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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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Epinephrine / physiology
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Humans
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Isoquinolines / chemical synthesis*
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Isoquinolines / chemistry
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Isoquinolines / pharmacology
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Male
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Phenylethanolamine N-Methyltransferase / antagonists & inhibitors*
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Phenylethanolamine N-Methyltransferase / chemistry*
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Rats
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Rats, Sprague-Dawley
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Receptors, Adrenergic, alpha-2 / chemistry
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Structure-Activity Relationship
Substances
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Enzyme Inhibitors
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Isoquinolines
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Receptors, Adrenergic, alpha-2
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Phenylethanolamine N-Methyltransferase
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Epinephrine