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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4
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pubmed:dateCreated |
2005-2-2
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pubmed:abstractText |
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.
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pubmed:grant |
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Feb
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pubmed:issn |
0960-894X
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
15
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pubmed:volume |
15
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
1143-7
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:15686930-Animals,
pubmed-meshheading:15686930-Binding Sites,
pubmed-meshheading:15686930-Enzyme Inhibitors,
pubmed-meshheading:15686930-Epinephrine,
pubmed-meshheading:15686930-Humans,
pubmed-meshheading:15686930-Isoquinolines,
pubmed-meshheading:15686930-Male,
pubmed-meshheading:15686930-Phenylethanolamine N-Methyltransferase,
pubmed-meshheading:15686930-Rats,
pubmed-meshheading:15686930-Rats, Sprague-Dawley,
pubmed-meshheading:15686930-Receptors, Adrenergic, alpha-2,
pubmed-meshheading:15686930-Structure-Activity Relationship
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pubmed:year |
2005
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pubmed:articleTitle |
Exploring the active site of phenylethanolamine N-methyltransferase with 3-hydroxyethyl- and 3-hydroxypropyl-7-substituted-1,2,3,4-tetrahydroisoquinolines.
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pubmed:affiliation |
Department of Medicinal Chemistry, University of Kansas, 1251 Wescoe Hall Drive, Lawrence, KS 66045, USA. ggrunewald@ku.edu
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pubmed:publicationType |
Journal Article,
Research Support, U.S. Gov't, P.H.S.,
Research Support, U.S. Gov't, Non-P.H.S.,
Research Support, N.I.H., Extramural
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