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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
3
|
pubmed:dateCreated |
1995-11-6
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pubmed:abstractText |
2-Methyl-4-phenyl-1,2,3,4-tetrahydroisoquinoline-4-ol(PI-OH) (2a) and its derivatives form a new class of compounds possessing norepinephrine (NE) potentiating activity. As a new series of compounds, the isomeric 4-(4-hydroxyphenyl)- and 4-(3-hydroxyphenyl)-2-methyl-1,2,3,4- tetrahydroisoquinolin-4-ols (3a and 3b), and 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinolin-4-ol (3c) were prepared and their NE potentiating activities were evaluated. The 4-(4-hydroxyphenyl) analogue (3a) had only moderate activity and the 4-(3-hydroxyphenyl) analogue (3b) possessed a slightly higher activity than PI-OH. The 4-(3,4-dihydroxyphenyl) analogue (3c) was the most active compound and the pD2 value was 7.71 +/- 0.06 (activity ratio; 26.9 fold) at a concentration of 3 x 10(-6) M. These results indicate the importance of dihydroxyphenylethanolamine moiety of 3c for the inhibition of NE uptake.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:month |
Apr
|
pubmed:issn |
1055-9612
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pubmed:author | |
pubmed:issnType |
Print
|
pubmed:volume |
11
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
175-83
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pubmed:dateRevised |
2006-11-15
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pubmed:meshHeading |
pubmed-meshheading:7548633-Animals,
pubmed-meshheading:7548633-Dopamine,
pubmed-meshheading:7548633-Drug Synergism,
pubmed-meshheading:7548633-Isoquinolines,
pubmed-meshheading:7548633-Muscle, Skeletal,
pubmed-meshheading:7548633-Muscle Contraction,
pubmed-meshheading:7548633-Norepinephrine,
pubmed-meshheading:7548633-Rats,
pubmed-meshheading:7548633-Vasoconstrictor Agents
|
pubmed:year |
1994
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pubmed:articleTitle |
Synthesis and pharmacological evaluation of phenolic 2-methyl-4-phenyl-1,2,3,4-tetrahydroisoquinolin-4-ols as a new norepinephrine potentiator.
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pubmed:affiliation |
Faculty of Pharmaceutical Sciences, University of Tokushima, Japan.
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pubmed:publicationType |
Journal Article,
In Vitro
|