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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
1
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pubmed:dateCreated |
1987-2-24
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pubmed:abstractText |
The 5-fluoro and 8-fluoro analogues of trimetoquinol, TMQ, have been synthesized and evaluated for beta 2- and beta 1-adrenoceptor activity in guinea pig trachea and atria, respectively. The fluoro analogues of TMQ maintained potent beta 2-adrenoceptor agonist activity but had reduced beta 1-adrenoceptor agonist activity. The changes in beta 1-activity of these compounds were correlated to differences in phenolic pKa's. The beta 1- and beta 2-adrenoceptor actions of 2 and 3 were blocked in a competitive manner by propranolol. The enhanced beta 2/beta 1 selectivity for the analogues was found to be 8-fluoro analogue 3 greater than 5-fluoro analogue 2 greater than trimetoquinol (1).
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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 |
Jan
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pubmed:issn |
0022-2623
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:volume |
30
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
86-90
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pubmed:dateRevised |
2007-11-14
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pubmed:meshHeading |
pubmed-meshheading:2879920-Adrenergic beta-Agonists,
pubmed-meshheading:2879920-Animals,
pubmed-meshheading:2879920-Atrial Function,
pubmed-meshheading:2879920-Guinea Pigs,
pubmed-meshheading:2879920-Indicators and Reagents,
pubmed-meshheading:2879920-Isoquinolines,
pubmed-meshheading:2879920-Kinetics,
pubmed-meshheading:2879920-Magnetic Resonance Spectroscopy,
pubmed-meshheading:2879920-Male,
pubmed-meshheading:2879920-Muscle Contraction,
pubmed-meshheading:2879920-Myocardial Contraction,
pubmed-meshheading:2879920-Propranolol,
pubmed-meshheading:2879920-Receptors, Adrenergic, beta,
pubmed-meshheading:2879920-Spectrophotometry, Infrared,
pubmed-meshheading:2879920-Structure-Activity Relationship,
pubmed-meshheading:2879920-Trachea,
pubmed-meshheading:2879920-Tretoquinol
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pubmed:year |
1987
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pubmed:articleTitle |
5-fluoro- and 8-fluorotrimetoquinol: selective beta 2-adrenoceptor agonists.
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pubmed:publicationType |
Journal Article,
Comparative Study,
In Vitro,
Research Support, U.S. Gov't, P.H.S.,
Research Support, Non-U.S. Gov't
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