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rdf:type |
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lifeskim:mentions |
umls-concept:C0006675,
umls-concept:C0014653,
umls-concept:C0026377,
umls-concept:C0205177,
umls-concept:C0220821,
umls-concept:C0456389,
umls-concept:C0597358,
umls-concept:C1280500,
umls-concept:C1550548,
umls-concept:C1555714,
umls-concept:C1705654
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pubmed:issue |
8
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pubmed:dateCreated |
1991-9-25
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pubmed:abstractText |
The conformational requisites at the receptor for unsymmetrically substituted phenyl-1,4-dihydropyridine calcium entry blockers are examined by screening a series of (2'-halophenyl)-1,4-dihydropyridines 1-4, with increasing bulk at the 2'-position of the phenyl ring, for their ability to relax potassium-contracted rabbit aortic smooth muscle and to competitively displace [3H]nitrendipine from its specific binding sites on guinea pig skeletal muscle. The fraction of synperiplanar rotamer in solution for these compounds, as determined by the nuclear Overhauser enhancement method, shows a positive correlation with vasorelaxant activity and receptor binding affinity. These findings are consistent with the synperiplanar rotamer of nonrigid unsymmetrically substituted phenyl 1,4-dihydropyridine calcium channel blockers being the receptor-bound conformation.
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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 |
Aug
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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 |
34
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
2521-4
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:1652021-Animals,
pubmed-meshheading:1652021-Aorta,
pubmed-meshheading:1652021-Binding, Competitive,
pubmed-meshheading:1652021-Calcium Channel Blockers,
pubmed-meshheading:1652021-Calcium Channels,
pubmed-meshheading:1652021-Chemical Phenomena,
pubmed-meshheading:1652021-Chemistry,
pubmed-meshheading:1652021-Dihydropyridines,
pubmed-meshheading:1652021-Guinea Pigs,
pubmed-meshheading:1652021-Halogens,
pubmed-meshheading:1652021-Male,
pubmed-meshheading:1652021-Molecular Conformation,
pubmed-meshheading:1652021-Molecular Structure,
pubmed-meshheading:1652021-Muscle, Smooth, Vascular,
pubmed-meshheading:1652021-Muscle Relaxation,
pubmed-meshheading:1652021-Muscles,
pubmed-meshheading:1652021-Nitrendipine,
pubmed-meshheading:1652021-Receptors, Nicotinic,
pubmed-meshheading:1652021-Structure-Activity Relationship
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pubmed:year |
1991
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pubmed:articleTitle |
Active conformation of 1,4-dihydropyridine calcium entry blockers. Effect of size of 2-aryl substituent on rotameric equilibria and receptor binding.
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pubmed:affiliation |
Department of Chemistry/Cardiopulmonary, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543-4000.
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pubmed:publicationType |
Journal Article
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