Source:http://linkedlifedata.com/resource/pubmed/id/19726200
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
19
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pubmed:dateCreated |
2009-9-16
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pubmed:abstractText |
Heteroaromatic carboxylic esters of (nor)tropine were synthesized. Tropine esters displaced [(3)H]strychnine binding to glycine receptors of rat spinal cord with low Hill slopes. Two-site displacement resulted in nanomolar IC(50,1) and micromolar IC(50,2) values, and IC(50,2)/IC(50,1) ratios up to 615 depending on the heteroaromatic rings and N-methyl substitution. Nortropeines displayed high affinity and low heterogeneity. IC(50,1) and IC(50,2) values of tropeines did not correlate suggesting different binding modes/sites. Glycine potentiated only the nanomolar displacement reflecting positive allosteric interactions and potentiation of ionophore function. Affinities of three (nor)tropeines were different for glycine receptors but identical for 5-HT(3) receptors.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical |
http://linkedlifedata.com/resource/pubmed/chemical/Esters,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Glycine,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Serotonin, 5-HT3,
http://linkedlifedata.com/resource/pubmed/chemical/Strychnine,
http://linkedlifedata.com/resource/pubmed/chemical/Tropanes,
http://linkedlifedata.com/resource/pubmed/chemical/tropine
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pubmed:status |
MEDLINE
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pubmed:month |
Oct
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pubmed:issn |
1464-3391
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pubmed:author | |
pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
17
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
6872-8
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pubmed:meshHeading |
pubmed-meshheading:19726200-Animals,
pubmed-meshheading:19726200-Binding, Competitive,
pubmed-meshheading:19726200-Binding Sites,
pubmed-meshheading:19726200-Esters,
pubmed-meshheading:19726200-Inhibitory Concentration 50,
pubmed-meshheading:19726200-Protein Binding,
pubmed-meshheading:19726200-Rats,
pubmed-meshheading:19726200-Receptors, Glycine,
pubmed-meshheading:19726200-Receptors, Serotonin, 5-HT3,
pubmed-meshheading:19726200-Spinal Cord,
pubmed-meshheading:19726200-Strychnine,
pubmed-meshheading:19726200-Tropanes
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pubmed:year |
2009
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pubmed:articleTitle |
Synthesis of heteroaromatic tropeines and heterogeneous binding to glycine receptors.
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pubmed:affiliation |
Department of Molecular Pharmacology, Institute of Biomolecular Chemistry, Chemical Research Center, Hungarian Academy of Sciences, H-1525 Budapest, PO Box 17, Hungary. maksay@chemres.hu
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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