rdf:type |
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lifeskim:mentions |
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pubmed:issue |
3
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pubmed:dateCreated |
1995-1-30
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pubmed:abstractText |
The binding selectivity of the muscarinic antagonist tripitramine has been tested on the five cloned human muscarinic receptor subtypes (Hm1 to Hm5) expressed in chinese hamster ovary (CHO-K1) cells. The results indicate that tripitramine binds to the muscarinic Hm2 receptor with a Ki value of 0.27 +/- 0.02 nM. Tripitramine distinguishes Hm2 vs. Hm4 by a factor of 24 and vs. Hm3 and Hm5 by a factor of 142 and 125, respectively. A lower affinity ratio, about 6-fold, was found between muscarinic Hm2 and Hm1 receptors. A comparative study with the well-known selective muscarinic M2 receptor antagonist methoctramine indicates that tripitramine has gained both potency and selectivity for the muscarinic Hm2 receptor subtype.
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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 |
http://linkedlifedata.com/resource/pubmed/chemical/Benzodiazepines,
http://linkedlifedata.com/resource/pubmed/chemical/DNA, Complementary,
http://linkedlifedata.com/resource/pubmed/chemical/Diamines,
http://linkedlifedata.com/resource/pubmed/chemical/Ligands,
http://linkedlifedata.com/resource/pubmed/chemical/Muscarinic Antagonists,
http://linkedlifedata.com/resource/pubmed/chemical/N-Methylscopolamine,
http://linkedlifedata.com/resource/pubmed/chemical/Parasympatholytics,
http://linkedlifedata.com/resource/pubmed/chemical/Receptors, Muscarinic,
http://linkedlifedata.com/resource/pubmed/chemical/Scopolamine Derivatives,
http://linkedlifedata.com/resource/pubmed/chemical/methoctramine,
http://linkedlifedata.com/resource/pubmed/chemical/tripitramine
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pubmed:status |
MEDLINE
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pubmed:month |
Aug
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pubmed:issn |
0014-2999
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pubmed:author |
|
pubmed:issnType |
Print
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pubmed:day |
16
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pubmed:volume |
268
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
459-62
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pubmed:dateRevised |
2008-11-21
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pubmed:meshHeading |
pubmed-meshheading:7805774-Animals,
pubmed-meshheading:7805774-Benzodiazepines,
pubmed-meshheading:7805774-CHO Cells,
pubmed-meshheading:7805774-Cricetinae,
pubmed-meshheading:7805774-DNA, Complementary,
pubmed-meshheading:7805774-Diamines,
pubmed-meshheading:7805774-Humans,
pubmed-meshheading:7805774-Ligands,
pubmed-meshheading:7805774-Muscarinic Antagonists,
pubmed-meshheading:7805774-N-Methylscopolamine,
pubmed-meshheading:7805774-Parasympatholytics,
pubmed-meshheading:7805774-Receptors, Muscarinic,
pubmed-meshheading:7805774-Scopolamine Derivatives,
pubmed-meshheading:7805774-Thermodynamics
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pubmed:year |
1994
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pubmed:articleTitle |
Binding profile of the selective muscarinic receptor antagonist tripitramine.
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pubmed:affiliation |
Institute of Pharmacology School of Medicine, University of Pisa, Italy.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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