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Predicate | Object |
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rdf:type | |
lifeskim:mentions | |
pubmed:issue |
1
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pubmed:dateCreated |
1982-7-19
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pubmed:abstractText |
Imipramine and some of its analogs (trimipramine, 3-chlorimipramine, desipramine, 3-chloro-2-hydroxyimipramine, 2-hydroxyimipramine, and didesmethylimipramine), were assayed for their potencies as antimuscarinic agents by their abilities to antagonize muscarinic receptor-mediated cyclic guanosine monophosphate (GMP) formation by cultured mouse neuroblastoma cells. Equilibrium dissociation constants for these compounds yielded the following rank order of potency at the muscarinic receptor: imipramine greater than trimipramine greater than 3-chlorimipramine greater than desipramine greater than 3-chloro-2-hydroxyimipramine greater than 2-hydroxyimipramine greater than didesmethylimipramine. These results indicate that didesmethylation of the side chain nitrogen or hydroxylation of the ring at the 2-position lead to marked reductions (30-fold and 12-fold, respectively) in antimuscarinic activity of imipramine.
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pubmed:language |
eng
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pubmed:journal | |
pubmed:citationSubset |
IM
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pubmed:chemical | |
pubmed:status |
MEDLINE
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pubmed:issn |
0033-3158
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pubmed:author | |
pubmed:issnType |
Print
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pubmed:volume |
76
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
26-8
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pubmed:dateRevised |
2003-11-14
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pubmed:meshHeading |
pubmed-meshheading:6281837-Animals,
pubmed-meshheading:6281837-Clone Cells,
pubmed-meshheading:6281837-Cyclic GMP,
pubmed-meshheading:6281837-Imipramine,
pubmed-meshheading:6281837-Mice,
pubmed-meshheading:6281837-Neuroblastoma,
pubmed-meshheading:6281837-Receptors, Cholinergic,
pubmed-meshheading:6281837-Receptors, Muscarinic,
pubmed-meshheading:6281837-Structure-Activity Relationship
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pubmed:year |
1982
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pubmed:articleTitle |
Anticholinergic activity of imipramine and some analogs at muscarinic receptors of cultured mouse neuroblastoma cells.
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pubmed:publicationType |
Journal Article
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