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rdf:type |
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lifeskim:mentions |
umls-concept:C0002395,
umls-concept:C0003753,
umls-concept:C0026336,
umls-concept:C0026339,
umls-concept:C0034826,
umls-concept:C0038760,
umls-concept:C0205314,
umls-concept:C0243072,
umls-concept:C0243192,
umls-concept:C0679622,
umls-concept:C1280500
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pubmed:issue |
9
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pubmed:dateCreated |
2008-5-12
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pubmed:abstractText |
A series of novel, potent, and selective muscarinic receptor 1 agonists (M1 receptor agonists) that employ a key N-substituted morpholine Arecoline moiety has been synthesized as part of research effort for the therapy of Alzheimer's diseases. The ester group of arecoline (which is reported as muscarinic agonist) has been replaced by N-substituted morpholine ring. The structure-activity relationship reveals that the electron donating 4-substituted sulfonyl derivatives (9a, 9b, 9c, and 9e) on the nitrogen atom of the morpholine ring increases the affinity of M1 receptor binding 50- to 80-fold greater than the corresponding arecoline. Other derivatives also showed considerable M1 receptor binding affinity.
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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 |
May
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pubmed:issn |
1464-3391
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pubmed:author |
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pubmed:issnType |
Electronic
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pubmed:day |
1
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pubmed:volume |
16
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
5157-63
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pubmed:dateRevised |
2011-11-17
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pubmed:meshHeading |
pubmed-meshheading:18359231-Alzheimer Disease,
pubmed-meshheading:18359231-Animals,
pubmed-meshheading:18359231-Binding, Competitive,
pubmed-meshheading:18359231-Disease Models, Animal,
pubmed-meshheading:18359231-Dose-Response Relationship, Drug,
pubmed-meshheading:18359231-Drug Evaluation, Preclinical,
pubmed-meshheading:18359231-Male,
pubmed-meshheading:18359231-Maze Learning,
pubmed-meshheading:18359231-Memory,
pubmed-meshheading:18359231-Memory Disorders,
pubmed-meshheading:18359231-Molecular Structure,
pubmed-meshheading:18359231-Morpholines,
pubmed-meshheading:18359231-Rats,
pubmed-meshheading:18359231-Rats, Wistar,
pubmed-meshheading:18359231-Receptor, Muscarinic M1,
pubmed-meshheading:18359231-Scopolamine Hydrobromide,
pubmed-meshheading:18359231-Stereoisomerism,
pubmed-meshheading:18359231-Structure-Activity Relationship,
pubmed-meshheading:18359231-Sulfonamides
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pubmed:year |
2008
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pubmed:articleTitle |
Effect of novel N-aryl sulfonamide substituted 3-morpholino arecoline derivatives as muscarinic receptor 1 agonists in Alzheimer's dementia models.
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pubmed:affiliation |
Department of Studies in Chemistry, University of Mysore, Manasagangotri, Mysore 570006, India.
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pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
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