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rdf:type |
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lifeskim:mentions |
umls-concept:C0034826,
umls-concept:C0053139,
umls-concept:C0201734,
umls-concept:C0243076,
umls-concept:C0392747,
umls-concept:C0596810,
umls-concept:C0871161,
umls-concept:C1515655,
umls-concept:C1554963,
umls-concept:C1627358,
umls-concept:C2349975
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pubmed:issue |
23
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pubmed:dateCreated |
2002-11-6
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pubmed:abstractText |
We previously reported the initial discovery of a novel class of stabilized benzylidene ketal M(2) receptor antagonists. This paper discusses new analogues consisting of benzamide modifications which not only improved M(2) receptor affinity and selectivity, but also enhanced the pharmacokinetic properties of the series. These changes led to the discovery of a highly potent and selective M(2) antagonist, which demonstrated in vivo efficacy and had good bioavailability in multiple species.
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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 |
Dec
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pubmed:issn |
0960-894X
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pubmed:author |
pubmed-author:BillardWilliamW,
pubmed-author:BinchHerbertH3rd,
pubmed-author:BoyleCraig DCD,
pubmed-author:CampionJenniferJ,
pubmed-author:ChackalamannilSamuelS,
pubmed-author:CoffinVicki LVL,
pubmed-author:CoxKathleen AKA,
pubmed-author:CrosbyGordonG,
pubmed-author:DuffyRuth ARA,
pubmed-author:GrotzDiane EDE,
pubmed-author:LachowiczJean EJE,
pubmed-author:LankinClaire MCM,
pubmed-author:McCombieStuart WSW,
pubmed-author:RupertoVilmaV,
pubmed-author:ViceSusan FSF,
pubmed-author:WilliamsMary-CohenMC
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pubmed:issnType |
Print
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pubmed:day |
2
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pubmed:volume |
12
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3479-82
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pubmed:dateRevised |
2004-11-17
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pubmed:meshHeading |
pubmed-meshheading:12419388-Acetylcholine,
pubmed-meshheading:12419388-Animals,
pubmed-meshheading:12419388-Area Under Curve,
pubmed-meshheading:12419388-Benzamides,
pubmed-meshheading:12419388-Benzylidene Compounds,
pubmed-meshheading:12419388-Drug Design,
pubmed-meshheading:12419388-Drug Evaluation, Preclinical,
pubmed-meshheading:12419388-Humans,
pubmed-meshheading:12419388-Microdialysis,
pubmed-meshheading:12419388-Microsomes, Liver,
pubmed-meshheading:12419388-Muscarinic Antagonists,
pubmed-meshheading:12419388-Rats,
pubmed-meshheading:12419388-Receptors, Muscarinic,
pubmed-meshheading:12419388-Structure-Activity Relationship
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pubmed:year |
2002
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pubmed:articleTitle |
Enhancement of pharmacokinetic properties and in vivo efficacy of benzylidene ketal M(2) muscarinic receptor antagonists via benzamide modification.
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pubmed:affiliation |
Schering-Plough Research Institute, Kenilworth, NJ 07033, USA. craig.boyle@spcorp.com
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pubmed:publicationType |
Journal Article
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