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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
10
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pubmed:dateCreated |
2009-5-22
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pubmed:abstractText |
The discovery of a series of pyrrole-sulfonamides as positive allosteric modulators (PAM) of alpha7 nAChRs is described. Optimization of this series led to the identification of 19 (A-867744), a novel type II PAM with good potency and selectivity. Compound 19 showed acceptable pharmacokinetic profile across species and brain levels sufficient to modulate alpha7 nAChRs. In a rodent model of sensory gating, 19 normalized gating deficits. These results suggest that 19 represents a novel class of molecules capable of allosteric modulation of the alpha7 nAChRs.
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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 |
1520-4804
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pubmed:author |
pubmed-author:BriggsClark ACA,
pubmed-author:BunnelleWilliam HWH,
pubmed-author:CurtisMichael PMP,
pubmed-author:El-KouhenRachidR,
pubmed-author:FaghihRaminR,
pubmed-author:GfesserGregory AGA,
pubmed-author:GopalakrishnanMuraliM,
pubmed-author:GopalakrishnanSujatha MSM,
pubmed-author:GronlienJens HalvardJH,
pubmed-author:MalyszJohnJ,
pubmed-author:MarshKennan CKC,
pubmed-author:RadekRichard JRJ,
pubmed-author:RobbHolly MHM,
pubmed-author:SarrisKathy AKA,
pubmed-author:WeenHildeH,
pubmed-author:WetterstrandCarolineC
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pubmed:issnType |
Electronic
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pubmed:day |
28
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pubmed:volume |
52
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
3377-84
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pubmed:dateRevised |
2010-6-4
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pubmed:meshHeading |
pubmed-meshheading:19419141-Allosteric Regulation,
pubmed-meshheading:19419141-Animals,
pubmed-meshheading:19419141-Brain,
pubmed-meshheading:19419141-Cells, Cultured,
pubmed-meshheading:19419141-Drug Discovery,
pubmed-meshheading:19419141-Mice,
pubmed-meshheading:19419141-Microsomes,
pubmed-meshheading:19419141-Oocytes,
pubmed-meshheading:19419141-Patch-Clamp Techniques,
pubmed-meshheading:19419141-Pharmacokinetics,
pubmed-meshheading:19419141-Pyrroles,
pubmed-meshheading:19419141-Receptors, Nicotinic,
pubmed-meshheading:19419141-Sensory Gating,
pubmed-meshheading:19419141-Sulfonamides,
pubmed-meshheading:19419141-Xenopus laevis
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pubmed:year |
2009
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pubmed:articleTitle |
Discovery of 4-(5-(4-chlorophenyl)-2-methyl-3-propionyl-1H-pyrrol-1-yl)benzenesulfonamide (A-867744) as a novel positive allosteric modulator of the alpha7 nicotinic acetylcholine receptor.
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pubmed:affiliation |
Neuroscience Research, Global Pharmaceutical Research and Development, Abbott Laboratories, Abbott Park, Illinois 60064, USA. ramin.faghih@abbott.com
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pubmed:publicationType |
Journal Article
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