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1000279-69-5

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Heteromeric neuronal nicotinic acetylcholine receptors with mutant B subunits acquire sensitivity to A7-selective positive allosteric modulatorss
Homomeric a7 nicotinic acetylcholine receptors (nAChR) have an intrinsically low probability of opening that can be overcome by a7-selective positive allosteric modulators (PAMs), which bind at a site involving the second transmembrane domain (TM2). Mutat
Stokes, Clare,Garai, Sumanta,Kulkarni, Abhijit R.,Cantwell, Lucas N.,Noviello, Colleen M.,Hibbs, Ryan E.,Horenstein, Nicole A.,Abboud, Khalil A.,Thakur, Ganesh A.,Papke, Roger L.
p. 252 - 268
(2019)
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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 α7 nicotinic acetylcholine receptor
The discovery of a series of pyrrole-sulfonamides as positive allosteric modulators (PAM) of α7 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
Faghih, Ramin,Gopalakrishnan, Sujatha M.,Gronlien, Jens Halvard,Malysz, John,Briggs, Clark A.,Wetterstrand, Caroline,Ween, Hilde,Curtis, Michael P.,Sarris, Kathy A.,Gfesser, Gregory A.,El-Kouhen, Rachid,Robb, Holly M.,Radek, Richard J.,Marsh, Kennan C.,Bunnelle, William H.,Gopalakrishnan, Murali
experimental part
p. 3377 - 3384
(2010/03/31)

PYRROLE DERIVATIVES AND THEIR METHODS OF USE
The invention relates to a series of substituted pyrrole derivatives, compositions comprising the same, and methods of treating conditions and disorders using such compounds and compositions.
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Page/Page column 59

(2008/06/13)

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Chemical Properties

Boiling Point: 610.0±65.0 °C(Predicted)
Density: 1.33±0.1 g/cm3(Predicted)
Solubility:Soluble in DMSO
PKA: 9.69±0.10(Predicted)
PSA: 90.54000
LogP: 6.12730

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