Old and New Pharmacology: Positive Allosteric Modulation of the α7 Nicotinic Acetylcholine Receptor by the 5-Hydroxytryptamine2B/C Receptor Antagonist SB-206553 (3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b′]di pyrrole-1(2H)-carboxamide)

@article{Dunlop2009OldAN,
  title={Old and New Pharmacology: Positive Allosteric Modulation of the $\alpha$7 Nicotinic Acetylcholine Receptor by the 5-Hydroxytryptamine2B/C Receptor Antagonist SB-206553 (3,5-Dihydro-5-methyl-N-3-pyridinylbenzo[1,2-b:4,5-b′]di pyrrole-1(2H)-carboxamide)},
  author={John Dunlop and Tim Yeung Wai Lock and Brian Jow and Fabrizio Sitzia and Steven M. Grauer and Flora Jow and Angela Kramer and Mark Bowlby and Andrew P. Randall and Dianne M Kowal and Adam Matthew Gilbert and Thomas A. Comery and James Larocque and Veronica Soloveva and Jon Brown and Renza Roncarati},
  journal={Journal of Pharmacology and Experimental Therapeutics},
  year={2009},
  volume={328},
  pages={766 - 776}
}
The α7 nicotinic acetylcholine receptor (nAChR) has been implicated in Alzheimer's disease and schizophrenia, leading to efforts targeted toward discovering agonists and positive allosteric modulators (PAMs) of this receptor. In a Ca2+ flux fluorometric imaging plate reader assay, SB-206553 (3,5-dihydro-5-methyl -N-3-pyridinylbenzo [1, 2-b:4,5 -b′]-di pyrrole-1(2H)-carboxamide), a compound known as a 5-hydroxytryptamine2B/2C receptor antagonist, produced an 8-fold potentiation of the evoked… 

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