Old and new pharmacology: positive allosteric modulation of the alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/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 alpha7 nicotinic acetylcholine receptor by the 5-hydroxytryptamine(2B/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 E Dunlop and Tim Lock and Brian Jow and Fabrizio Sitzia and Steven M. Grauer and Flora Jow and Angela Kramer and Mark Bowlby and Andrew Randall and Dianne M Kowal and Adam Gilbert and Thomas A. Comery and James P Larocque and Veronica Soloveva and Jon Thomas Brown and Renza Roncarati},
  journal={The Journal of pharmacology and experimental therapeutics},
  year={2009},
  volume={328 3},
  pages={766-76}
}
The alpha7 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-hydroxytryptamine(2B/2C) receptor antagonist, produced an 8-fold potentiation of the… CONTINUE READING

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