Literature DB >> 18490160

Discovery of N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide as an agonist of the alpha7 nicotinic acetylcholine receptor: in vitro and in vivo activity.

Brad A Acker1, E Jon Jacobsen, Bruce N Rogers, Donn G Wishka, Steven C Reitz, David W Piotrowski, Jason K Myers, Mark L Wolfe, Vincent E Groppi, Bruce A Thornburgh, Paula M Tinholt, Rodney R Walters, Barbara A Olson, Laura Fitzgerald, Brian A Staton, Thomas J Raub, Michael Krause, Kai S Li, William E Hoffmann, Mihaly Hajos, Raymond S Hurst, Daniel P Walker.   

Abstract

A novel alpha7 nAChR agonist, N-[(3R,5R)-1-azabicyclo[3.2.1]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (3a, PHA-709829), has been identified for the potential treatment of cognitive deficits in schizophrenia. The compound shows potent and selective alpha7 in vitro activity, excellent brain penetration, good rat oral bioavailability and robust in vivo efficacy in a rat auditory sensory gating model.

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Year:  2008        PMID： 18490160     DOI： 10.1016/j.bmcl.2008.04.070

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  16 in total

Review 1.  The therapeutic potential of α7 nicotinic acetylcholine receptor (α7 nAChR) agonists for the treatment of the cognitive deficits associated with schizophrenia.

Authors:  Corinne Beinat; Samuel D Banister; Marco Herrera; Vivian Law; Michael Kassiou
Journal:  CNS Drugs       Date:  2015-07       Impact factor: 5.749

Review 2.  Cancer 'survivor-care': I. the α7 nAChR as potential target for chemotherapy-related cognitive impairment.

Authors:  R B Raffa
Journal:  J Clin Pharm Ther       Date:  2010-08-24       Impact factor: 2.512

3.  The frequency-dependence of the nicotine-induced inhibition of dopamine is controlled by the α7 nicotinic receptor.

Authors:  Andrew T Seipel; Jerrel L Yakel
Journal:  J Neurochem       Date:  2010-08-19       Impact factor: 5.372

4.  Stimulation of nAchRα7 Receptor Inhibits TNF Synthesis and Secretion in Response to LPS Treatment of Mast Cells by Targeting ERK1/2 and TACE Activation.

Authors:  F Guzmán-Mejía; C López-Rubalcava; C González-Espinosa
Journal:  J Neuroimmune Pharmacol       Date:  2017-08-18       Impact factor: 4.147

5.  Preclinical assessment of an adjunctive treatment approach for cognitive impairment associated with schizophrenia using the alpha7 nicotinic acetylcholine receptor agonist WYE-103914/SEN34625.

Authors:  Karen L Marquis; Thomas A Comery; Flora Jow; Rachel L Navarra; Steven M Grauer; Claudine Pulicicchio; Cody Kelley; Julie A Brennan; Renza Roncarati; Carla Scali; Simon Haydar; Chiara Ghiron; Georg C Terstappen; John Dunlop
Journal:  Psychopharmacology (Berl)       Date:  2011-06-04       Impact factor: 4.530

6.  Multiple pharmacophores for the selective activation of nicotinic alpha7-type acetylcholine receptors.

Authors:  Nicole A Horenstein; Fedra M Leonik; Roger L Papke
Journal:  Mol Pharmacol       Date:  2008-09-02       Impact factor: 4.436

7.  α7 nicotinic ACh receptor-deficient mice exhibit sustained attention impairments that are reversed by β2 nicotinic ACh receptor activation.

Authors:  Benjamin Kolisnyk; Mohammed A Al-Onaizi; Vania F Prado; Marco A M Prado
Journal:  Br J Pharmacol       Date:  2015-09-22       Impact factor: 8.739

Review 8.  Therapeutic potential of α7 nicotinic acetylcholine receptor agonists to combat obesity, diabetes, and inflammation.

Authors:  Han Xie; Natesh Yepuri; Qinghe Meng; Ravi Dhawan; Colin A Leech; Oleg G Chepurny; George G Holz; Robert N Cooney
Journal:  Rev Endocr Metab Disord       Date:  2020-08-26       Impact factor: 6.514

9.  TC-5619: an alpha7 neuronal nicotinic receptor-selective agonist that demonstrates efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia.

Authors:  T A Hauser; A Kucinski; K G Jordan; G J Gatto; S R Wersinger; R A Hesse; E K Stachowiak; M K Stachowiak; R L Papke; P M Lippiello; M Bencherif
Journal:  Biochem Pharmacol       Date:  2009-05-29       Impact factor: 5.858

10.  Neuroprotective and anti-inflammatory effects of a therapy combining agonists of nicotinic α7 and σ1 receptors in a rat model of Parkinson's disease.

Authors:  Steven Vetel; Laura Foucault-Fruchard; Claire Tronel; Frédéric Buron; Jackie Vergote; Sylvie Bodard; Sylvain Routier; Sophie Sérrière; Sylvie Chalon
Journal:  Neural Regen Res       Date:  2021-06       Impact factor: 5.135
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