| Title : 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 - Acker_2008_Bioorg.Med.Chem.Lett_18_3611 |
| Author(s) : Acker BA , Jacobsen EJ , Rogers BN , Wishka DG , Reitz SC , Piotrowski DW , Myers JK , Wolfe ML , Groppi VE , Thornburgh BA , Tinholt PM , Walters RR , Olson BA , Fitzgerald L , Staton BA , Raub TJ , Krause M , Li KS , Hoffmann WE , Hajos M , Hurst RS , Walker DP |
| Ref : Bioorganic & Medicinal Chemistry Lett , 18 :3611 , 2008 |
|
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. |
| PubMedSearch : Acker_2008_Bioorg.Med.Chem.Lett_18_3611 |
| PubMedID: 18490160 |
Acker BA, Jacobsen EJ, Rogers BN, Wishka DG, Reitz SC, Piotrowski DW, Myers JK, Wolfe ML, Groppi VE, Thornburgh BA, Tinholt PM, Walters RR, Olson BA, Fitzgerald L, Staton BA, Raub TJ, Krause M, Li KS, Hoffmann WE, Hajos M, Hurst RS, Walker DP (2008)
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
Bioorganic & Medicinal Chemistry Lett
18 :3611
Acker BA, Jacobsen EJ, Rogers BN, Wishka DG, Reitz SC, Piotrowski DW, Myers JK, Wolfe ML, Groppi VE, Thornburgh BA, Tinholt PM, Walters RR, Olson BA, Fitzgerald L, Staton BA, Raub TJ, Krause M, Li KS, Hoffmann WE, Hajos M, Hurst RS, Walker DP (2008)
Bioorganic & Medicinal Chemistry Lett
18 :3611