| Title : A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6\/4beta4 nicotinic receptor agonists - Lowe_2010_Bioorg.Med.Chem.Lett_20_4749 |
| Author(s) : Lowe JA, 3rd , DeNinno SL , Coe JW , Zhang L , Mente S , Hurst RS , Mather RJ , Ward KM , Shrikhande A , Rollema H , Johnson DE , Horner W , Gorczyca R , Tingley FD, 3rd , Kozak R , Majchrzak MJ , Tritto T , Sadlier J , Shaffer CL , Ellerbrock B , Osgood SM , MacDougall MC , McDowell LL |
| Ref : Bioorganic & Medicinal Chemistry Lett , 20 :4749 , 2010 |
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Abstract :
We report the synthesis of a series of [3.2.1]azabicyclic biaryl ethers as selective agonists of alpha3- and alpha6-containing nicotinic receptors. In particular, compound 17a from this series is a potent alpha3beta4 and alpha6/4beta4 receptor agonist in terms of both binding and functional activity. Compound 17a also shows potent in vivo activity in CNS-mediated animal models that are sensitive to antipsychotic drugs. Compound 17a may thus be a useful tool for studying the role of alpha3beta4 and alpha6/4beta4 nicotinic receptors in CNS pharmacology. |
| PubMedSearch : Lowe_2010_Bioorg.Med.Chem.Lett_20_4749 |
| PubMedID: 20663668 |
Lowe JA, 3rd, DeNinno SL, Coe JW, Zhang L, Mente S, Hurst RS, Mather RJ, Ward KM, Shrikhande A, Rollema H, Johnson DE, Horner W, Gorczyca R, Tingley FD, 3rd, Kozak R, Majchrzak MJ, Tritto T, Sadlier J, Shaffer CL, Ellerbrock B, Osgood SM, MacDougall MC, McDowell LL (2010)
A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6\/4beta4 nicotinic receptor agonists
Bioorganic & Medicinal Chemistry Lett
20 :4749
Lowe JA, 3rd, DeNinno SL, Coe JW, Zhang L, Mente S, Hurst RS, Mather RJ, Ward KM, Shrikhande A, Rollema H, Johnson DE, Horner W, Gorczyca R, Tingley FD, 3rd, Kozak R, Majchrzak MJ, Tritto T, Sadlier J, Shaffer CL, Ellerbrock B, Osgood SM, MacDougall MC, McDowell LL (2010)
Bioorganic & Medicinal Chemistry Lett
20 :4749