A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.

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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

A novel series of [3.2.1] azabicyclic biaryl ethers as alpha3beta4 and alpha6/4beta4 nicotinic receptor agonists.

Bioorg Med Chem Lett. 2010 Aug 15;20(16):4749-52. doi: 10.1016/j.bmcl.2010.06.142.

PubMed ID

20663668 [ View in PubMed

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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.

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Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Nicotine	Neuronal acetylcholine receptor subunit beta-2	Ki (nM)	9.46	N/A	N/A	Details