3,5-Bicyclic aryl piperidines: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation

doi:10.1016/j.bmcl.2005.08.035

Bioorganic & Medicinal Chemistry Letters

Volume 15, Issue 22, 15 November 2005, Pages 4889-4897

https://doi.org/10.1016/j.bmcl.2005.08.035 Get rights and content

Abstract

3,5-Bicyclic aryl piperidines are a new class of high-affinity α4β2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the α4β2 nicotinic acetylcholine receptor for smoking cessation, and a number of compounds fulfill potency, selectivity, and efficacy requirements in vitro. In vivo, selected agents demonstrate potent partial agonist efficacy on the mesolimbic dopamine system, a key measure of therapeutic potential for smoking cessation.

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3,5-Bicyclic aryl piperidines: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation

Abstract

Graphical abstract

Neuropharmacology

Mol. Pharmacol.

Curr. Drug. Targets CNS Neuro. Disord.

Psychopharmacology

Annu. Rev. Med.

Respiration

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J. Am. Chem. Soc.

J. Org. Chem.

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Pharmacol. Biochem. Behav.

J. Clin. Psychiatry. Monograph.

Addiction

Pharmacol. Biochem. Behav.

J. Nic. Tobacco Res.

J. Neurobiol.

Addiction

Mayo Clin. Proc.

Drugs

Drug Disc. Today

CNS Drugs

J. Theor. Biol.

Bioorg. Med. Chem. Lett.