In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation : Carbon analogs of (-)-cytisine

Jotham W COE; Michael G VETELINO; David W SCHULZ; Hans ROLLEMA; F. David TINGLEY; Brian T O'NEILL; Crystal G BASHORE; Michael C WIRTZ; Paige R BROOKS; Eric P ARNOLD; Lorraine A LEBEL; Carol B FOX; Steven B SANDS; Thomas I DAVIS

doi:10.1016/j.bmcl.2005.04.036

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In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation : Carbon analogs of (-)-cytisine

Journal article

Peer reviewed

In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation : Carbon analogs of (-)-cytisine

Jotham W COE, Michael G VETELINO, David W SCHULZ, Hans ROLLEMA, F. David TINGLEY, Brian T O'NEILL, Crystal G BASHORE, Michael C WIRTZ, Paige R BROOKS, Eric P ARNOLD, …

Bioorganic & medicinal chemistry letters, Vol.15(12), pp.2974-2979

2005

DOI: 10.1016/j.bmcl.2005.04.036

PMID: 15908213

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https://doi.org/10.7270/q25q4wwbView

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Abstract

The preparation and biological activity of analogs of (-)-cytisine, an alpha4beta2 nicotinic receptor partial agonist, are discussed. All-carbon-containing phenyl ring replacements of the pyridone ring system, generated via Heck cyclization protocols, exhibited weaker affinity and lower efficacy partial agonist profiles relative to (-)-cytisine. In vivo, selected compounds exhibit lower efficacy partial agonist profiles than that of (-)-cytisine.

Toxicology

Neuropharmacology

Neurotransmitters. Neurotransmission. Receptors

Pharmacology. Drug treatments

Biological and medical sciences

Cholinergic system

Medical sciences

Tobacco, tobacco smoking

Details

Title: Subtitle: In pursuit of α4β2 nicotinic receptor partial agonists for smoking cessation : Carbon analogs of (-)-cytisine
Creators: Jotham W COE - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Michael G VETELINO - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
David W SCHULZ - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Hans ROLLEMA - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
F. David TINGLEY - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Brian T O'NEILL - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Crystal G BASHORE - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Michael C WIRTZ - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Paige R BROOKS - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Eric P ARNOLD - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Lorraine A LEBEL - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Carol B FOX - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Steven B SANDS - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Thomas I DAVIS - Pfizer Global Research and Development, Grolon Laboratories, Eastern Point Road, Groton, CT 06340, United States
Resource Type: Journal article
Publication Details: Bioorganic & medicinal chemistry letters, Vol.15(12), pp.2974-2979
DOI: 10.1016/j.bmcl.2005.04.036
PMID: 15908213
NLM abbreviation: Bioorg Med Chem Lett
ISSN: 0960-894X
eISSN: 1464-3405
Publisher: Elsevier
Language: English
Date published: 2005
Academic Unit: Endocrinology and Metabolism; Internal Medicine
Record Identifier: 9984094376602771

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