Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT(1A) partial agonists - PubMed (original) (raw)

. 2011 Jan 15;21(2):865-8.

doi: 10.1016/j.bmcl.2010.11.066. Epub 2010 Nov 21.

Brian M Campbell, Amy B Dounay, David L Gray, Longfei Xie, Christopher J O'Donnell, Nancy C Stratman, Kim Zoski, Elena Drummond, Gary Bora, Al Probert, Tammy Whisman

Affiliations

PMID: 21185183
DOI: 10.1016/j.bmcl.2010.11.066

Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT(1A) partial agonists

Martin Pettersson et al. Bioorg Med Chem Lett. 2011.

Abstract

Compounds with combined norepinephrine reuptake inhibitor (NRI) and serotonin 1A (5-HT(1A)) partial agonist pharmacology may offer a new therapeutic approach for treating symptoms of neuropsychiatric disorders including ADHD, depression, and anxiety. Herein we describe the design and optimization of novel chemical matter that exhibits favorable dual NRI and 5-HT(1A) partial agonist activity. Lead compounds in this series were found to be devoid of activity at the dopamine transporter and were shown to be brain penetrant with high receptor occupancy.

Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT(1A) partial agonists - PubMed (original) (raw)

Design, synthesis, and pharmacological evaluation of azetedine and pyrrolidine derivatives as dual norepinephrine reuptake inhibitors and 5-HT(1A) partial agonists

Abstract

MeSH terms

Substances

LinkOut - more resources

Full Text Sources

Other Literature Sources

Chemical Information