Journal article
Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H-3 receptor antagonists with robust wake-promoting activity
Bioorganic & medicinal chemistry letters, v 21(21), pp 6362-6365
01 Nov 2011
PMID: 21944855
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
A series of pyridazinone-phenethylamine derivatives with moderate to low nanomolar affinity for rat and human H3R are described. These analogs exhibited excellent selectivity and metabolic stability, with acceptable rat pharmacokinetic properties. In vivo, 7 and 11 demonstrated potent H3R functional antagonism in the rat dipsogenia model and robust wake-promoting activity in the rat electroencephalogram/electromyography (EEG/EMG) model. (C) 2011 Elsevier Ltd. All rights reserved.
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Details
- Title
- Synthesis and evaluation of pyridazinone-phenethylamine derivatives as selective and orally bioavailable histamine H-3 receptor antagonists with robust wake-promoting activity
- Creators
- Reddeppa Reddy Dandu - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAJohn A. Gruner - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAJoanne R. Mathiasen - Cephalon Inc, Discovery Res, W Chester, PA 19380 USALisa D. Aimone - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAGreg Hostetler - Cephalon Inc, Discovery Res, W Chester, PA 19380 USACaitlyn Benfield - Cephalon Inc, Discovery Res, W Chester, PA 19380 USARobert J. Bendesky - Cephalon Inc, Discovery Res, W Chester, PA 19380 USAVal R. Marcy - Cephalon Inc, Discovery Res, W Chester, PA 19380 USARita Raddatz - Cephalon Inc, Discovery Res, W Chester, PA 19380 USARobert L. Hudkins - Cephalon Inc, Discovery Res, W Chester, PA 19380 USA
- Publication Details
- Bioorganic & medicinal chemistry letters, v 21(21), pp 6362-6365
- Publisher
- Elsevier
- Number of pages
- 4
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000296025900030
- Scopus ID
- 2-s2.0-80054781630
- Other Identifier
- 991021900016804721
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InCites Highlights
Data related to this publication, from InCites Benchmarking & Analytics tool:
- Web of Science research areas
- Chemistry, Medicinal
- Chemistry, Organic