Journal article
Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor
Bioorganic & medicinal chemistry letters, v 14(22), pp 5605-5609
15 Nov 2004
PMID: 15482933
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
[Display omitted]
SAR studies of a series of piperazinebenzylamines resulted in the discovery of potent antagonists of the human melanocortin-4 receptor. Compounds
11c,
11d, and
11l, which had
K
i values of 21, 14, and 15
nM, respectively, possessed low efficacy in cAMP stimulation (∼15% of α-MSH maximal level) mediated by MC4R, and functioned as antagonists in inhibition of α-MSH-stimulated cAMP release in a dose-dependent manner (
11l, IC
50
=
36
nM).
Metrics
Details
- Title
- Piperazinebenzylamines as potent and selective antagonists of the human melanocortin-4 receptor
- Creators
- Joseph Pontillo - Neurocrine Biosciences (United States)Joseph A. Tran - Neurocrine Biosciences (United States)Beth A. Fleck - Neurocrine Biosciences (United States)Dragan Marinkovic - Neurocrine Biosciences (United States)Melissa Arellano - Neurocrine Biosciences (United States)Fabio C. Tucci - Neurocrine Biosciences (United States)Marion Lanier - Neurocrine Biosciences (United States)Jodie Nelson - Neurocrine Biosciences (United States)Jessica Parker - Neurocrine Biosciences (United States)John Saunders - Neurocrine Biosciences (United States)Brian Murphy - Neurocrine Biosciences (United States)Alan C. Foster - Neurocrine Biosciences (United States)Chen Chen - Neurocrine Biosciences (United States)
- Publication Details
- Bioorganic & medicinal chemistry letters, v 14(22), pp 5605-5609
- Publisher
- Elsevier
- Number of pages
- 5
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Pharmacology and Physiology
- Web of Science ID
- WOS:000224715300030
- Scopus ID
- 2-s2.0-5144234838
- Other Identifier
- 991021902519804721
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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