Journal article
Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways
Bioorganic & medicinal chemistry, v 17(17), pp 6442-6450
2009
PMID: 19646882
Featured in Collection : UN Sustainable Development Goals @ Drexel
Abstract
A novel family of 1,3,5-trisubstituted 1,2,4-triazoles was discovered as potent and selective ligands for the δ opioid receptor by rational design. These compounds exhibited differential stimulation of signaling pathways.
A novel family of 1,3,5-trisubstituted 1,2,4-triazoles was discovered as potent and selective ligands for the δ opioid receptor by rational design. Compound
5b exhibited low-nanomolar in vitro binding affinity (IC
50
=
5.8
nM), excellent selectivity for the δ opioid receptor over the alternative μ and κ opioid receptors, full agonist efficacy in receptor down-regulation and MAP kinase activation assays, and low-efficacy partial agonist activity in stimulation of GTPγS binding. The apparent discrepancy observed in these functional assays may stem from different signaling pathways involved in each case, as found previously for other G-protein coupled receptors. More biological studies are underway to better understand the differential stimulation of signaling pathways by these novel compounds.
Metrics
Details
- Title
- Novel delta opioid receptor agonists exhibit differential stimulation of signaling pathways
- Creators
- Youyi Peng - Department of Pharmacology, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School (UMDNJ-RWJMS) and the Informatics Institute of UMDNJ, Piscataway, NJ 08854, United StatesQiang Zhang - Department of Pharmacology, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School (UMDNJ-RWJMS) and the Informatics Institute of UMDNJ, Piscataway, NJ 08854, United StatesSonia Arora - Department of Pharmacology, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School (UMDNJ-RWJMS) and the Informatics Institute of UMDNJ, Piscataway, NJ 08854, United StatesSusan M Keenan - Department of Pharmacology, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School (UMDNJ-RWJMS) and the Informatics Institute of UMDNJ, Piscataway, NJ 08854, United StatesSandhya Kortagere - Department of Pharmacology, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School (UMDNJ-RWJMS) and the Informatics Institute of UMDNJ, Piscataway, NJ 08854, United StatesKenneth M Wannemacher - Department of Biochemistry and Molecular Biology, University of Medicine and Dentistry of New Jersey, New Jersey Medical School (UMDNJ-NJMS), Newark, NJ 07101, United StatesRichard D Howells - Department of Biochemistry and Molecular Biology, University of Medicine and Dentistry of New Jersey, New Jersey Medical School (UMDNJ-NJMS), Newark, NJ 07101, United StatesWilliam J Welsh - Department of Pharmacology, University of Medicine and Dentistry of New Jersey-Robert Wood Johnson Medical School (UMDNJ-RWJMS) and the Informatics Institute of UMDNJ, Piscataway, NJ 08854, United States
- Publication Details
- Bioorganic & medicinal chemistry, v 17(17), pp 6442-6450
- Publisher
- Elsevier
- Resource Type
- Journal article
- Language
- English
- Academic Unit
- Microbiology and Immunology
- Web of Science ID
- WOS:000269029100036
- Scopus ID
- 2-s2.0-68949114811
- Other Identifier
- 991014878287504721
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InCites Highlights
Data related to this publication, from InCites Benchmarking & Analytics tool:
- Web of Science research areas
- Biochemistry & Molecular Biology
- Chemistry, Medicinal
- Chemistry, Organic