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1,3-Biarylureas as selective non-peptide antagonists of the orexin-1 receptor
- Source :
- Bioorganic & Medicinal Chemistry Letters. 11:1907-1910
- Publication Year :
- 2001
- Publisher :
- Elsevier BV, 2001.
-
Abstract
- This communication reports SARs for the first orexin-1 receptor antagonist series of 1-aryl-3-quinolin-4-yl and 1-aryl-3-naphthyridin-4-yl ureas. One of these compounds, 31 (SB-334867), has excellent selectivity for the orexin-1 receptor, blood-brain barrier permeability and shows in vivo activity following ip dosing.
- Subjects :
- Central Nervous System
Receptors, Neuropeptide
Indoles
medicine.drug_class
Clinical Biochemistry
Pharmaceutical Science
CHO Cells
Pharmacology
Blood–brain barrier
Sensitivity and Specificity
Biochemistry
Permeability
Receptors, G-Protein-Coupled
Structure-Activity Relationship
SB-334867
Orexin Receptors
In vivo
Cricetinae
Drug Discovery
medicine
Animals
Humans
Urea
Selective receptor modulator
Naphthyridines
Infusions, Intravenous
Receptor
Molecular Biology
Benzoxazoles
Chemistry
Organic Chemistry
Antagonist
Receptor antagonist
Orexin
medicine.anatomical_structure
Blood-Brain Barrier
Quinolines
Molecular Medicine
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 11
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....5e603ea593060555151d534b4cadea8d