Abstract
CB1 receptor antagonists that are peripherally restricted were targeted. Compounds with permanent charge as well as compounds that have increased polar surface area were made and tested against CB1 for binding and activity. Sulfonamide and sulfamide with high polar surface area and good activity at CB1 were rationally designed and pharmacologically tested. Further optimization of these compounds and testing could lead to the development of a new class of therapeutics to treat disorders where the CB1 receptor system has been implicated.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / genetics
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Animals
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CHO Cells
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Cannabinoid Receptor Modulators / chemical synthesis*
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Cannabinoid Receptor Modulators / chemistry
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Cannabinoid Receptor Modulators / metabolism
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Cannabinoid Receptor Modulators / pharmacology*
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Cell Line
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Cricetinae
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Dogs
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Drug Design*
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Drug Discovery*
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Ligands
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Molecular Structure
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Piperidines / metabolism
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Protein Binding
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Pyrazoles / metabolism
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Radioligand Assay
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Receptor, Cannabinoid, CB1 / antagonists & inhibitors*
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Receptor, Cannabinoid, CB1 / chemistry
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Rimonabant
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Stereoisomerism
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Structure-Activity Relationship
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Sulfonamides / chemistry
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Cannabinoid Receptor Modulators
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Ligands
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Piperidines
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Pyrazoles
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Receptor, Cannabinoid, CB1
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Sulfonamides
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Rimonabant