Abstract
A series of highly potent & selective adamantane derived CB2 agonists was identified in a high-throughput screen. A SAR was established and physicochemical properties were significantly improved. This was accompanied by potency of the compounds on the Q63R variant and varying β-arrestin data which will support the insight into their relevance for the in vivo situation.
Copyright © 2013 Elsevier Ltd. All rights reserved.
MeSH terms
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Adamantane / analogs & derivatives*
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Adamantane / pharmacology
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Cannabinoid Receptor Agonists / chemistry*
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Cannabinoid Receptor Agonists / pharmacology*
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Drug Evaluation, Preclinical / methods
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High-Throughput Screening Assays / methods
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Humans
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Models, Molecular
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Receptor, Cannabinoid, CB2 / agonists*
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Structure-Activity Relationship
Substances
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Cannabinoid Receptor Agonists
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Receptor, Cannabinoid, CB2
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Adamantane