Abstract
Purinergic receptor P2X3 has been linked to analgesia in a number of pre-clinical models of pain, and is expressed in the human pain perception pathway. Only few P2X3-selective antagonists have been reported to date. This Letter describes the SAR and in vivo analgesic profile of a novel scaffold of selective P2X3 antagonists.
Copyright © 2012 Elsevier Ltd. All rights reserved.
MeSH terms
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Analgesics / administration & dosage
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Analgesics / chemical synthesis*
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Analgesics / therapeutic use
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Animals
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Chronic Pain / drug therapy*
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Chronic Pain / metabolism
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Dose-Response Relationship, Drug
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High-Throughput Screening Assays
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Humans
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Injections, Spinal
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Injections, Subcutaneous
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Purinergic P2 Receptor Antagonists / administration & dosage
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Purinergic P2 Receptor Antagonists / chemical synthesis*
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Purinergic P2 Receptor Antagonists / therapeutic use
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Pyrimidinones / administration & dosage
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Pyrimidinones / chemical synthesis*
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Pyrimidinones / therapeutic use
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Pyrroles / administration & dosage
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Pyrroles / chemical synthesis*
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Pyrroles / therapeutic use
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Rats
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Rats, Sprague-Dawley
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Receptors, Purinergic P2X3 / chemistry*
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Receptors, Purinergic P2X3 / metabolism
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Small Molecule Libraries
Substances
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Analgesics
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Purinergic P2 Receptor Antagonists
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Pyrimidinones
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Pyrroles
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Receptors, Purinergic P2X3
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Small Molecule Libraries