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Discovery of P2X3 selective antagonists for the treatment of chronic pain.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2012 Apr 01; Vol. 22 (7), pp. 2565-71. Date of Electronic Publication: 2012 Feb 09. - Publication Year :
- 2012
-
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.<br /> (Copyright © 2012 Elsevier Ltd. All rights reserved.)
- Subjects :
- Analgesics administration & dosage
Analgesics therapeutic use
Animals
Chronic Pain metabolism
Dose-Response Relationship, Drug
High-Throughput Screening Assays
Humans
Injections, Spinal
Injections, Subcutaneous
Purinergic P2 Receptor Antagonists administration & dosage
Purinergic P2 Receptor Antagonists therapeutic use
Pyrimidinones administration & dosage
Pyrimidinones therapeutic use
Pyrroles administration & dosage
Pyrroles therapeutic use
Rats
Rats, Sprague-Dawley
Receptors, Purinergic P2X3 metabolism
Small Molecule Libraries
Analgesics chemical synthesis
Chronic Pain drug therapy
Purinergic P2 Receptor Antagonists chemical synthesis
Pyrimidinones chemical synthesis
Pyrroles chemical synthesis
Receptors, Purinergic P2X3 chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 22
- Issue :
- 7
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 22370269
- Full Text :
- https://doi.org/10.1016/j.bmcl.2012.01.124