Abstract
The P2X7 receptor is involved in several processes relevant to inflammation (cytokine release, NO generation, killing of intracellular pathogens, cytotoxicity), thus, it may be an appealing target for pharmacological intervention. The characterisation of native and recombinant P2X7 receptor continues to be hindered by the lack of specific and subtypeselective agonists and antagonists. BzATP is currently the most potent agonist known at the endogenous and recombinant P2X7 receptor A tyrosine derivative named KN-62 exhibits selective P2X7 receptor-blocking properties. In this review article we have reported novel series of KN-62-related compounds of the general structure R1-Tyr(OR2)-piperazinyl-R3, in which three positions (R1, R2 and R3) were systematically varied. Two recent articles published by AstraZeneca have reported that novel series of cyclic imides and adamantane amides are potent P2X7 receptor antagonists.
Keywords: p2x7 purinoreceptor, atp-receptor, ionotropic receptor, agonist, antagonis
Current Topics in Medicinal Chemistry
Title: Agonists and Antagonists Acting at P2X7 Receptor
Volume: 4 Issue: 16
Author(s): Pier Giovanni Baraldi, Francesco Di Virgilio and Romeo Romagnoli
Affiliation:
Keywords: p2x7 purinoreceptor, atp-receptor, ionotropic receptor, agonist, antagonis
Abstract: The P2X7 receptor is involved in several processes relevant to inflammation (cytokine release, NO generation, killing of intracellular pathogens, cytotoxicity), thus, it may be an appealing target for pharmacological intervention. The characterisation of native and recombinant P2X7 receptor continues to be hindered by the lack of specific and subtypeselective agonists and antagonists. BzATP is currently the most potent agonist known at the endogenous and recombinant P2X7 receptor A tyrosine derivative named KN-62 exhibits selective P2X7 receptor-blocking properties. In this review article we have reported novel series of KN-62-related compounds of the general structure R1-Tyr(OR2)-piperazinyl-R3, in which three positions (R1, R2 and R3) were systematically varied. Two recent articles published by AstraZeneca have reported that novel series of cyclic imides and adamantane amides are potent P2X7 receptor antagonists.
Export Options
About this article
Cite this article as:
Baraldi Giovanni Pier, Virgilio Di Francesco and Romagnoli Romeo, Agonists and Antagonists Acting at P2X7 Receptor, Current Topics in Medicinal Chemistry 2004; 4 (16) . https://dx.doi.org/10.2174/1568026043387223
DOI https://dx.doi.org/10.2174/1568026043387223 |
Print ISSN 1568-0266 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4294 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
- Announcements
Related Articles
-
Microscopies at the Nanoscale for Nano-Scale Drug Delivery Systems
Current Drug Targets Context-dependent Action of Transforming Growth Factor β Family Members on Normal and Cancer Stem Cells
Current Pharmaceutical Design Proteomics in the Search for Biomarkers of Animal Cancer
Current Protein & Peptide Science The Hsp32 Inhibitors SMA-ZnPP and PEG-ZnPP Exert Major Growth-Inhibitory Effects on CD34+/CD38+ and CD34+/CD38- AML Progenitor Cells
Current Cancer Drug Targets Therapeutic Potential of Janus Kinase 3 (JAK3) Inhibitors
Current Pharmaceutical Design CXXC5 Associates with Smads to Mediate TNF-α Induced Apoptosis
Current Molecular Medicine One Special Question to Start with: Can HIF/NFkB be a Target in Inflammation?
Endocrine, Metabolic & Immune Disorders - Drug Targets The Chemistry and Biology of the Bryostatins: Potential PKC Inhibitors in Clinical Development
Current Medicinal Chemistry DNA Methylation: A Possible Target for Current and Future Studies on Cancer?
Epigenetic Diagnosis & Therapy (Discontinued) Need to Think Outside Organ-based Diagnosis to Molecular Diagnostics
Applied Clinical Research, Clinical Trials and Regulatory Affairs Protein Kinase B/AKT and Focal Adhesion Kinase: Two Close Signaling Partners in Cancer
Anti-Cancer Agents in Medicinal Chemistry Systemic and Biophase Bioavailability and Pharmacokinetics of Nanoparticulate Drug Delivery Systems
Current Drug Delivery Development of Arene Ruthenium Antitumor Complexes
Mini-Reviews in Medicinal Chemistry Gene Therapy for Pituitary Tumors
Current Gene Therapy Epigenetic Modifications as Therapeutic Targets
Current Drug Targets Eosinophils in Cancer: Favourable or Unfavourable?
Current Medicinal Chemistry The Complex Biology of FOXO
Current Drug Targets The Significance of Transferrin Receptors in Oncology: the Development of Functional Nano-based Drug Delivery Systems
Current Drug Delivery Specific Immune Intervention with Monoclonal Antibodies for the Treatment of Multiple Sclerosis
Current Medicinal Chemistry Flavonoids: Prospective Drug Candidates
Mini-Reviews in Medicinal Chemistry