Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders
The ATP-gated P2X7 ion channel is an abundant microglial protein in the CNS that plays an important pathological role in executing ATP-driven danger signal transduction. Emerging data has generated scientific interest and excitement around targeting the P2X7 ion channel as a potential drug target fo...
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| Format: | Article |
| Language: | English |
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Frontiers Media S.A.
2018-02-01
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| Series: | Frontiers in Pharmacology |
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| Online Access: | http://journal.frontiersin.org/article/10.3389/fphar.2018.00030/full |
| _version_ | 1811240042766532608 |
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| author | Anindya Bhattacharya |
| author_facet | Anindya Bhattacharya |
| author_sort | Anindya Bhattacharya |
| collection | DOAJ |
| description | The ATP-gated P2X7 ion channel is an abundant microglial protein in the CNS that plays an important pathological role in executing ATP-driven danger signal transduction. Emerging data has generated scientific interest and excitement around targeting the P2X7 ion channel as a potential drug target for CNS disorders. Over the past years, a wealth of data has been published on CNS P2X7 biology, in particular the role of P2X7 in microglial cells, and in vivo effects of brain-penetrant P2X7 antagonists. Likewise, significant progress has been made around the medicinal chemistry of CNS P2X7 ligands, as antagonists for in vivo target validation in models of CNS diseases, to identification of two clinical compounds (JNJ-54175446 and JNJ-55308942) and finally, discovery of P2X7 PET ligands. This review is an attempt to bring together the current understanding of P2X7 in the CNS with a focus on P2X7 as a drug target in neuropsychiatric disorders. |
| first_indexed | 2024-04-12T13:13:29Z |
| format | Article |
| id | doaj.art-e7062608e938493d90d93be7ec6d6219 |
| institution | Directory Open Access Journal |
| issn | 1663-9812 |
| language | English |
| last_indexed | 2024-04-12T13:13:29Z |
| publishDate | 2018-02-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Pharmacology |
| spelling | doaj.art-e7062608e938493d90d93be7ec6d62192022-12-22T03:31:48ZengFrontiers Media S.A.Frontiers in Pharmacology1663-98122018-02-01910.3389/fphar.2018.00030319765Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric DisordersAnindya BhattacharyaThe ATP-gated P2X7 ion channel is an abundant microglial protein in the CNS that plays an important pathological role in executing ATP-driven danger signal transduction. Emerging data has generated scientific interest and excitement around targeting the P2X7 ion channel as a potential drug target for CNS disorders. Over the past years, a wealth of data has been published on CNS P2X7 biology, in particular the role of P2X7 in microglial cells, and in vivo effects of brain-penetrant P2X7 antagonists. Likewise, significant progress has been made around the medicinal chemistry of CNS P2X7 ligands, as antagonists for in vivo target validation in models of CNS diseases, to identification of two clinical compounds (JNJ-54175446 and JNJ-55308942) and finally, discovery of P2X7 PET ligands. This review is an attempt to bring together the current understanding of P2X7 in the CNS with a focus on P2X7 as a drug target in neuropsychiatric disorders.http://journal.frontiersin.org/article/10.3389/fphar.2018.00030/fullP2X7microgliadepressionIL-1betaschizophreniabipolar disorder |
| spellingShingle | Anindya Bhattacharya Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders Frontiers in Pharmacology P2X7 microglia depression IL-1beta schizophrenia bipolar disorder |
| title | Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders |
| title_full | Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders |
| title_fullStr | Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders |
| title_full_unstemmed | Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders |
| title_short | Recent Advances in CNS P2X7 Physiology and Pharmacology: Focus on Neuropsychiatric Disorders |
| title_sort | recent advances in cns p2x7 physiology and pharmacology focus on neuropsychiatric disorders |
| topic | P2X7 microglia depression IL-1beta schizophrenia bipolar disorder |
| url | http://journal.frontiersin.org/article/10.3389/fphar.2018.00030/full |
| work_keys_str_mv | AT anindyabhattacharya recentadvancesincnsp2x7physiologyandpharmacologyfocusonneuropsychiatricdisorders |