Abstract
The peripheral benzodiazepine receptors (PBRs) have been identified to bind selectively benzodiazepine ligands and an isoquinoline carboxamide derivative PK 11195 with high affinity. PBRs are present in the central nervous system (CNS), peripheral tissues, and most organs in the human body. PBRs are different from the central benzodiazepine receptors (CBRs) related to the nerve cell membrane GABAA receptor and are thought to play several physiological and pathophysiological functions in the CNS and immune system due to their meanly localization in glial cells, the mitochondrial outer membrane of peripheral cells and blood leucocytes and to their important roles in steroidogenesis, cell proliferation and differentiation. Recent research has shown that the density of PBRs is significanly increased in CNS several disorders, such as epilepsy, multiple sclerosis, cerebral ischemia, astrocytoma, brain injury and neurodegenerative diseases.Recent progress in the pharmacology of PBRs is reviewed here with respect to the functions in the brain and peripheral tissues including apoptosis, immune system modulation, seizure promotion, reactions of anticonvulsants on peripheral blood cells, and adverse drug reactions (ADR) of anticonvulsants.
Keywords: benzodiazepine receptor, pbrs, isoquinoline carboxamide, pk11195
Current Medicinal Chemistry
Title: The Role of Peripheral Benzodiazepine Receptors (PBRs) in CNS Pathophysiology
Volume: 9 Issue: 15
Author(s): Senyang Lang
Affiliation:
Keywords: benzodiazepine receptor, pbrs, isoquinoline carboxamide, pk11195
Abstract: The peripheral benzodiazepine receptors (PBRs) have been identified to bind selectively benzodiazepine ligands and an isoquinoline carboxamide derivative PK 11195 with high affinity. PBRs are present in the central nervous system (CNS), peripheral tissues, and most organs in the human body. PBRs are different from the central benzodiazepine receptors (CBRs) related to the nerve cell membrane GABAA receptor and are thought to play several physiological and pathophysiological functions in the CNS and immune system due to their meanly localization in glial cells, the mitochondrial outer membrane of peripheral cells and blood leucocytes and to their important roles in steroidogenesis, cell proliferation and differentiation. Recent research has shown that the density of PBRs is significanly increased in CNS several disorders, such as epilepsy, multiple sclerosis, cerebral ischemia, astrocytoma, brain injury and neurodegenerative diseases.Recent progress in the pharmacology of PBRs is reviewed here with respect to the functions in the brain and peripheral tissues including apoptosis, immune system modulation, seizure promotion, reactions of anticonvulsants on peripheral blood cells, and adverse drug reactions (ADR) of anticonvulsants.
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Cite this article as:
Lang Senyang, The Role of Peripheral Benzodiazepine Receptors (PBRs) in CNS Pathophysiology, Current Medicinal Chemistry 2002; 9 (15) . https://dx.doi.org/10.2174/0929867023369745
DOI https://dx.doi.org/10.2174/0929867023369745 |
Print ISSN 0929-8673 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-533X |
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