دورية أكاديمية
PET imaging of beta-adrenoceptors in human brain: A realistic goal or a mirage?
| العنوان: | PET imaging of beta-adrenoceptors in human brain: A realistic goal or a mirage? |
|---|---|
| المؤلفون: | van Waarde, Aaren, Vaalburg, W., Doze, Petra, Bosker, Fokko, Elsinga, P.H |
| المصدر: | van Waarde , A , Vaalburg , W , Doze , P , Bosker , F & Elsinga , P H 2004 , ' PET imaging of beta-adrenoceptors in human brain: A realistic goal or a mirage? ' , Current Pharmaceutical Design , vol. 10 , no. 13 , pp. 1519 - 1536 . |
| سنة النشر: | 2004 |
| المجموعة: | University of Groningen research database |
| مصطلحات موضوعية: | beta-adrenoceptors, positron emission tomography, human, brain, depression, multiple sclerosis, radiopharmaceuticals, imaging, POSITRON-EMISSION-TOMOGRAPHY, ADRENERGIC-RECEPTOR SUBTYPES, IN-VIVO QUANTIFICATION, CENTRAL-NERVOUS-SYSTEM, RADIOLIGAND BINDING ASSAY, DEPRESSED SUICIDE VICTIMS, PARTIAL AGONIST ACTIVITY, ALZHEIMER-TYPE DEMENTIA, REVEALS HIGH-AFFINITY, GUINEA-PIG ATRIA |
| الوصف: | Beta-adrenoceptors are predominantly located in the cerebral cortex, nucleus accumbens and striatum. At lower densities, they are also present in amygdala, hippocampus and cerebellum. Beta-2 sites regulate glial proliferation during ontogenic development, after trauma and in neurodegenerative diseases. The densities of beta-1 adrenoceptors are changed by stress, in several mood disorders (depression, excessive hostility, schizophrenia) and during treatment of patients with antidepressants. A technique for beta-adrenoceptor imaging in the human brain is not yet available. Although 24 (ant)agonists have been labeled with either 11C or 18F and some of these are successful myocardial imaging agents, only two (S-1’-18F-fluorocarazolol and S-1’-18F-fluoroethylcarazolol) could actually visualize ß-adrenoceptors within the central nervous system. Unfortunately, these radiopharmaceuticals showed a positive Ames test. They may be mutagenic and cannot be employed for human studies. Screening of more than 150 beta-blockers described in the literature yields only two compounds (exaprolol and L643,717) which can still be radiolabeled and evaluated for ß-adenoceptor imaging. However, other imaging techniques could be examined. Cerebral ß-adrenoceptors might be labeled after temporary opening of the blood-brain barrier (BBB) and simultaneous administration of a hydrophilic ligand such as S-11C-CGP12388. Another approach to target ß-adrenoceptor ligands to the CNS is esterification of a myocardial imaging agent (such as 11C-CGP12177), resulting in a lipophilic prodrug which can cross the BBB and is split by tissue esterases. BBB opening is not feasible in healthy subjects, but the prodrug approach may be successful and deserves to be explored. |
| نوع الوثيقة: | article in journal/newspaper |
| وصف الملف: | application/pdf |
| اللغة: | Dutch; Flemish |
| العلاقة: | https://research.rug.nl/en/publications/c0101078-01c8-441a-998c-bbc3e5071587Test |
| الإتاحة: | https://hdl.handle.net/11370/c0101078-01c8-441a-998c-bbc3e5071587Test https://research.rug.nl/en/publications/c0101078-01c8-441a-998c-bbc3e5071587Test https://pure.rug.nl/ws/files/16298211/Waarde2004.pdfTest |
| حقوق: | info:eu-repo/semantics/openAccess |
| رقم الانضمام: | edsbas.B93EB32F |
| قاعدة البيانات: | BASE |
| الوصف غير متاح. |