2’-[18F]Fluoroflumazenil
- PMID: 20641363
- Bookshelf ID: NBK23160
2’-[18F]Fluoroflumazenil
Excerpt
Benzodiazepines are used for their sedative, anxiolytic, and muscle-relaxant properties. Their mechanism of action involves the binding of a ligand to a specific benzodiazepine receptor. Alteration of the central benzodiazepine receptor (CBR) has been reported in various diseases and pathologic conditions such as Alzheimer’s disease, epilepsy, or cerebral ischemia (1-4).
CBRs have been studied in vivo by positron emission tomography (PET) and single photon emission computed tomography, and the existence of a specific benzodiazepine receptor linked to the γ-aminobutyric acid (GABA) receptor/chloride ionophore has been shown by use of diazepam (4).
[11C]Flumazenil, a highly selective benzodiazepine antagonist, has been the most widely used agent for PET imaging of CBRs, but the short half-life of 11C (20 min) limits its use. To overcome this great disadvantage, the flumazenil analog [18F]fluoroethyl 8-fluoro-5-methyl-6-oxo-5,6-dihydro-4H-benzo-[f]imidazo[1,5-a][1,4]diazepine-3-carboxylate ([18F]fluoroflumazenil; [18F]FFMZ) has been developed and is currently under study. It can be conveniently synthesized and labeled, and preliminary research shows some favorable specific binding properties for CBRs.
Sections
Similar articles
-
Biological properties of 2'-[18F]fluoroflumazenil for central benzodiazepine receptor imaging.Nucl Med Biol. 2005 Apr;32(3):263-8. doi: 10.1016/j.nucmedbio.2004.12.004. Nucl Med Biol. 2005. PMID: 15820761
-
Biological evaluation of 2'-[18F]fluoroflumazenil ([18F]FFMZ), a potential GABA receptor ligand for PET.Nucl Med Biol. 2004 Feb;31(2):291-5. doi: 10.1016/j.nucmedbio.2003.09.003. Nucl Med Biol. 2004. PMID: 15013496
-
N-Benzyl-N-methyl-2-[7,8-dihydro-7-(2-[18F]fluoroethyl)-8-oxo-2-phenyl-9H-purin-9-yl]acetamide.2010 May 6 [updated 2010 Aug 19]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2010 May 6 [updated 2010 Aug 19]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 20734501 Free Books & Documents. Review.
-
N-Benzyl-N-ethyl-2-[7,8-dihydro-7-(2-[18F]fluoroethyl)-8-oxo-2-phenyl-9H-purin-9-yl]acetamide.2010 May 6 [updated 2010 Aug 19]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2010 May 6 [updated 2010 Aug 19]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 20734500 Free Books & Documents. Review.
-
N-Acetyl-N-(2-[18F]fluoroethoxybenzyl)-2-phenoxy-5-pyridinamine.2008 Aug 12 [updated 2008 Aug 22]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. 2008 Aug 12 [updated 2008 Aug 22]. In: Molecular Imaging and Contrast Agent Database (MICAD) [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2004–2013. PMID: 20641889 Free Books & Documents. Review.
References
-
- Marczynski TJ . GABAergic deafferentation hypothesis of brain aging and Alzheimer's disease; pharmacologic profile of the benzodiazepine antagonist, flumazenil. Rev Neurosci. 1995;6(3):221–258. - PubMed
-
- Thomas RJ . Seizures and epilepsy in the elderly. Arch Intern Med. 1997;157(6):605–617. - PubMed
-
- Nutt DJ , Malizia AL . New insights into the role of the GABA(A)-benzodiazepine receptor in psychiatric disorder. Br J Psychiatry. 2001;179:390–396. - PubMed
-
- Mohler H , Okada T . Benzodiazepine receptor: demonstration in the central nervous system. Science. 1977;198(4319):849–851. - PubMed
-
- Yoon YH , Jeong JM , Kim HW , Hong SH , Lee YS , Kil HS , Chi DY , Lee DS , Chung JK , Lee MC . Novel one-pot one-step synthesis of 2'-[(18)F]fluoroflumazenil (FFMZ) for benzodiazepine receptor imaging. Nucl Med Biol. 2003;30(5):521–527. - PubMed
Publication types
LinkOut - more resources
Full Text Sources
Miscellaneous
