A comparison of methods for the separation of [11C]Ro 15-1788 (flumazenil) from its metabolites in the blood of rabbits, baboons and humans
- PMID: 1646188
- DOI: 10.1016/0883-2889(91)90102-7
A comparison of methods for the separation of [11C]Ro 15-1788 (flumazenil) from its metabolites in the blood of rabbits, baboons and humans
Abstract
The determination of the percentage of unchanged [11C]Ro 15-1788 with respect to total radioactivity, essential for the pharmacokinetic exploitation of data of blood radioactivity decrease obtained in PET studies, may be carried out with equal results using either an extraction procedure or a TLC method. The analysis of blood samples of various sources (rabbits, baboons, healthy volunteers and anxious patients) and the use of an automatic linear scanner to quantify the radioactive distribution on the TLC plates lead to the conclusion that only [11C]Ro 15-1788 and its acid metabolite [11C]Ro 15-3890 and no other radioactive compound are present in blood at detectable concentration.
Similar articles
-
Plasma pharmacokinetics and metabolism of the benzodiazepine antagonist [11C] Ro 15-1788 (flumazenil) in baboon and human during positron emission tomography studies.Eur J Drug Metab Pharmacokinet. 1991 Apr-Jun;16(2):141-52. doi: 10.1007/BF03189951. Eur J Drug Metab Pharmacokinet. 1991. PMID: 1657612
-
Quantitative evaluation of benzodiazepine receptors in live Papio papio baboons using positron emission tomography.Mol Pharmacol. 1990 Oct;38(4):445-50. Mol Pharmacol. 1990. PMID: 2172764
-
Simple analytic method of 11C-flumazenil metabolite in blood.J Nucl Med. 2003 Mar;44(3):417-21. J Nucl Med. 2003. PMID: 12621009
-
Metabolite analysis of [11C]flumazenil in human plasma: assessment as the standardized value for quantitative PET studies.Ann Nucl Med. 1998 Feb;12(1):55-9. doi: 10.1007/BF03165418. Ann Nucl Med. 1998. PMID: 9559964
-
Synthesis of ethyl 8-fluoro-5,6-dihydro-5-[11C]methyl-6-oxo-4H-imidazo [1,5-a] [1,4]benzodiazepine-3-carboxylate (RO 15.1788-11C): a specific radioligand for the in vivo study of central benzodiazepine receptors by positron emission tomography.Int J Appl Radiat Isot. 1984 Oct;35(10):973-6. doi: 10.1016/0020-708x(84)90215-1. Int J Appl Radiat Isot. 1984. PMID: 6094361
Cited by
-
Use of a standardized uptake value for parametric in vivo imaging of benzodiazepine receptor distribution on [11C]flumazenil brain PET.Eur J Nucl Med Mol Imaging. 2004 Jun;31(6):846-51. doi: 10.1007/s00259-004-1458-4. Epub 2004 Feb 21. Eur J Nucl Med Mol Imaging. 2004. PMID: 14985864 Clinical Trial.
-
Carbon-11 and iodine-123 labelled iomazenil: a direct PET-SPET compari son.Eur J Nucl Med. 1996 Jan;23(1):5-12. doi: 10.1007/BF01736983. Eur J Nucl Med. 1996. PMID: 8586102
-
[11C]flumazenil binding is increased in a dose-dependent manner with tiagabine-induced elevations in GABA levels.PLoS One. 2012;7(2):e32443. doi: 10.1371/journal.pone.0032443. Epub 2012 Feb 27. PLoS One. 2012. PMID: 22384252 Free PMC article.
-
Tiagabine increases [11C]flumazenil binding in cortical brain regions in healthy control subjects.Neuropsychopharmacology. 2009 Feb;34(3):624-33. doi: 10.1038/npp.2008.104. Epub 2008 Jul 9. Neuropsychopharmacology. 2009. PMID: 18615011 Free PMC article.
-
Kinetic modelling of [11C]flumazenil using data-driven methods.Eur J Nucl Med Mol Imaging. 2009 Apr;36(4):659-70. doi: 10.1007/s00259-008-0990-z. Epub 2008 Nov 29. Eur J Nucl Med Mol Imaging. 2009. PMID: 19043703
Publication types
MeSH terms
Substances
LinkOut - more resources
Full Text Sources
Research Materials