Literature DB >> 6094361

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.

M Maziere, P Hantraye, C Prenant, J Sastre, D Comar.   

Abstract

A method of labelling 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 benzodiazepine antagonist with carbon-11 has been developed. RO 15.1788-11C was prepared by methylation of the nor derivative by I11CH3. About 100 mCi (maximum 153 mCi, 5.66 GBq) of the chemically and radiochemically pure labelled product were obtained within 25 min with a specific activity on average of 1100 mCi/mumol (maximum 1740 mCi/mu mol--64.4 GBq/mu mol). Preliminary results obtained after i.v. administration in the baboon have shown RO 15.1788-11C to be of interest as a benzodiazepine radioligand for the in vivo study of benzodiazepine receptors by positron emission tomography.

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Year:  1984        PMID: 6094361     DOI: 10.1016/0020-708x(84)90215-1

Source DB:  PubMed          Journal:  Int J Appl Radiat Isot        ISSN: 0020-708X


  22 in total

1.  [11C]Ro 15-4513, a ligand for visualization of benzodiazepine receptor binding. Preparation, autoradiography and positron emission tomography.

Authors:  C Halldin; L Farde; J E Litton; H Hall; G Sedvall
Journal:  Psychopharmacology (Berl)       Date:  1992       Impact factor: 4.530

Review 2.  Applications of positron emission tomography (PET) in neurology.

Authors:  Y F Tai; P Piccini
Journal:  J Neurol Neurosurg Psychiatry       Date:  2004-05       Impact factor: 10.154

Review 3.  Uses and limitations of positron emission tomography in clinical pharmacokinetics/dynamics (Part II).

Authors:  L L Ponto; J A Ponto
Journal:  Clin Pharmacokinet       Date:  1992-04       Impact factor: 6.447

4.  Population pharmacokinetic analysis for simultaneous determination of B (max) and K (D) in vivo by positron emission tomography.

Authors:  Lia C Liefaard; Bart A Ploeger; Carla F M Molthoff; Ronald Boellaard; Adriaan A Lammertsma; Meindert Danhof; Rob A Voskuyl
Journal:  Mol Imaging Biol       Date:  2005 Nov-Dec       Impact factor: 3.488

Review 5.  Development of (18)F-labeled radiotracers for neuroreceptor imaging with positron emission tomography.

Authors:  Peter Brust; Jörg van den Hoff; Jörg Steinbach
Journal:  Neurosci Bull       Date:  2014-08-29       Impact factor: 5.203

6.  Three-dimensional visualization and quantification of the benzodiazepine receptor population within a living human brain using PET and MRI.

Authors:  S Pauli; G Sedvall
Journal:  Eur Arch Psychiatry Clin Neurosci       Date:  1997       Impact factor: 5.270

7.  PET imaging of ischemia-induced impairment of mitochondrial complex I function in monkey brain.

Authors:  Hideo Tsukada; Hiroyuki Ohba; Shingo Nishiyama; Masakatsu Kanazawa; Takeharu Kakiuchi; Norihiro Harada
Journal:  J Cereb Blood Flow Metab       Date:  2014-01-22       Impact factor: 6.200

Review 8.  Where have we got to with neuroreceptor mapping of the human brain?

Authors:  B Mazière; M Mazière
Journal:  Eur J Nucl Med       Date:  1990

9.  Kinetic modelling of [11C]flumazenil using data-driven methods.

Authors:  Isabelle Miederer; Sibylle I Ziegler; Christoph Liedtke; Mary E Spilker; Matthias Miederer; Till Sprenger; Klaus J Wagner; Alexander Drzezga; Henning Boecker
Journal:  Eur J Nucl Med Mol Imaging       Date:  2008-11-29       Impact factor: 9.236

10.  Plasma pharmacokinetics and metabolism of the benzodiazepine antagonist [11C] Ro 15-1788 (flumazenil) in baboon and human during positron emission tomography studies.

Authors:  D Debruyne; P Abadie; L Barre; F Albessard; M Moulin; E Zarifian; J C Baron
Journal:  Eur J Drug Metab Pharmacokinet       Date:  1991 Apr-Jun       Impact factor: 2.441

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