In vivo quantification of monoamine oxidase A in baboon brain: a PET study using [(11)C]befloxatone and the multi-injection approach.

Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism
M BottlaenderMarie-Claude Grégoire

Abstract

[(11)C]befloxatone is a high-affinity, reversible, and selective radioligand for the in vivo visualization of the monoamine oxidase A (MAO-A) binding sites using positron emission tomography (PET). The multi-injection approach was used to study in baboons the interactions between the MAO-A binding sites and [(11)C]befloxatone. The model included four compartments and seven parameters. The arterial plasma concentration, corrected for metabolites, was used as input function. The experimental protocol-three injections of labeled and/or unlabeled befloxatone-allowed the evaluation of all the model parameters from a single PET experiment. In particular, the brain regional concentrations of the MAO-A binding sites (B'(max)) and the apparent in vivo befloxatone affinity (K(d)) were estimated in vivo for the first time. A high binding site density was found in almost all the brain structures (170+/-39 and 194+/-26 pmol/mL in the frontal cortex and striata, respectively, n=5). The cerebellum presented the lowest binding site density (66+/-13 pmol/mL). Apparent affinity was found to be similar in all structures (K(d)V(R)=6.4+/-1.5 nmol/L). This study is the first PET-based estimation of the B(max) of an enzyme.

References

Jul 1, 1991·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·A A LammertsmaR S Frackowiak
Mar 15, 1989·Biochemical Pharmacology·A M O'CarrollK F Tipton
Oct 1, 1986·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·S C HuangM E Phelps
Apr 1, 1983·Naunyn-Schmiedeberg's Archives of Pharmacology·A M O'CarrollK F Tipton
Apr 1, 1996·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·M G Livingston, H M Livingston
Apr 1, 1996·Nuclear Medicine and Biology·S M AmetameyP A Schubiger
Mar 1, 1997·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·J DelforgeA Syrota
May 1, 1997·Nuclear Medicine and Biology·M BergströmB Långström
Apr 15, 1999·Annual Review of Neuroscience·J C ShihM J Ridd
May 20, 1999·Journal of Affective Disorders·P RosenzweigE Legangneux
May 3, 2001·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·J DelforgeA Syrota
Dec 12, 2001·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·J DelforgeA Syrota
Nov 20, 2002·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Jean LoganDavid Alexoff
Feb 28, 2003·The Journal of Pharmacology and Experimental Therapeutics·Michel BottlaenderHeric Valette
Aug 5, 2005·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Nathalie GinovartAlan A Wilson
Nov 3, 2005·Molecular Imaging and Biology : MIB : the Official Publication of the Academy of Molecular Imaging·Joanna S FowlerGene-Jack Wang
Jan 6, 2006·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Anne-Sophie VillégierJean-Pol Tassin
Jul 25, 2006·Neurotoxicology·A LewisR A Lea
Aug 4, 2006·Life Sciences·Jan van AmsterdamAntoon Opperhuizen
Jan 19, 2007·The European Journal of Neuroscience·Karine GuillemLuis Stinus
May 24, 2007·Journal of Cerebral Blood Flow and Metabolism : Official Journal of the International Society of Cerebral Blood Flow and Metabolism·Jean-Dominique GallezotMarie-Claude Grégoire
Jan 15, 2009·Journal of Clinical Psychopharmacology·Claire LeroyChristian Trichard
Feb 6, 2009·The Journal of Neuroscience : the Official Journal of the Society for Neuroscience·Ludovic LericheDeniz Kirik
May 7, 2009·Lab on a Chip·Hendrik KortmannAndreas Schmid

❮ Previous
Next ❯

Citations

Nov 10, 2012·EJNMMI Research·Stefanie DedeurwaerdereMarie-Claude Grégoire
Jul 31, 2014·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Julia SacherJeffrey H Meyer
Jun 26, 2010·European Journal of Nuclear Medicine and Molecular Imaging·Sandra M Sanabria-Bohórquez, Koen Van Laere
Jun 5, 2014·Future Medicinal Chemistry·Sarah Chajkowski-Scarry, John M Rimoldi
Sep 1, 2015·The International Journal of Neuropsychopharmacology·Lina ChiuccarielloJeffrey H Meyer
Jun 18, 2015·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Nathan J KollaJeffrey H Meyer
Nov 29, 2013·Journal of Labelled Compounds & Radiopharmaceuticals·Ken KersemansFilip De Vos
Feb 16, 2011·Journal of Nuclear Medicine : Official Publication, Society of Nuclear Medicine·Nicolas TournierMichel Bottlaender

❮ Previous
Next ❯

Software Mentioned

Winflow
JMBS

Related Concepts

Trending Feeds

COVID-19

Coronaviruses encompass a large family of viruses that cause the common cold as well as more serious diseases, such as the ongoing outbreak of coronavirus disease 2019 (COVID-19; formally known as 2019-nCoV). Coronaviruses can spread from animals to humans; symptoms include fever, cough, shortness of breath, and breathing difficulties; in more severe cases, infection can lead to death. This feed covers recent research on COVID-19.

Blastomycosis

Blastomycosis fungal infections spread through inhaling Blastomyces dermatitidis spores. Discover the latest research on blastomycosis fungal infections here.

Nuclear Pore Complex in ALS/FTD

Alterations in nucleocytoplasmic transport, controlled by the nuclear pore complex, may be involved in the pathomechanism underlying multiple neurodegenerative diseases including Amyotrophic Lateral Sclerosis and Frontotemporal Dementia. Here is the latest research on the nuclear pore complex in ALS and FTD.

Applications of Molecular Barcoding

The concept of molecular barcoding is that each original DNA or RNA molecule is attached to a unique sequence barcode. Sequence reads having different barcodes represent different original molecules, while sequence reads having the same barcode are results of PCR duplication from one original molecule. Discover the latest research on molecular barcoding here.

Chronic Fatigue Syndrome

Chronic fatigue syndrome is a disease characterized by unexplained disabling fatigue; the pathology of which is incompletely understood. Discover the latest research on chronic fatigue syndrome here.

Evolution of Pluripotency

Pluripotency refers to the ability of a cell to develop into three primary germ cell layers of the embryo. This feed focuses on the mechanisms that underlie the evolution of pluripotency. Here is the latest research.

Position Effect Variegation

Position Effect Variagation occurs when a gene is inactivated due to its positioning near heterochromatic regions within a chromosome. Discover the latest research on Position Effect Variagation here.

STING Receptor Agonists

Stimulator of IFN genes (STING) are a group of transmembrane proteins that are involved in the induction of type I interferon that is important in the innate immune response. The stimulation of STING has been an active area of research in the treatment of cancer and infectious diseases. Here is the latest research on STING receptor agonists.

Microbicide

Microbicides are products that can be applied to vaginal or rectal mucosal surfaces with the goal of preventing, or at least significantly reducing, the transmission of sexually transmitted infections. Here is the latest research on microbicides.