MAO-A inhibition in brain after dosing with esuprone, moclobemide and placebo in healthy volunteers: in vivo studies with positron emission tomography

European Journal of Clinical Pharmacology
M BergströmB Långström

Abstract

The aim of the study was to investigate whether or not esuprone binds substantially to MAO-A in the human brain. In a randomised double-blind placebo-controlled study 16 male healthy volunteers were examined with positron emission tomography (PET) with [11C]harmine. Eight of the volunteers were given daily doses of 800 mg esuprone, four were given bi-daily doses of 300 mg moclobemide, and four volunteers were given placebo tablets. PET was performed before initiation of a 7-day treatment period. On day 7, one investigation was made immediately before administration of the drug, representing 23 h after the previous day's treatment for esuprone and 11 h after the last tablets of moclobemide. Further investigations were made 4 h and 8 h after the morning dose on day 7. PET showed a high degree of binding of [11C]harmine, a high-affinity ligand for MAO-A, before the start of treatment, and a marked and similar reduction after treatment with esuprone and moclobemide. A slight tendency for normalisation of enzyme binding was observed at the last time point. In the placebo group no change was observed. Plasma kinetics of esuprone showed a rapid elimination with a half-life of about 4 h. The study demonstrates that esuprone was compara...Continue Reading

Citations

Mar 12, 2004·Forensic Science International : Synergy·Christian GiroudPatrice Mangin
Nov 6, 2009·Neuropsychopharmacology : Official Publication of the American College of Neuropsychopharmacology·Joanna S FowlerKaren Apelskog-Torres
Aug 2, 2007·Nuclear Medicine Communications·Rajan MurthyRamin Parsey
May 18, 2005·NeuroRx : the Journal of the American Society for Experimental NeuroTherapeutics·David J Brooks
Jun 5, 2014·Future Medicinal Chemistry·Sarah Chajkowski-Scarry, John M Rimoldi
Sep 5, 2012·Expert Review of Clinical Pharmacology·Spyros N DeftereosAris Persidis
Jun 3, 2008·Seminars in Nuclear Medicine·Jeffrey H Meyer
Feb 14, 2015·Journal of Labelled Compounds & Radiopharmaceuticals·Joanna S FowlerNora D Volkow
Jun 19, 2004·Bioorganic & Medicinal Chemistry Letters·Franco ChimentiFrancesco Ortuso
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
Dec 30, 2014·Bioorganic & Medicinal Chemistry·Hanno SchiefersteinFrank Rösch
Feb 28, 2003·The Journal of Pharmacology and Experimental Therapeutics·Michel BottlaenderHeric Valette
Feb 3, 2000·Journal of Epidemiology and Community Health·B BurströmM Whitehead
Mar 26, 2010·Clinical Pharmacology and Therapeutics·S ZamunerA C Hooker
Oct 31, 2002·Human Psychopharmacology·Alain Patat

❮ Previous
Next ❯

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.

Related Papers

Nordic Journal of Psychiatry
Kurt Bjerregaard Bjerregaard Stage, Danish University Antidepressant Group
American Journal of Medical Genetics. Part B, Neuropsychiatric Genetics : the Official Publication of the International Society of Psychiatric Genetics
Yuhui SunQi Xu
© 2021 Meta ULC. All rights reserved