Histamine H3 receptor antagonists/inverse agonists: Where do they go?

N Ghamari, O Zarei, JA Arias-Montaño, D Reiner… - Pharmacology & …, 2019 - Elsevier
Since the discovery of the histamine H 3 receptor in 1983, tremendous advances in the
pharmacological aspects of H 3 receptor antagonists/inverse agonists have been …

[HTML][HTML] Application of cross-species PET imaging to assess neurotransmitter release in brain

SJ Finnema, M Scheinin, M Shahid, J Lehto… - …, 2015 - Springer
Rationale This review attempts to summarize the current status in relation to the use of
positron emission tomography (PET) imaging in the assessment of synaptic concentrations …

The histamine system and cognitive function: An in vivo H3 receptor PET imaging study in healthy volunteers and patients with schizophrenia

A Arumuham, MM Nour, M Veronese… - Journal of …, 2023 - journals.sagepub.com
Background: The histamine-3 receptor (H3R) is an auto-and heteroreceptor that inhibits the
release of histamine and other neurotransmitters. Post-mortem evidence has found altered …

[HTML][HTML] Is there a role for GPCR agonist radiotracers in PET neuroimaging?

M Colom, B Vidal, L Zimmer - Frontiers in Molecular Neuroscience, 2019 - frontiersin.org
Positron emission tomography (PET) is a molecular imaging modality that enables in vivo
exploration of metabolic processes and especially the pharmacology of neuroreceptors. G …

[PDF][PDF] 11C dosimetry scans should be abandoned

P Zanotti-Fregonara, AA Lammertsma… - Journal of Nuclear …, 2021 - Soc Nuclear Med
Before a new tracer can be used in clinical research, it is customary to perform dosimetry
scans in animals and humans to assess whether the radiation exposure is acceptable. The …

Progress in the development of histamine H3 receptor antagonists/inverse agonists: a patent review (2013-2017)

D Łażewska, K Kieć-Kononowicz - Expert opinion on therapeutic …, 2018 - Taylor & Francis
Introduction: Since years, ligands blocking histamine H3 receptor (H3R) activity
(antagonists/inverse agonists) are interesting targets in the search for new cures for CNS …

[HTML][HTML] News and views on in vivo imaging of neurotransmission using PET and MRI

CY Sander, S Hesse - The quarterly journal of nuclear medicine …, 2017 - ncbi.nlm.nih.gov
Molecular neuroimaging with PET is an integrated tool in psychiatry research and drug-
development for as long as this modality has been available, in particular for studying …

[HTML][HTML] Histamine-3 receptor availability and glutamate levels in the brain: a PET-1H-MRS study of patients with schizophrenia and healthy controls

A Arumuham, MM Nour, M Veronese… - International Journal …, 2024 - academic.oup.com
Background The histamine-3 receptor (H3R) may have a role in cognitive processes,
through its action as a presynaptic heteroreceptor inhibiting the release of glutamate in the …

Pharmacokinetic and pharmacodynamic assessment of histamine H3 receptor occupancy by enerisant: a human PET study with a novel H3 binding ligand, [11C] …

Y Kimura, K Takahata, T Shimazaki, S Kitamura… - European Journal of …, 2021 - Springer
Purpose Histamine H 3 receptor antagonists and inverse agonists have been extensively
developed to treat sleep–wake, neurocognitive, and allied disorders. However, potential …

[HTML][HTML] Development of TASP0410457 (TASP457), a novel dihydroquinolinone derivative as a PET radioligand for central histamine H3 receptors

K Koga, J Maeda, M Tokunaga, M Hanyu… - EJNMMI research, 2016 - Springer
Abstract Background Histamine H 3 receptor (H 3 R) is a potential therapeutic target of sleep-
and cognition-related disorders. The purpose of the present study is to develop a novel …