ArticleSynapse (New York, N.Y.)2013
Evaluation of serotonin 5-HT(1A) receptors in rodent models using [¹⁸F]mefway PET.
Article in Synapse (New York, N.Y.), 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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16 citing papers in PubMed, 24 citations in OpenAlex.
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- Assessment of brain beta-amyloid deposition in transgenic mouse models of Alzheimer's disease with PET imaging agentsBMC neuroscience · 2018Article
- Effects of hypothyroidism on serotonin 1A receptors in the rat brain.Psychopharmacology · 2018Article
- Comparative assessment of (18) F-Mefway as a serotonin 5-HT1A receptor PET imaging agent across species: Rodents, nonhuman primates, and humans.The Journal of comparative neurology · 2016Article
- Synthesis and evaluation of (S)-[(18)F]fesetron in the rat brain as a potential PET imaging agent for serotonin 5-HT3 receptors.Bioorganic & medicinal chemistry letters · 2016Article
- P-Glycoprotein, not BCRP, Limits the Brain Uptake of [(18)F]Mefway in Rodent Brain.Molecular imaging and biology · 2016Article
- Molecular Targets of Cannabidiol in Neurological Disorders.Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics · 2015Review
- Synthesis and Evaluation of Mefway Analogs as Ligands for Serotonin 5HTMedicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2015Article
- 18F-Mefway PET imaging of serotonin 1A receptors in humans: a comparison with 18F-FCWAY.PloS one · 2015Article
- First-in-human evaluation of 18F-mefway, a PET radioligand specific to serotonin-1A receptors.Journal of nuclear medicine : official publication, Society of Nuclear Medicine · 2014Article
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8 authors at 1 institution in 1 country.
Funding
Abstract
introductionSerotonin 5-HT(1A) receptors have been investigated in various CNS disorders, including epilepsy, mood disorders, and neurodegeneration. [¹⁸F]Mefway (N-{2-[4-(2'-methoxyphenyl)piperazinyl]ethyl}-N-(2-pyridyl)-N-(cis/trans-4'-[¹⁸F]fluoromethylcyclohexane)-carboxamide) has been developed as a suitable positron emission tomography (PET) imaging agent for these receptors. We have now evaluated the suitability of [¹⁸F]trans-mefway in rat and mouse models using PET and computerized tomography (CT) imaging and corroborated with ex vivo and in vitro autoradiographic studies.
methodsNormal Sprague-Dawley rats and Balb/C mice were used for PET/CT imaging using intravenously injected [¹⁸F]trans-mefway. Brain PET data were coregistered with rat and mouse magnetic resonance imaging template and regional distribution of radioactivity was quantitated. Selected animals were used for ex vivo autoradiographic studies to confirm regional brain distribution and quantitative measures of binding, using brain region to cerebellum ratios. Binding affinity of trans-mefway and WAY-100635 was measured in rat brain homogenates. Distribution of [¹⁸F]trans-4-fluoromethylcyclohexane carboxylate ([¹⁸F]FMCHA), a major metabolite of [¹⁸F] trans-mefway, was assessed in the rat by PET/CT.
resultsThe inhibition constant, K(i) for trans-mefway was 0.84 nM and that for WAY-100635 was 1.07 nM. Rapid brain uptake of [¹⁸F]trans-mefway was observed in all rat brain regions and clearance from cerebellum was fast and was used as a reference region in all studies. Distribution of [¹⁸F]trans-mefway in various brain regions was consistent in PET and in vitro studies. The dorsal raphe was visualized and quantified in the rat PET but identification in the mouse was difficult. The rank order of binding to the various brain regions was hippocampus > frontal cortex > anterior cingulate cortex > lateral septal nuclei > dorsal raphe nuclei.
conclusion[¹⁸F]trans-Mefway appears to be an effective 5-HT(1A) receptor imaging agent in rodents for studies of various disease models.
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