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PubMed Publications| Keyword search (4,163 papers available) |  |
"Benkelfat C" Authored Publications:
| Title | Authors | PubMed ID | |
|---|---|---|---|
| 1 | Radiosynthesis and In Vivo Evaluation of Four Positron Emission Tomography Tracer Candidates for Imaging of Melatonin Receptors | Bdair H; Singleton TA; Ross K; Jolly D; Kang MS; Aliaga A; Tuznik M; Kaur T; Yous S; Soucy JP; Massarweh G; Scott PJH; Koeppe R; Spadoni G; Bedini A; Rudko DA; Gobbi G; Benkelfat C; Rosa-Neto P; Brooks AF; Kostikov A; | 35420022 PERFORM |
| 2 | Metabotropic glutamate type 5 receptor binding availability during dextroamphetamine sensitization in mice and humans. | Smart K, Nagano-Saito A, Milella MS, Sakae DY, Favier M, Vigneault E, Louie L, Hamilton A, Ferguson SSG, Rosa-Neto P, Narayanan S, El Mestikawy S, Leyton M, Benkelfat C | 32559027 CSBN |
| 3 | mGlu5 receptor availability in youth at risk for addictions: effects of vulnerability traits and cannabis use. | Cox SML, Tippler M, Jaworska N, Smart K, Castellanos-Ryan N, Durand F, Allard D, Benkelfat C, Parent S, Dagher A, Vitaro F, Boivin M, Pihl RO, Côté S, Tremblay RE, Séguin JR, Leyton M | 32413893 CSBN |
| 4 | Extra-striatal D2/3 receptor availability in youth at risk for addiction. | Jaworska N, Cox SML, Tippler M, Castellanos-Ryan N, Benkelfat C, Parent S, Dagher A, Vitaro F, Boivin M, Pihl RO, Côté SM, Tremblay RE, Séguin JR, Leyton M | 32259831 CSBN |
| 5 | Cocaine cue-induced dopamine release in the human prefrontal cortex. | Milella MS, Fotros A, Gravel P, Casey KF, Larcher K, Verhaeghe JA, Cox SM, Reader AJ, Dagher A, Benkelfat C, Leyton M | 26900792 CSBN |
| 6 | Dopamine and light: effects on facial emotion recognition. | Cawley E, Tippler M, Coupland NJ, Benkelfat C, Boivin DB, Aan Het Rot M, Leyton M | 28633582 CSBN |
| 7 | Dopamine cross-sensitization between psychostimulant drugs and stress in healthy male volunteers. | Booij L, Welfeld K, Leyton M, Dagher A, Boileau I, Sibon I, Baker GB, Diksic M, Soucy JP, Pruessner JC, Cawley-Fiset E, Casey KF, Benkelfat C | 26905412 PSYCHOLOGY |
| 8 | Effect of (Z)-isomer content on [11C]ABP688 binding potential in humans. | Smart K, Cox SML, Kostikov A, Shalai A, Scala SG, Tippler M, Jaworska N, Boivin M, Séguin JR, Benkelfat C, Leyton M | 30607444 CSBN |
| 9 | Sex differences in [11C]ABP688 binding: a positron emission tomography study of mGlu5 receptors. | Smart K, Cox SML, Scala SG, Tippler M, Jaworska N, Boivin M, Séguin JR, Benkelfat C, Leyton M | 30627817 CSBN |
| 10 | Posterior dopamine D2/3 receptors and brain network functional connectivity. | Nagano-Saito A, Lissemore JI, Gravel P, Leyton M, Carbonell F, Benkelfat C | 28700819 PERFORM |
| Title: | Radiosynthesis and In Vivo Evaluation of Four Positron Emission Tomography Tracer Candidates for Imaging of Melatonin Receptors | ||||
| Authors: | Bdair H, Singleton TA, Ross K, Jolly D, Kang MS, Aliaga A, Tuznik M, Kaur T, Yous S, Soucy JP, Massarweh G, Scott PJH, Koeppe R, Spadoni G, Bedini A, Rudko DA, Gobbi G, Benkelfat C, Rosa-Neto P, Brooks AF, Kostikov A | ||||
| Link: | https://pubmed.ncbi.nlm.nih.gov/35420022/ | ||||
| DOI: | 10.1021/acschemneuro.1c00678 | ||||
| Publication: | ACS chemical neuroscience | ||||
| Keywords: | PET; [11C]UCM1014; [11C]UCM765; [18F]3FAGM; [18F]FAAGM; agomelatine; carbon-11; fluorine-18; melatonin; melatonin receptors; positron emission tomography; | ||||
| PMID: | 35420022 | Category: | Date Added: | 2022-04-14 | |
| Dept Affiliation: |
PERFORM
1 McGill University, McConnell Brain Imaging Centre, Department of Neurology and Neurosurgery, Montreal Neurological Institute, Montreal, Quebec H3A 2B4, Canada. 2 McGill University, Department of Psychiatry, Irving Ludmer Psychiatry Research and Training Building, Montreal, Quebec H3A 1A1, Canada. 3 Translational Neuroimaging Laboratory, McGill University Research Centre for Studies in Aging, Alzheimer's Disease Research Unit, Douglas Research Institute, Le Centre intégré universitaire de santé et de services sociaux (CIUSSS) de l'Ouest-de-l'Île-de-Montréal, Montreal, Quebec H4H 1R3, Canada. 4 University of Michigan Medical School, Department of Radiology, Ann Arbor, Michigan 48109-5610, United States. 5 University of Lille, Lille Neurosciences and Cognition Research Center, Lille, Hauts-de-France FR 59000, France. 6 Concordia University, PERFORM Centre, Montreal, Québec H4B 1R6, Canada. 7 University Carlo Bo, Department Biomolecular Science, Urbino IT 61029, Italy. 8 Department of Biomedical Engineering, McGill University, Montreal, Quebec H3A 2B4, Canada. 9 McGill University, Department of Chemistry, Montreal, Quebec H3A 0B8, Canada. |
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Description: |
Melatonin is a neurohormone that modulates several physiological functions in mammals through the activation of melatonin receptor type 1 and 2 (MT1 and MT2). The melatonergic system is an emerging therapeutic target for new pharmacological interventions in the treatment of sleep and mood disorders; thus, imaging tools to further investigate its role in the brain are highly sought-after. We aimed to develop selective radiotracers for in vivo imaging of both MT1 and MT2 by positron emission tomography (PET). We identified four previously reported MT ligands with picomolar affinities to the target based on different scaffolds which were also amenable for radiolabeling with either carbon-11 or fluorine-18. [11C]UCM765, [11C]UCM1014, [18F]3-fluoroagomelatine ([18F]3FAGM), and [18F]fluoroacetamidoagomelatine ([18F]FAAGM) have been synthesized in high radiochemical purity and evaluated in wild-type rats. All four tracers showed moderate to high brain permeability in rats with maximum standardized uptake values (SUVmax of 2.53, 1.75, 3.25, and 4.47, respectively) achieved 1-2 min after tracer administration, followed by a rapid washout from the brain. Several melatonin ligands failed to block the binding of any of the PET tracer candidates, while in some cases, homologous blocking surprisingly resulted in increased brain retention. Two 18F-labeled agomelatine derivatives were brought forward to PET scans in non-human primates and autoradiography on human brain tissues. No specific binding has been detected in blocking studies. To further investigate pharmacokinetic properties of the putative tracers, microsomal stability, plasma protein binding, log D, and membrane bidirectional permeability assays have been conducted. Based on the results, we conclude that the fast first pass metabolism by the enzymes in liver microsomes is the likely reason of the failure of our PET tracer candidates. Nevertheless, we showed that PET imaging can serve as a valuable tool to investigate the brain permeability of new therapeutic compounds targeting the melatonergic system. |
