5-HT2A receptor SPECT imaging with [ 123 I]R91150 under P-gp inhibition with tariquidar: More is better?

Tsartsalis, Stergios; Tournier, Benjamin B.; Huynh-Gatz, Trinh; Dumas, Noé; Ginovart, Nathalie; Moulin-Sallanon, Marcelle; Millet, Philippe

doi:10.1016/j.nucmedbio.2015.09.003

Cited by 6 publications

(3 citation statements)

References 45 publications

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“…Metabolite correction and plasma protein binding analysis for the estimation of radiotracer plasma input function was performed in an independent group of four rats, as previously described (Gandelman et al, 1994;Millet et al, 2008;Millet et al, 2012;Mintun et al, 1984;Tsartsalis et al, 2014;Tsartsalis et al, 2015). A detailed description can be found in Supplementary Materials and Methods paragraph S1.1.…”

Section: Spect Single-and Multi-injection Imaging and Quantificationmentioning

confidence: 99%

“…This difference in non-displaceable binding between striatum and cerebellum and within the striatal subregions does not impede the use of these simplified methods, provided that it is stable across different subjects of a given population and independent of the experimental conditions of a biological study. (Lyoo et al, 2015;Tsartsalis et al, 2016b). BP ND values obtained with the SRTM, LNIGA and SUR present a reasonable variability and may thus be employed as an index of D 2/3 receptor expression in preclinical biological studies.…”

Section: Impact Of Non-specific Binding On Bp Ndmentioning

confidence: 99%

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A single-scan protocol for absolute D2/3 receptor quantification with [123I]IBZM SPECT

et al. 2017

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A partial saturation protocol permits the non-invasive and time-efficient estimation of B and appK separately. Given the different biological phenomena that underlie these parameters, this method may be applied for the in-depth study of the dopaminergic system in translational molecular imaging studies. It can detect the biological variations in these parameters, dissociating the variations in receptor density (B) from affinity (1/appK), which reflects the interactions of the receptor with its endogenous ligand.

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Section: Spect Single-and Multi-injection Imaging and Quantificationmentioning

confidence: 99%

Section: Impact Of Non-specific Binding On Bp Ndmentioning

confidence: 99%

A single-scan protocol for absolute D2/3 receptor quantification with [123I]IBZM SPECT

et al. 2017

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“…In a more-recent study, R91150 was labeled with 18 F and evaluated as a potential PET radioligand in mice . However, it was later found to be a p -gp substrate because it exhibited a 3-fold increase in its brain uptake upon tariquidar treatment, as demonstrated by SPECT imaging …”

Section: -Ht2a Receptor Radioligandsmentioning

confidence: 99%

New Trends and Current Status of Positron-Emission Tomography and Single-Photon-Emission Computerized Tomography Radioligands for Neuronal Serotonin Receptors and Serotonin Transporter

et al. 2017

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The critical role of serotonin (5-hydroxytryptamine; 5-HT) and its receptors (5-HTRs) in the pathophysiology of diverse neuropsychiatric and neurodegenerative disorders render them attractive diagnostic and therapeutic targets for brain disorders. Therefore, the in vivo assessment of binding of 5-HT receptor ligands under a multitude of physiologic and pathologic scenarios may support more-accurate identification of disease and its progression and the patient's response to therapy as well as the screening of novel therapeutic strategies. The present Review aims to focus on the current status of radioligands used for positron-emission tomography (PET) and single-photon-emission computerized tomography (SPECT) imaging of human brain serotonin receptors. We further elaborate upon and emphasize the attributes that qualify a radioligand for theranostics on the basis of its frequency of use in clinics, its benefit to risk assessment in humans, and its continuous evolution, along with the major limitations.

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Dual-radiotracer translational SPECT neuroimaging. Comparison of three methods for the simultaneous brain imaging of D2/3 and 5-HT2A receptors

et al. 2018

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5-HT2A receptor SPECT imaging with [ 123 I]R91150 under P-gp inhibition with tariquidar: More is better?

Cited by 6 publications

References 45 publications

A single-scan protocol for absolute D2/3 receptor quantification with [123I]IBZM SPECT

A single-scan protocol for absolute D2/3 receptor quantification with [123I]IBZM SPECT

New Trends and Current Status of Positron-Emission Tomography and Single-Photon-Emission Computerized Tomography Radioligands for Neuronal Serotonin Receptors and Serotonin Transporter

Dual-radiotracer translational SPECT neuroimaging. Comparison of three methods for the simultaneous brain imaging of D2/3 and 5-HT2A receptors

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