4.7 Article

[18F]F13640: a selective agonist PET radiopharmaceutical for imaging functional 5-HT1A receptors in humans

Related references

Note: Only part of the references are listed.
Review Pharmacology & Pharmacy

Translating biased agonists from molecules to medications: Serotonin 5-HT1A receptor functional selectivity for CNS disorders

Adrian Newman-Tancredi et al.

Summary: Biased agonism at G-protein-coupled receptors has gained increasing interest for the discovery of more effective and safer drugs. However, most studies are limited to in vitro tests, and few biased agonists have been tested in vivo. The study of biased agonism at 5-HT1A receptors has been limited by the availability of ligands with poor target selectivity or partial agonism. However, the development of new selective and efficacious agonists has advanced the study of biased agonism at this receptor and opened up new therapeutic opportunities.

PHARMACOLOGY & THERAPEUTICS (2022)

Article Clinical Neurology

Brain5-HT1AReceptor Binding in Multiple System Atrophy: An [18F]-MPPF PETStudy

Marie Meyer et al.

Summary: This study compared brain 5-hydroxytryptamine(1A) receptor binding between multiple system atrophy (MSA) patients, Parkinson's disease (PD) patients, and healthy controls. The findings showed dysfunction in several brain regions in MSA patients, which may contribute to symptoms like fatigue, pain, and apathy.

MOVEMENT DISORDERS (2021)

Review Psychiatry

Towards in vivo imaging of functionally active 5-HT1A receptors in schizophrenia: concepts and challenges

Oriane Razakarivony et al.

Summary: The PET neuroimaging study targeting the 5-HT1A receptor can specifically visualize and quantify functionally active receptors using a specific radioligand [F-18]-F13640, helping researchers to track receptor changes and correlate them with disease states. This approach has the potential to improve differentiation of different schizophrenia phenotypes and deepen understanding of the basis of therapeutic responses.

TRANSLATIONAL PSYCHIATRY (2021)

Article Neurosciences

Validation of kinetic modeling of [15O]H2O PET using an image derived input function on hybrid PET/MRI

Mark B. Vestergaard et al.

Summary: The study aimed to validate the use of IDIF in the kinetic modeling of CBF by comparing with the reference standard AIF and phase-contrast mapping MRI. Results showed that global CBF values modeled using IDIF correlated with values from AIF, indicating similar perfusion deficits in patient group.

NEUROIMAGE (2021)

Article Neurosciences

[18F]F13640, a 5-HT1A Receptor Radiopharmaceutical Sensitive to Brain Serotonin Fluctuations

Matthieu Colom et al.

Summary: The study evaluated the sensitivity of the radiopharmaceutical [F-18]F13640 to endogenous serotonin release, demonstrating its effectiveness in measuring neurotransmitter fluctuations but highlighting the importance of longer PET scans for accurate displacement measurements.

FRONTIERS IN NEUROSCIENCE (2021)

Article Clinical Neurology

The selective 5-HT1A receptor agonist, NLX-112, exerts anti-dyskinetic effects in MPTP-treated macaques

R. Depoortere et al.

PARKINSONISM & RELATED DISORDERS (2020)

Article Anatomy & Morphology

18F-F13640 preclinical evaluation in rodent, cat and primate as a 5-HT1A receptor agonist for PET neuroimaging

Benjamin Vidal et al.

BRAIN STRUCTURE & FUNCTION (2018)

Article Radiology, Nuclear Medicine & Medical Imaging

Development of a Dedicated Rebinner with Rigid Motion Correction for the mMR PET/MR Scanner, and Validation in a Large Cohort of 11C-PIB Scans

Anthonin Reilhac et al.

JOURNAL OF NUCLEAR MEDICINE (2018)

Article Neurosciences

Macroanatomy and 3D probabilistic atlas of the human insula

Isabelle Faillenot et al.

NEUROIMAGE (2017)

Article Engineering, Biomedical

Multi-atlas attenuation correction supports full quantification of static and dynamic brain PET data in PET-MR

Ines Merida et al.

PHYSICS IN MEDICINE AND BIOLOGY (2017)

Article Radiology, Nuclear Medicine & Medical Imaging

11C-CUMI-101, a PET Radioligand, Behaves as a Serotonin 1A Receptor Antagonist and Also Binds to α1 Adrenoceptors in Brain

Stal Saurav Shrestha et al.

JOURNAL OF NUCLEAR MEDICINE (2014)

Article Multidisciplinary Sciences

Switching brain serotonin with oxytocin

Raphaelle Mottolese et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2014)

Article Biochemistry & Molecular Biology

PET Radiotracers for Molecular Imaging of Serotonin 5-HT1A Receptors

T. Billard et al.

CURRENT MEDICINAL CHEMISTRY (2013)

Article Biochemistry & Molecular Biology

Measuring endogenous changes in serotonergic neurotransmission in humans: a [11C]CUMI-101 PET challenge study

S. Selvaraj et al.

MOLECULAR PSYCHIATRY (2012)

Article Radiology, Nuclear Medicine & Medical Imaging

In vitro assessment of the agonist properties of the novel 5-HT1A receptor ligand, CUMI-101 (MMP), in rat brain tissue

Nicola Hendry et al.

NUCLEAR MEDICINE AND BIOLOGY (2011)

Review Cell Biology

5-HT1A receptor-regulated signal transduction pathways in brain

Abigail M. Polter et al.

CELLULAR SIGNALLING (2010)

Article Radiology, Nuclear Medicine & Medical Imaging

Modeling considerations for 11C-CUMI-101, an agonist radiotracer for imaging serotonin 1A receptor in vivo with PET

Matthew S. Milak et al.

JOURNAL OF NUCLEAR MEDICINE (2008)

Article Neurosciences

Automatic segmentation of brain MRIs of 2-year-olds into 83 regions of interest

Ioannis S. Gousias et al.

NEUROIMAGE (2008)

Review Pharmacology & Pharmacy

Functional selectivity through protean and biased agonism: Who steers the ship?

Terry Kenakin

MOLECULAR PHARMACOLOGY (2007)

Article Multidisciplinary Sciences

Serotonin 1A receptors in the living brain of Alzheimer's disease patients

V Kepe et al.

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA (2006)

Article Endocrinology & Metabolism

Regional heterogeneity of 5-HT1A receptors in human cerebellum as assessed by positron emission tomography

RV Parsey et al.

JOURNAL OF CEREBRAL BLOOD FLOW AND METABOLISM (2005)

Review Pharmacology & Pharmacy

Multiple signaling states of G-protein-coupled receptors

DM Perez et al.

PHARMACOLOGICAL REVIEWS (2005)

Article Radiology, Nuclear Medicine & Medical Imaging

Graphical analysis of PET data applied to reversible and irreversible tracers

J Logan

NUCLEAR MEDICINE AND BIOLOGY (2000)

Article Radiology, Nuclear Medicine & Medical Imaging

Quantitative imaging of 5-HT1A receptor binding in healthy volunteers with [18F]p-MPPF

J Passchier et al.

NUCLEAR MEDICINE AND BIOLOGY (2000)