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Preclinical Characterization of 18F-MK-6240, a Promising PET Tracer for In Vivo Quantification of Human Neurofibrillary Tangles
TLDR
18F-MK-6240 is a promising PET tracer for the in vivo quantification of NFTs in AD patients, indicating favorable tracer kinetics and distribution in the brain.
Discovery of 6-(Fluoro-(18)F)-3-(1H-pyrrolo[2,3-c]pyridin-1-yl)isoquinolin-5-amine ([(18)F]-MK-6240): A Positron Emission Tomography (PET) Imaging Agent for Quantification of Neurofibrillary Tangles
TLDR
6 exhibits high specificity and selectivity for binding to NFTs, with suitable physicochemical properties and in vivo pharmacokinetics.
Translational characterization of [11C]GSK931145, a PET ligand for the glycine transporter type 1
TLDR
[11C]GSK931145 entered primate and human brain and yielded a heterogeneous pattern of uptake which was similar in both species with highest uptake in midbrain, thalamus, and cerebellum.
Prediction of Repeat-Dose Occupancy from Single-Dose Data: Characterisation of the Relationship between Plasma Pharmacokinetics and Brain Target Occupancy
TLDR
This approach increases the value of SD occupancy studies that are performed as part of first time in human drug development programmes by providing an estimate of the dose required to achieve the desired TO at RD.
Identification and evaluation of [11C]GSK931145 as a novel ligand for imaging the type 1 glycine transporter with positron emission tomography
TLDR
GlyT1 PET radioligands selected from a library of compounds based on favorable physicochemical and pharmacological properties were identified as the most promising ligand for imaging GlyT1 in the porcine brain, possessing good brain penetration, specific signal, and reversible kinetics.
Brain Imaging of Alzheimer Dementia Patients and Elderly Controls with 18F-MK-6240, a PET Tracer Targeting Neurofibrillary Tangles
TLDR
This pilot study suggests that simplified ratio methods such as SUVR can be used to quantify NFT binding and support further clinical development of 18F-MK-6240 for potential application in longitudinal studies.
Phosphodiesterase 10A PET Radioligand Development Program: From Pig to Human
TLDR
The first human administration of 11C-IMA107 has demonstrated the expected regional distribution and suitably fast kinetics, indicating that 12C- IMA107 will be a useful tool for the investigation of PDE10A status in the living human brain.
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