Dysregulated HPA axis during postnatal developmental stages in the BTBR T Itpr3/J mouse: A model of autism spectrum disorder.

Autism spectrum disorder (ASD) is a neurodevelopmental disorder. Some children with ASD show enhanced cortisol response to stress. BTBR T Itpr3/J (BTBR) mice, an ASD model, display behavior consistent with the three diagnostic categories of ASD and exhibit an exaggerated response to stress in adulthood.

Potential for visualization of intracellular pH gradient in the brain using PET imaging.

Intracellular pH is a valuable index for predicting neuronal damage and injury. However, no PET probe is currently available for monitoring intracellular pH . In this study, we developed a new approach for visualizing the hydrolysis rate of monoacylglycerol lipase, which is widely distributed in neurons and astrocytes throughout the brain.

Small-animal PET study for noninvasive quantification of transmembrane AMPA receptor regulatory protein -8 (TARP -8) in the brain.

Transmembrane AMPA receptor regulatory protein γ-8 (TARP γ-8) mediates various AMPA receptor functions. Recently, [C]TARP-2105 was developed as a PET ligand for TARP γ-8 imaging. We performed a full kinetic analysis of [C]TARP-2105 using PET with [C]TARP-2105 for the first time.

Imaging of Transmembrane AMPA Receptor Regulatory Proteins by Positron Emission Tomography.

The transmembrane α-amino-3-hydroxyl-5-methyl-4-isoxazolepropionic acid (AMPA) receptor regulatory protein γ-8 (TARP γ-8) constitutes an auxiliary subunit of AMPA receptors, which mediates various brain functions including learning and memory. TARP γ-8 has emerged as a promising therapeutic target for central nervous system disorders. Despite considerable efforts, previously reported TARP γ-8 PET radioligands, such as [C]TARP-1903 and [C]TARP-1811 series, were plagued by limited brain uptake and/or high nonspecific binding in vivo.

Synthesis of [C]carbonyl-labeled cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl)carbamate ([C-carbonyl]PK68) as a potential PET tracer for receptor-interacting protein 1 kinase.

Background: Receptor-interacting protein 1 kinase (RIPK1) is a key enzyme in the regulation of cellular necroptosis. Recently, cyclohexyl (5-(2-acetamidobenzo[d]thiazol-6-yl)-2-methylpyridin-3-yl)carbamate (PK68, 5) has been developed as a potent inhibitor of RIPK1. Herein, we synthesized [C]carbonyl-labeled PK68 ([C-carbonyl]PK68, [C]PK68) as a potential PET tracer for imaging RIPK1 and evaluated its brain uptake in vivo.