Novel GAT-1 Radiotracer Screening Data for PET Imaging

A 2026 figshare dataset by Jiwei Gu documents the synthesis and evaluation of 105 tiagabine-based compounds as potential brain-penetrant radioligands for GABA Transporter 1 (GAT-1). It details the screening process that identified four lead candidates (GATT-31, GATT-34, GATT-39, GATT-44) based on affinity, lipophilicity, and efflux liability. The data supports the first reported in vivo PET imaging of GAT-1 in nonhuman primates.

Use Cases

• Modeling the relationship between compound structure and GAT-1 affinity using screening data for 105 derivatives.
• Analyzing the correlation between lipophilicity and brain uptake for the four lead radioligands (GATT-31, GATT-34, GATT-39, GATT-44).
• Comparing the metabolic stability and binding specificity of [18F]GATT-44 against other candidates from in vivo primate PET data.
• Training models to predict P-glycoprotein efflux liability from chemical features of tiagabine-based compounds.

Strengths

• Data originates from a published scientific study reporting the first successful in vivo imaging of GAT-1.
• Screening results are provided for a defined library of 105 synthesized compounds.
• Evaluation includes in vitro affinity, lipophilicity, efflux liability, and in vivo PET imaging in nonhuman primates.

Limitations

• The dataset is very small at 1.9 KB, indicating limited raw data or summary statistics rather than full experimental records.
• Specific sample sizes, column names, and raw measurement values for each compound are not provided in the description.
• Geographic and species coverage is limited to nonhuman primate studies at a single research institution.

Provenance

Source

figshare, authored by Jiwei Gu.

Collection Method

Experimental data from the design, synthesis, in vitro screening, and in vivo PET evaluation of novel radioligands.

Time Range

The study period is not specified, but the dataset was published in 2026.

Freshness

Last updated in April 2026.