Gallium-68 DOTATATE (or Ga-68 DOTATATE) is a PET radiotracer that is useful for evaluating primary and metastatic well-differentiated neuroendocrine tumors. It is a form of somatostatin-receptor (SSTR) functional imaging and most often combined with cross-sectional imaging in the form of PET-CT.
CAT No: 10-101-338
CAS No:1027785-90-5
Synonyms/Alias:Dotatate gallium Ga-68; Gallium 68 dotatate; 68Ga-DOTATATE; (68Ga)Gallium dotatate
Chemical Name:gallium;2-[4-[2-[[(2R)-1-[[(4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-4-[[(1S,2R)-1-carboxy-2-hydroxypropyl]carbamoyl]-7-[(1R)-1-hydroxyethyl]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-19-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethyl]-7,10-bis(carboxylatomethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetate
Ga-68 DOTA-TATE is a radiolabeled somatostatin analog, widely recognized for its unique ability to bind with high affinity to somatostatin receptor subtype 2 (SSTR2). This compound is synthesized by chelating gallium-68, a positron-emitting radioisotope, to the DOTA-TATE peptide, enabling targeted molecular imaging. The exceptional stability of the DOTA chelator, combined with the specificity of the TATE sequence, allows for precise localization of SSTR2-expressing cells. Its rapid pharmacokinetic profile and favorable biodistribution further enhance its utility in research settings, making it a preferred choice for studies involving receptor-targeted imaging and tracer development.
Molecular Imaging Research: Ga-68 DOTA-TATE serves as a cornerstone in the field of molecular imaging, facilitating the visualization and quantification of somatostatin receptor expression in various biological models. By leveraging the high specificity of the TATE peptide for SSTR2, researchers can non-invasively monitor receptor distribution and density in vivo using positron emission tomography (PET). This capability supports the investigation of receptor dynamics under physiological and experimental conditions, enabling the study of disease progression, receptor modulation, and the effects of pharmacological interventions on SSTR2 expression.
Neuroendocrine Tumor Models: In preclinical studies, Ga-68 DOTA-TATE is extensively utilized for the in vivo imaging of neuroendocrine tumor (NET) models. The radiotracer's affinity for SSTR2, commonly overexpressed in NETs, allows scientists to track tumor growth, metastasis, and response to experimental therapies in animal models. This application is invaluable for evaluating the efficacy of novel therapeutics targeting somatostatin receptors and for optimizing imaging protocols that may later be translated into broader research use.
Pharmacokinetic and Biodistribution Studies: Researchers employ Ga-68 DOTA-TATE to conduct detailed pharmacokinetic and biodistribution studies in animal models. The radiolabeled compound's rapid clearance and organ-specific uptake profiles provide insights into its in vivo behavior, informing the design and optimization of new somatostatin analogs and imaging agents. Such studies are critical for understanding tracer kinetics, minimizing off-target effects, and improving the specificity and sensitivity of receptor-targeted imaging approaches.
Radiotracer Development and Validation: The properties of Ga-68 DOTA-TATE make it an ideal reference standard for the development and validation of new radiotracers targeting somatostatin receptors. By comparing novel compounds to this well-characterized agent, researchers can benchmark affinity, stability, and imaging performance. This process accelerates the identification of promising candidates for further preclinical investigation, ensuring that only the most effective tracers proceed to advanced stages of research.
Receptor Occupancy and Drug Interaction Studies: Ga-68 DOTA-TATE is instrumental in receptor occupancy studies, where it is used to quantify the binding of experimental drugs to SSTR2 in vivo. By measuring changes in tracer uptake before and after administration of candidate compounds, scientists can assess receptor engagement, competitive binding, and pharmacodynamic effects. These studies provide critical data for dose optimization and for elucidating the mechanisms underlying drug-receptor interactions in complex biological systems.
Peptide-based Imaging Agent Research: The ongoing exploration of peptide-based imaging agents benefits significantly from the use of Ga-68 DOTA-TATE as a model compound. Its robust performance in targeting SSTR2 serves as a benchmark for the design of new peptides with improved pharmacological properties or alternative targeting profiles. Comparative studies using this agent inform the rational modification of peptide sequences, chelator chemistry, and radiolabeling techniques, ultimately contributing to the advancement of next-generation molecular imaging probes for diverse research needs.
2. TMEM16F and dynamins control expansive plasma membrane reservoirs
5. The spatiotemporal control of signalling and trafficking of the GLP-1R
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