Indium In-111 Pentetreotide is an indium 111 radioconjugate of pentetreotide, the diethylenetriaminopentaacetic (DTPA) conjugate of the human hormone somatostatin peptide analogue (octreotide), used for radioimaging neuroendocrine tumor cells. The pentetreotide moiety of indium In 111 pentetreotide binds to somatostatin receptors (SSTRs), especially type 2 receptors, present on the cell membranes of many types of neuroendocrine tumor cells. Upon binding and internalization, this radioconjugate allows for specific imaging of neuroendocrine tumors that overexpress somatostatin using scintigraphic imaging techniques. In addition, high dose indium In 111 pentetreotide may specifically deliver a cytotoxic dose of gamma radiation to SSTR-positive cells thereby killing SSTR-expressing tumor cells.
CAT No: 10-101-336
CAS No:139096-04-1
Chemical Name:2-[2-[[2-[1-[[10-(4-aminobutyl)-16-benzyl-4-(1,3-dihydroxybutan-2-ylcarbamoyl)-7-(1-hydroxyethyl)-13-(1H-indol-3-ylmethyl)-9-oxido-6,12,15,18-tetraoxo-1,2-dithia-5,8,11,14,17-pentazacycloicos-8-en-19-yl]amino]-1-oxo-3-phenylpropan-2-yl]imino-2-oxidoethyl]-(carboxylatomethyl)amino]ethyl-(3,3-dicarboxypropyl)amino]acetate;indium-111(3+)
Indium In-111 pentetreotide is a radiolabeled peptide compound comprised of the somatostatin analog octreotide conjugated to the chelating agent DTPA and complexed with the radioisotope indium-111. This unique molecular construct is engineered to bind with high affinity to somatostatin receptor subtypes, particularly type 2, which are frequently overexpressed in various neuroendocrine and related tumor cells. Its structure enables targeted receptor-mediated localization, making it an invaluable tool in receptor expression studies and radiopharmaceutical research. The compound's ability to deliver a gamma-emitting radionuclide to specific cellular targets underpins its significance in molecular imaging and radiolabeling applications within the biochemical and life science research sectors.
Receptor binding studies: Indium In-111 pentetreotide serves as a robust probe for investigating the distribution, density, and functional status of somatostatin receptors in cell lines and tissue samples. By exploiting the high specificity of octreotide for somatostatin receptor subtypes, researchers can quantify receptor expression levels, analyze receptor-ligand interactions, and map receptor-positive cells with high precision. This capability is essential for elucidating receptor-mediated signaling pathways and for validating new somatostatin analogs or antagonists in preclinical studies.
Radioligand binding assays: The gamma-emitting properties of the indium-111 isotope within this conjugate enable its use in sensitive radioligand binding assays. It facilitates the quantitative evaluation of receptor occupancy, binding kinetics, and competitive inhibition by unlabeled ligands, supporting the characterization of novel compounds targeting the somatostatin receptor family. These assays are fundamental for drug discovery efforts focused on neuroendocrine signaling and for optimizing ligand-receptor interaction parameters.
Molecular imaging research: Indium-labeled octreotide derivatives are widely employed in the development and validation of imaging protocols for somatostatin receptor-positive cells and tissues. The radiotracer's emission properties make it suitable for gamma camera and SPECT imaging in animal models, allowing for the non-invasive visualization of receptor expression dynamics, tumor localization, and tracer biodistribution. Such approaches are vital for advancing preclinical imaging technologies and for correlating molecular target expression with physiological or pathological states.
Internalization and trafficking studies: The ability of indium In-111 pentetreotide to undergo receptor-mediated internalization provides a platform for studying endocytosis, intracellular trafficking, and receptor recycling in somatostatin receptor-expressing systems. By tracking the radiolabeled peptide's cellular journey, researchers can dissect the mechanisms governing ligand uptake, intracellular fate, and receptor turnover, yielding insights into receptor biology and the design of more effective targeting agents.
Radiopharmaceutical development: As a model compound, indium In-111 pentetreotide is frequently used in the optimization and validation of new radiopharmaceuticals targeting peptide receptors. Its well-characterized pharmacokinetics and receptor affinity make it an important reference standard for evaluating alternative chelators, radionuclides, or peptide analogs in early-stage development. Through comparative studies, it supports the refinement of labeling chemistries, stability assessments, and the establishment of critical parameters for future radiolabeled peptide agents intended for research applications.
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