Abstract
Radio-labeled somatostatin analogs have recently gained popularity as agents useful in intraoperative tumor localization, external scintigraphy and in situ radiotherapy. We have synthesized and characterized a series of novel N-terminally extended multiply-tyrosinated somatostatin analogs that possess high binding affinity for somatostatin receptors, exhibit biological activity comparable to the native peptide and retain these characteristics after iodination. These analogs can be radio-iodinated to high specific activities. Following radioiodination, these analogs exhibit minimal radiolysis and may be clinically useful for tumor localization, scanning and therapy.
MeSH terms
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Adenocarcinoma, Bronchiolo-Alveolar / diagnosis
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Adenocarcinoma, Bronchiolo-Alveolar / pathology
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Adenylyl Cyclase Inhibitors
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Aged
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Amino Acid Sequence
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Brain Neoplasms / diagnosis
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Brain Neoplasms / secondary
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Diagnostic Imaging
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Growth Hormone / antagonists & inhibitors
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Humans
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Iodine / chemistry
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Lung Neoplasms / diagnosis
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Lung Neoplasms / pathology
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Male
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Neuroblastoma / drug therapy
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Neuroblastoma / metabolism
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Peptides / metabolism*
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Peptides / pharmacokinetics
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Radionuclide Imaging / methods
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Somatostatin / analogs & derivatives*
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Somatostatin / chemical synthesis
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Somatostatin / pharmacology*
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Tissue Distribution
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Tumor Cells, Cultured
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Tyrosine / chemistry
Substances
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Adenylyl Cyclase Inhibitors
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Peptides
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Tyrosine
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Somatostatin
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Growth Hormone
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Iodine