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Octreotide, sold under the brand name Sandostatin among others, is an octapeptide that mimics natural somatostatin pharmacologically, though it is a more potent inhibitor of growth hormone, glucagon, and insulin than the natural hormone. It was first synthesized in 1979 and binds predominantly to the somatostatin receptors SSTR2 and SSTR5. [5]
The natural somatostatin receptor ligand, the 14 amino acid peptide somatostatin (A), was abridged to the biologically more stable 8 amino acid peptide Octreotide (OC, B). Introduction of a tyrosine into the 3rd position of the Octreotide sequence resulted in Tyr3-Octreotide (TOC, C), which allows for iodination of the tyrosine residue with the ...
An octreotide scan is a type of SPECT scintigraphy used to find carcinoid, pancreatic neuroendocrine tumors, and to localize sarcoidosis. It is also called somatostatin receptor scintigraphy (SRS). Octreotide , a drug similar to somatostatin , is radiolabeled with indium-111 , [ 1 ] and is injected into a vein and travels through the bloodstream.
Octreotide is used for suppression of the hormonal syndromes which accompany several pancreatic islet cell tumors, including the Zollinger-Ellison syndrome of gastrinoma and the chronic hypoglycemia of insulinoma. It is also effective in suppression of the carcinoid syndrome, caused by advanced or extra-gastrointestinal carcinoid tumors.
The nomenclature of the somatostatin receptor antagonists is also based on this order. The structure of somatostatin receptor antagonists are similar to that of the agonists. Some agonists were already approved by the FDA for clinical use, such as In-DTPA-octreotide and Ga-DOTATATE. [4]
It is a non-selective somatostatin receptor antagonist, [37] inhibiting the effects of somatostatin on target cells in the gastrointestinal tract, pancreas, hypothalamus, and central nervous system. [2] Cyclosomatostatin is used as a research chemical to investigate the effects of somatostatin on different cell types by antagonizing its ...
The US Food and Drug Administration (FDA) approved 177 Lu dotatate based primarily on evidence from one clinical trial, NETTER-1 of 229 participants with somatostatin-receptor positive midgut GEP-NETs. [15] Enrolled participants had tumors which could not be surgically removed and were worsening while receiving treatment with octreotide. [15]
Octreotide is a synthetic modification of somatostatin with a longer half-life. [ citation needed ] OctreoScan, also called somatostatin receptor scintigraphy (SRS or SSRS), utilizes intravenously administered octreotide that is chemically bound to a radioactive substance, often indium -111, to detect larger lesions with tumor cells that are ...