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INHIBITION OF AMYLIN RELEASE WITH SOMATOSTATIN TYPE-5 RECEPTOR (SSTR-5), DETERMINATION OF AMYLIN RELEASE INHIBITION
INHIBITION OF AMYLIN RELEASE WITH SOMATOSTATIN TYPE-5 RECEPTOR (SSTR-5), DETERMINATION OF AMYLIN RELEASE INHIBITION
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机译:生长抑素5型受体(SSTR-5)抑制胰岛淀粉样多肽释放,测定胰岛淀粉样多肽释放抑制剂
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摘要
A method of determining the ability of a compound to both bind to somatostatin type-5 receptor ("SSTR-5") and inhibit amylin release. The method includes obtaining a preparation, either a cell preparation or a membrane preparation, which contains SSTR-5; incubating the preparation, the compound, and a SSTR-5 ligand, at least one of the ligand and the compound being detectably labeled; determining the ability of the compound to compete against the ligand for binding to SSTR-5; if and only if the compound is determined to be able to bind to SSTR-5, obtaining pancreatic cells; incubating the compound, the pancreatic cells, and an amylin release stimulator under conditions in which the amylin release stimulator would induce release of amylin from the pancreatic cells; and determining the ability of the compound to inhibit amylin release. Also disclosed is a method of treating hyper-amylinemia with a ligand selective for SSTR-5.
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