HTS028M - ChemiSCREEN™ sst2 Somatostatin Receptor Membrane Preparation

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    Somatostatin (sst) is a multifunctional peptide with two biologically active forms, sst-14 and sst-28, which are synthesized in neurons throughout the brain as well as in peripheral tissues such as the pancreas and the gut (Gillies, 1997). SST exerts a diverse array of effects that include inhibition of endocrine secretion, modulation of neurotransmission, and regulation of cell proliferation by stimulating a family of five G-protein-coupled receptors. Somatostatin receptor sst2 mRNA is predominantly expressed in central nervous system. Study using sst2 knock-out mice has found the increased anxiety-related behaviour while locomotor and exploratory activity was decreased in stress-inducing situations (coupled with an increase in pituitary ACTH release, a regulator of the stress response) (Viollet et al., 2000) . In the periphery, inhibition of glucagon release by sst in mouse islets is primarily mediated via sst2 (Strowski et al., 2000). In addition, endogenous sst functions through sst2 to suppress gastric acid secretion through inhibition of gastrin activity (Martinez et al., 1998). sst2 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression; thus, they are ideal HTS tools for screening of agonists and antagonists of sst2. The membrane preparations exhibit a Kd of 0.95 nM for [125I]-Somatostatin 14. With 0.75 nM [125I]-Somatostatin 14, 5 mg/well sst2 Membrane Prep typically yields greater than 14-fold signal-to-background ratio.

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    Item Unit of Measure: EA
    Quantity: 200 units
    Storage: On receipt of material store at -70°C. Unopened reagent is stable for a minimum of 1 year from date of shipment when stored at recommended storage temperature. Avoid repeat freeze/thaw cycles. For maximum recovery of product, centrifuge original vial
    Applications: Radioligand Binding Assay
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous sst2 expression.
    Reference 1: 1. Gillies G (1997) Somatostatin: the neuroendocrine story. Trends Pharmacol. Sci. 18: 87-95.
    Reference 2: 2. Martinez V et al. (1998) High basal gastric acid secretion in somatostatin receptor subtype 2 knockout mice. Gastroenterology 114: 1125 - 1132.
    Reference 3: 3. Strowski MZ et al. (2000) Somatostatin inhibits insulin and glucagon secretion via two receptors subtypes: an in vitro study of pancreatic islets from somatostatin receptor 2 knockout mice. Endocrinology 141: 111 - 117.
    Reference 4: 4. Viollet C et al. (2000) Involvement of sst2 somatostatin receptor in locomotor, exploratory activity and emotional reactivity in mice Eur. J. Neurosci. 12: 3761 – 3770.