HTS060M - ChemiScreen™ V2 Vasopressin Receptor Membrane Preparation

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    Arginine vasopressin (AVP) is a 9 amino acid peptide that functions as an antidiuretic, vasoconstrictor and neurotransmitter. The three vasopressin receptors, V1a, V1b and V2, are GPCRs; V1a and V1b couple to Gq and calcium release, whereas V2 couples to Gs. V2 expressed in renal collecting ducts plays an important role in regulating renal free water excretion (Birnbaumer, 2000). Mutations in V2 result in X-linked nephrogenic diabetes insipidus, a syndrome in which the kidney is unable to concentrate urine, leading to dehydration and hypernatremia (Birnbaumer, 2001). Conversely, elevated levels of AVP lead to hyponatremia in the syndrome of inappropriate antidiuretic hormone secretion (SIADH), congestive heart failure or cirrhosis, and V2 selective antagonists have been developed to treat these conditions (Verbalis, 2002). V2 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 antagonists of V2 interactions and its ligands. The membrane preparations exhibit a Kd of 2.83 nM for [3H]-[Arg8] Vasopression. With 3.5 nM [3H]-[Arg8] Vasopression, 10 mg/well V2 Membrane Prep yields greater than 8-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.
    Applications: Radioligand Binding Assay, GTPγS Binding
    Host Cell: Chem-1, an adherent mammalian cell line with no endogenous V2 expression.
    Reference 1: 1. Birnbaumer M (2000) Vasopressin receptors. Trends Endocrinol. Metab. 11:406-10.
    Reference 2: 2. Birnbaumer M (2001) The V2 vasopressin receptor mutations and fluid homeostasis. Cardiovasc. Res. 51: 409-415.
    Reference 3: 3. Verbalis JG (2002) Vasopressin V2 receptor antagonists. J. Mol. Endocrinol. 29: 1-9.