Calcium Flux Assay

HTS136C - ChemiSCREEN™ Human Recombinant V1B Vasopressin Receptor Calcium-Optimized Stable Cell Line

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HTS136C
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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 (Birnbaumer, 2000). The V1B receptor is expressed prominently in the anterior pituitary, where it mediates vasopressin-induced release of ACTH (Tanoue et al., 2004). A selective antagonist of V1B has recently been developed and shown to reduce depression, anxiety, and aggression in rodents (Blanchard et al, 2005; Griebel et al., 2002). The cloned human V1B-expressing cell line is made in the Chem-1 host, which supports high levels of recombinant V1B expression on the cell surface and contains high levels of the promiscuous G protein Gα15 to couple the receptor to the calcium signaling pathway. Thus, the cell line is an ideal tool for screening for antagonists of interactions between V1B and its ligands.

    Additional Resource :  HTS136C060515 Datasheet

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    Contents: 2 vials of mycoplasma-free cells, 1 mL per vial.
    Storage: Vials are to be stored in liquid N2.
    Applications: Calcium Flux Assay
    Host Cell: Chem-1, an adherent cell line expressing the promiscuous G-protein, Gα15.
    Exongenous Gene Expression: Human V1B cDNA (Accession Number: NM_000707- see CODING SEQUENCE below) and promiscuous G protein are expressed in a bicistronic vector
    GMO: This product contains genetically modified organisms.
    Reference 1: 1. Birnbaumer M (2000) Vasopressin receptors. Trends Endocrinol. Metab. 11:406-10.
    Reference 2: 2. Blanchard RJ et al. (2005) AVP V1b selective antagonist SSR149415 blocks aggressive behaviors in hamsters. Pharmacol. Biochem. Behav. 80: 189-194.
    Reference 3: 3. Griebel G et al. (2002) Anxiolytic- and antidepressant-like effects of the non-peptide vasopressin V1b receptor antagonist, SSR149415, suggest an innovative approach for the treatment of stress-related disorders. Proc. Natl. Acad. Sci. USA 99: 6
    Reference 4: 4. Tanoue A et al. (2004) The vasopressin V1b receptor critically regulates hypothalamic-pituitary-adrenal axis activity under both stress and resting conditions. J. Clin. Invest. 113: 302-309.
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