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Beschreibung

Human AVPR1 cDNA encoding V1A, 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. V1 receptors regulate fluid homeostasis by stimulating contraction of glomerular mesangial cells and renal vascular smooth muscle cells (Birnbaumer, 2000). Chemicon&prime,s V1A 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 V1A interactions with its ligands. The membrane preparations exhibit a Kd of 55 pM for [125I]-vasopressin antagonist ([125I]-phenylacetyl-D-Tyr(Me)-Phe-Gln-Asn-Arg -Pro-Arg-Tyr-NH2). With 10 &mu,g/well V1A Membrane Prep and 0.1 nM [125]-vasopressin V1A antagonist, greater than 12-fold signal-to-background ratio were obtained.