HTS057M - ChemiScreen™ PRP/GPR10 Prolactin-Releasing Peptide Receptor Membrane Preparation

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    PRP, also known as GPR10 or hGR3, is a Gq-coupled receptor for prolactin-releasing peptide that is expressed in the pituitary (Hinuma et al., 1998). Genetic studies in rodents indicate that lack of GPR10 leads to hyperphagia, obesity and dyslipidemia (Gu et al., 2004; Watanabe et al., 2005). In humans, genetic variations in GPR10 are associated with lowered blood pressure (Bhattacharyya et al., 2003). GPR10/PRP 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 GPR10/PRP interactions with prolactin-releasing peptide. The membrane preparations exhibit a Kd of 0.59-0.66 nM for [125I]-PRP-20. With 5 mg/well PRP Membrane Prep and 0.25 nM [125I]-PRP-20, a greater than 30-fold signal-to-background ratio was obtained.

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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, GTPγS Binding
    Species: Human Full-length human GPR10 cDNA encoding PRP (Accession Number: NM_004248)
    Host Cell: Chem-1, an adherent mammalian cell line without any endogenous GPR10 expression.
    Reference 1: 1. Bhattacharyya S et al. (2003) Association of polymorphisms in GPR10, the gene encoding the prolactin-releasing peptide receptor with blood pressure, but not obesity, in a U.K. Caucasian population. Diabetes 52: 1296-9.
    Reference 2: 2. Gu W et al. (2004) The prolactin-releasing peptide receptor (GPR10) regulates body weight homeostasis in mice. J. Mol. Neurosci. 22: 93-103.
    Reference 3: 3. Hinuma S et al. (1998) A prolactin-releasing peptide in the brain. Nature 393: 272-6.
    Reference 4: 4. Watanabe TK et al. (2005) Mutated G-protein-coupled receptor GPR10 is responsible for the hyperphagia/dyslipidaemia/obesity locus of Dmo1 in the OLETF rat. Clin. Exp. Pharmacol. Physiol. 32: 355-66.