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HTS100M ChemiSCREEN™ Human δ Opioid Receptor Membrane Preparation

Human Delta / OP1 / DOP / DOR GPCR membrane preparation for Radioligand binding Assays & GTPγS.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.
Host Cell: Chem-1 Uni Prot Number: P41143 Entrez Gene Number: NM_000911.3
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HTS100M
200 units  
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      Overview

      Replacement Information

      Key Specifications Table

      SpeciesHost CellsProtein Target
      Human Chem-1Delta / OP1 / DOP / DOR
      Description
      Catalogue NumberHTS100M
      Brand Family Chemicon®
      Trade Name
      • ChemiScreen
      • Chemicon
      DescriptionChemiSCREEN™ Human δ Opioid Receptor Membrane Preparation
      OverviewFull-length human OPRD1 cDNA encoding δ opioid receptor
      Background InformationOpiates derived from the opium poppy, Papaver somniferum, have been used in for millenia for their anti-diarrheal, analgesic and euphoric properties. More recently, endogenous peptides, enkephalins, dynorphins, and endorphins, were found to bind to the same sites as opiate alkaloids. The receptors for the classical opioids are three related GPCRs, δ, κ, and μ (also known as OP1, OP2 and OP3, resepctively), that activate Gi/o to reduce intracellular cAMP levels. Although most clinically used opioids function by activation of the µ opioid receptor, agonits of spinal δ opioid receptors have antinociceptive activity that is independent of µ. In addition, activation of δ increases locomotor activity, inhibits gastrointestinal motility, and decreases respiratory frequency (Dhawan et al., 1996). Agonists for δ opioid receptors also exhibit antidepressant-like activity in animal models (Broom et al., 2002). Chemicon's δ 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 at δ. The membrane preparations exhibit a Kd of 1.12 nM for [3H]-DADLE. With 0.9 nM [3H]-DADLE, 10 µg/well δ Membrane Prep typically yields greater than 4-fold signal-to-background ratio.
      References
      Product Information
      FormatMembranes
      PresentationOne package contains enough membranes for at least 200 assays (units), where a unit is the amount of membrane that will yield greater than 4-fold signal:background with 3H-labeled DADLE at 0.9 nM

      Liquid in packaging buffer: 50 mM Tris pH 7.4, 10% glycerol and 1% BSA with no preservatives.
      Packaging method: Membranes protein were adjusted to 1 mg/mL in packaging buffer, and dispensed at 1 mL/vial. Vials were rapidly frozen, and stored at -80°C.
      Quality LevelMQ100
      Applications
      ApplicationHuman Delta / OP1 / DOP / DOR GPCR membrane preparation for Radioligand binding Assays & GTPγS.
      Key Applications
      • Radioligand binding assay
      • GTPγS binding
      Application NotesRadioligand binding assay and GTPγS
      Biological Information
      Entrez Gene Number
      Gene Symbol
      • OPRD1
      • OPRD
      • DOR-1
      GPCR ClassA
      Host CellsChem-1
      Protein TargetDelta / OP1 / DOP / DOR
      Target Sub-FamilyOpioid
      UniProt Number
      UniProt SummaryFUNCTION: SwissProt: P41143 # Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Highly stereoselective. receptor for enkephalins.
      SIZE: 372 amino acids; 40413 Da
      SUBUNIT: Interacts with GPRASP1.
      SUBCELLULAR LOCATION: Cell membrane; Multi-pass membrane protein.
      SIMILARITY: SwissProt: P41143 ## Belongs to the G-protein coupled receptor 1 family.
      Incubation ConditionsMembranes are mixed with radioactive ligand and unlabeled competitor (see Figures 1 and 2 for concentrations tested) in binding buffer in a nonbinding 96-well plate, and incubated for 1-2 h. Prior to filtration, an FC 96-well harvest plate (Millipore cat. # MAHF C1H) is coated with 0.33% polyethyleneimine for 30 min, then washed with 50mM Tris-HCl. Binding reaction is transferred to the filter plate, and washed 3 times (1 mL per well per wash) with Wash Buffer. The plate is dried and counted.

      Binding buffer: 50 mM Tris-HCl, filtered and stored at 4°C
      Radioligand: [3H] DADLE (Perkin Elmer#: NET-648)
      Wash Buffer: 50 mM Tris-HCl, filtered and stored at 4°C.
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Table 1. Signal:background and specific binding values obtained in a competition binding assay with δ membrane prep and unlabeled DPDPE.
      Product Usage Statements
      10 µg/well
      Signal:Background 7.32
      Specific Binding (cpm) 955


      SPECIFICATIONS: 1 unit = 10 µg
      Bmax for [3H] DADLE binding: 11.6 pmol/mg protein
      Kd for [3H] DADLE binding: ~1.12 nM Usage Statement
      • Unless otherwise stated in our catalog or other company documentation accompanying the product(s), our products are intended for research use only and are not to be used for any other purpose, which includes but is not limited to, unauthorized commercial uses, in vitro diagnostic uses, ex vivo or in vivo therapeutic uses or any type of consumption or application to humans or animals.
      Storage and Shipping Information
      Storage ConditionsStore at –70°C. Product is stable for at least 6 months from the date of receipt when stored as directed. Do not freeze and thaw.
      Packaging Information
      Material Size200 units
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalog Number GTIN
      HTS100M 04053252323379

      Documentation

      ChemiSCREEN™ Human δ Opioid Receptor Membrane Preparation SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overviewPub Med ID
      Behavioral effects of delta-opioid receptor agonists: potential antidepressants?
      Broom, Daniel C, et al
      Jpn J Pharmacol, 90:1-6 (2002)  2002

      		12396021 12396021

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