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ChemiScreen™ BB1 Bombesin/Neuromedin B Receptor Membrane Preparation

Bombesin, a bioactive peptide first identified in amphibian skin, is related to two mammalian peptides, gastrin-releasing peptide (GRP) and neuromedin B (NMB). A family of 3 GPCRs, including NMB-R (BB1), GRP-R (BB2) and BRS-3 (BB3), mediate the biological effects of the peptides. The receptors differ in their affinities for the peptides; BB2 binds to GRP with 50-300-fold greater affinity than to NMB, whereas BB1 binds to NMB with 10-800-fold greater affinity than to GRP (Tokita et al., 2004). Binding of ligand to BB1 activates Gq to increase intracellular calcium concentrations. The CNS is a major site of NMB and BB1 expression, and BB1 appears to be involved in thermoregulation (Ohki-Hamazaki et al., 2005). BB1 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 BB1 interactions with neuromedin B. The membrane preparations exhibit a Kd of 0.35-0.43 nM for [125I]-Bombesin. With 5 mg/well BB1 Membrane Prep and 0.3 nM [125I]-bombesin, a greater than 40-fold signal-to-background ratio was obtained.

Catalog No. Size Price Quantity
HTS123M 1 Vial $646.90

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Application
Radioligand Binding Assay
Family
Bombesin
Target
BB1
Accession Number
NM_002511
Species
Human
Host Cell Type
Chem-1
Content
1 Vial (1 mL) for two 96-well plates or 200 units
Storage
Vial to be stored 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.