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Description

The histamine H2 receptor is a widely distributed G-protein coupled receptor, which is important in regulating a host of physiologic actions extending from gastric acid secretion to gastrointestinal motility (Del Valle and Gantz, 1997). Histamine mediated activation of its receptor leads to signaling through both adenylate cyclase and phosphoinositide /protein kinase C second messenger systems (Hill, 1990). Antagonists for this receptor have proven to be effective therapy for acid peptic disorders of the GI tract. Certain antagonists are used in the treatment of neuropsychiatric and neurological diseases e.g. schizophrenia, Alzheimer&prime,s disease and Parkinson&prime,s disease. Chemicon&prime,s H2 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 H2. The membrane preparations exhibit a Kd of 0.8 nM for [125I]-Iodoaminopotentidine. With 0.65 nM [125I]-Iodoaminopotentidine, 10 microg/well H2 Membrane Prep typically yields greater than 7-fold signal-to-background ratio., Full-length human HRH2 cDNA encoding H2