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Vol. 59, Issue 3, 434-441, March 2001
Departments of Molecular Biology (Y.Z., K.B.T., X.L., R.S.A.,
D.J.B.) Bioinformatics (D.M., L.V.), Renal Pharmacology (H.-L.W.,
G.M.D., I.J.M., J.P.H., L.R.F.), Clinical Cellular Biochemical
Pathology (R.B., J.A., L.A.T.), Gene Expression Science (N.C.H.),
Pulmonary Pharmacology (H.M.S.), and Immunology (C.M.D.), SmithKline
Beecham Pharmaceuticals, King of Prussia, Pennsylvania; and Department
of Vascular Biology (S.W.), SmithKline Beecham Pharmaceuticals, New
Frontiers Science Park, Harlow, Essex, England
Using a genomics-based reverse pharmacological approach for screening
orphan G-protein coupled receptors, we have identified and cloned a
novel high-affinity histamine receptor. This receptor, termed AXOR35,
is most closely related to the H3 histamine receptor, sharing 37%
protein sequence identity. A multiple responsive element/cyclic AMP-responsive element-luciferase reporter assay was used to identify histamine as a ligand for AXOR35. When transfected into human embryonic
kidney 293 cells, the AXOR35 receptor showed a strong, dose-dependent
calcium mobilization response to histamine and H3 receptor agonists
including imetit and immepip. Radioligand binding confirmed that the
AXOR35 receptor was a high-affinity histamine receptor. The
pharmacology of the AXOR35 receptor was found to closely resemble that
of the H3 receptor; the major difference was that
(R)-
-methylhistamine was a low potency agonist of the AXOR35 receptor. Thioperamide is an antagonist at AXOR 35. Expression of AXOR35 mRNA in human tissues is highest in peripheral blood mononuclear cells and in tissues likely to contain high concentrations of blood cells, such as bone marrow and lung. In situ hybridization analysis of a wide survey of mouse tissues showed that mouse AXOR35 mRNA is selectively expressed in hippocampus. The identification and
localization of this new histamine receptor will expand our understanding of the physiological and pathological roles of histamine and may provide additional opportunities for pharmacological
modification of these actions.
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