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Molecular Pharmacology

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Rapid CommunicationAccelerated Communication

Cloning, Expression, and Pharmacological Characterization of a Novel Human Histamine Receptor

Yuan Zhu, David Michalovich, Hsiao-Ling Wu, K. B. Tan, George M. Dytko, Ishrat J. Mannan, Rogely Boyce, James Alston, Lauren A Tierney, Xiaotong Li, Nicole C. Herrity, Lisa Vawter, Henry M. Sarau, Robert S. Ames, Colleen M. Davenport, J. Paul Hieble, Shelagh Wilson, Derk J. Bergsma and Laura R. Fitzgerald
Molecular Pharmacology March 2001, 59 (3) 434-441; DOI: https://doi.org/10.1124/mol.59.3.434
Yuan Zhu
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David Michalovich
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Hsiao-Ling Wu
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K. B. Tan
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George M. Dytko
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Ishrat J. Mannan
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Rogely Boyce
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Xiaotong Li
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Nicole C. Herrity
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Lisa Vawter
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Henry M. Sarau
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Robert S. Ames
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Colleen M. Davenport
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J. Paul Hieble
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Shelagh Wilson
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Derk J. Bergsma
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Laura R. Fitzgerald
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Abstract

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)-α-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.

Footnotes

    • Received November 29, 2000.
    • Accepted January 5, 2001.
  • Send reprint requests to: Dr. Yuan Zhu, Department of Molecular Biology, SmithKline Beecham Pharmaceuticals, 709 Swedeland Road, PO Box 1539, King of Prussia, PA 19406. E-mail:yuan_zhu-1{at}sbphrd.com

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Molecular Pharmacology: 59 (3)
Molecular Pharmacology
Vol. 59, Issue 3
1 Mar 2001
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Rapid CommunicationAccelerated Communication

Cloning, Expression, and Pharmacological Characterization of a Novel Human Histamine Receptor

Yuan Zhu, David Michalovich, Hsiao-Ling Wu, K. B. Tan, George M. Dytko, Ishrat J. Mannan, Rogely Boyce, James Alston, Lauren A Tierney, Xiaotong Li, Nicole C. Herrity, Lisa Vawter, Henry M. Sarau, Robert S. Ames, Colleen M. Davenport, J. Paul Hieble, Shelagh Wilson, Derk J. Bergsma and Laura R. Fitzgerald
Molecular Pharmacology March 1, 2001, 59 (3) 434-441; DOI: https://doi.org/10.1124/mol.59.3.434

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Rapid CommunicationAccelerated Communication

Cloning, Expression, and Pharmacological Characterization of a Novel Human Histamine Receptor

Yuan Zhu, David Michalovich, Hsiao-Ling Wu, K. B. Tan, George M. Dytko, Ishrat J. Mannan, Rogely Boyce, James Alston, Lauren A Tierney, Xiaotong Li, Nicole C. Herrity, Lisa Vawter, Henry M. Sarau, Robert S. Ames, Colleen M. Davenport, J. Paul Hieble, Shelagh Wilson, Derk J. Bergsma and Laura R. Fitzgerald
Molecular Pharmacology March 1, 2001, 59 (3) 434-441; DOI: https://doi.org/10.1124/mol.59.3.434
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