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Molecular Pharmacology

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Rapid CommunicationAccelerated CommunicationA

Cloning and Functional Expression of the Human Histamine H3 Receptor

Timothy W. Lovenberg, Barbara L. Roland, Sandy J. Wilson, Xiaoxia Jiang, Jayashree Pyati, Arne Huvar, Michael R. Jackson and Mark G. Erlander
Molecular Pharmacology June 1999, 55 (6) 1101-1107; DOI: https://doi.org/10.1124/mol.55.6.1101
Timothy W. Lovenberg
R.W. Johnson Pharmaceutical Research Institute, San Diego, California
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Barbara L. Roland
R.W. Johnson Pharmaceutical Research Institute, San Diego, California
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Sandy J. Wilson
R.W. Johnson Pharmaceutical Research Institute, San Diego, California
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Xiaoxia Jiang
R.W. Johnson Pharmaceutical Research Institute, San Diego, California
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Jayashree Pyati
R.W. Johnson Pharmaceutical Research Institute, San Diego, California
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Arne Huvar
R.W. Johnson Pharmaceutical Research Institute, San Diego, California
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Michael R. Jackson
R.W. Johnson Pharmaceutical Research Institute, San Diego, California
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Mark G. Erlander
R.W. Johnson Pharmaceutical Research Institute, San Diego, California
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Abstract

Histamine regulates neurotransmitter release in the central and peripheral nervous systems through H3 presynaptic receptors. The existence of the histamine H3 receptor was demonstrated pharmacologically 15 years ago, yet despite intensive efforts, its molecular identity has remained elusive. As part of a directed effort to discover novel G protein-coupled receptors through homology searching of expressed sequence tag databases, we identified a partial clone (GPCR97) that had significant homology to biogenic amine receptors. The GPCR97 clone was used to probe a human thalamus library, which resulted in the isolation of a full-length clone encoding a putative G protein-coupled receptor. Homology analysis showed the highest similarity to M2 muscarinic acetylcholine receptors and overall low homology to all other biogenic amine receptors. Transfection of GPCR97 into a variety of cell lines conferred an ability to inhibit forskolin-stimulated cAMP formation in response to histamine, but not to acetylcholine or any other biogenic amine. Subsequent analysis revealed a pharmacological profile practically indistinguishable from that for the histamine H3 receptor. In situ hybridization in rat brain revealed high levels of mRNA in all neuronal systems (such as the cerebral cortex, the thalamus, and the caudate nucleus) previously associated with H3 receptor function. Its widespread and abundant neuronal expression in the brain highlights the significance of histamine as a general neurotransmitter modulator. The availability of the human H3 receptor cDNA should greatly aid in the development of chemical and biological reagents, allowing a greater appreciation of the role of histamine in brain function.

Footnotes

    • Received February 12, 1999.
    • Accepted April 2, 1999.
  • Send reprint requests to: Dr. Timothy W. Lovenberg, R.W. Johnson Pharmaceutical Research Institute, 3535 General Atomics Ct., San Diego, CA. E-mail:tlovenbe{at}prius.jnj.com

  • The American Society for Pharmacology and Experimental Therapeutics
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Molecular Pharmacology: 55 (6)
Molecular Pharmacology
Vol. 55, Issue 6
1 Jun 1999
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Rapid CommunicationAccelerated CommunicationA

Cloning and Functional Expression of the Human Histamine H3 Receptor

Timothy W. Lovenberg, Barbara L. Roland, Sandy J. Wilson, Xiaoxia Jiang, Jayashree Pyati, Arne Huvar, Michael R. Jackson and Mark G. Erlander
Molecular Pharmacology June 1, 1999, 55 (6) 1101-1107; DOI: https://doi.org/10.1124/mol.55.6.1101

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Rapid CommunicationAccelerated CommunicationA

Cloning and Functional Expression of the Human Histamine H3 Receptor

Timothy W. Lovenberg, Barbara L. Roland, Sandy J. Wilson, Xiaoxia Jiang, Jayashree Pyati, Arne Huvar, Michael R. Jackson and Mark G. Erlander
Molecular Pharmacology June 1, 1999, 55 (6) 1101-1107; DOI: https://doi.org/10.1124/mol.55.6.1101
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