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Vol. 55, Issue 6, 1101-1107, June 1999
R.W. Johnson Pharmaceutical Research Institute, San Diego,
California
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.
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G. Drutel, N. Peitsaro, K. Karlstedt, K. Wieland, M. J. Smit, H. Timmerman, P. Panula, and R. Leurs Identification of Rat H3 Receptor Isoforms with Different Brain Expression and Signaling Properties Mol. Pharmacol., January 1, 2001; 59(1): 1 - 8. [Abstract] [Full Text]
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R. B. Silver, C. J. Mackins, N. C. E. Smith, I. L. Koritchneva, K. Lefkowitz, T. W. Lovenberg, and R. Levi Coupling of histamine H3 receptors to neuronal Na+/H+ exchange: A novel protective mechanism in myocardial ischemia PNAS, February 27, 2001; 98(5): 2855 - 2859. [Abstract] [Full Text] [PDF]
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