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Vol. 59, Issue 1, 1-8, January 2001
Leiden/Amsterdam Center for Drug Research, Division of Medicinal
Chemistry, Faculty of Chemistry, Vrije Universiteit, Amsterdam, The
Netherlands (G.D., K.W., M.J.S., H.T., R.L.); Department of Biology,
Åbo Akademi University, Biocity, Turku, Finland (N.P., K.K., P.P.);
and Institute of Biomedicine, Department of Anatomy, University of
Helsinki, Helsinki, Finland (P.P.)
We identified the cDNAs of three functional rat H3 receptor
isoforms (H3A, H3B, and H3C) and
one nonfunctional truncated H3 receptor (H3T).
The H3A, H3B, and H3C receptor
isoforms vary in the length of their third intracellular loop; the
H3B and H3C receptor lack 32 and 48 amino
acids, respectively. Transient expression of the H3A,
H3B, and H3C receptors in COS-7 cells results
in high affinity binding for the H3 antagonist
[125I]iodophenpropit, which is displaced by selective
H3 agonists and antagonists. The three isoforms
differentially couple to the Gi protein-dependent
inhibition of adenylate cyclase or stimulation of p44/p42 mitogen
activated protein kinase (MAPK), a new signaling pathway for the
H3 receptor. Whereas the H3A receptor was less effective in inhibiting forskolin-induced cAMP production compared with
the H3B or H3C receptor, this isoform was more
effective in the stimulation of p44/p42 MAPK. The H3
receptor isoforms also displayed differential CNS expression in key
areas involved in regulation of sensory, endocrine, and cognitive
functions. A differential H3 receptor isoform expression
was seen in, for example, hippocampus, where a characteristic
dorsoventral distribution was revealed. Differential H3
receptor expression was also characteristic for the cerebellum,
indicating possible histaminergic regulation of motor functions. The
identification of these new H3 receptor isoforms and their
specific signaling properties adds a new level of complexity to our
understanding of the role of histamine, and the H3 receptor in brain function. The heterogeneous distribution of the isoforms suggests that H3 receptor isoform-specific regulation is
important in several brain functions.
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