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Vol. 59, Issue 3, 427-433, March 2001
The Centre for Addiction and Mental Health, Toronto, Ontario,
Canada (T.N., S.R.G., R.C., B.F.O.); Departments of Pharmacology
(S.R.G., D.K.L., S.P.L., B.F.O.) and Medicine (S.R.G.), University of
Toronto, Toronto, Ontario, Canada; Department of Biochemistry
(D.A.S., V.S., B.L.R.) and National Institute of Mental Health
Psychoactive Drug Screening Program (L.R., B.L.R.), Case Western
Reserve University Medical School, Cleveland, Ohio; and Department of
Pharmacology, University of Virginia Health Sciences Center,
Charlottesville, Virginia (K.R.L).
We report the discovery, tissue distribution and pharmacological
characterization of a novel receptor, which we have named H4. Like the
three histamine receptors reported previously (H1, H2, and H3), the H4
receptor is a G protein-coupled receptor and is most closely related to
the H3 receptor, sharing 58% identity in the transmembrane regions.
The gene encoding the H4 receptor was discovered initially in a search
of the GenBank databases as sequence fragments retrieved in a partially
sequenced human genomic contig mapped to chromosome 18. These sequences
were used to retrieve a partial cDNA clone and, in combination with
genomic fragments, were used to determine the full-length open reading frame of 390 amino acids. Northern analysis revealed a 3.0-kb transcript in rat testis and intestine. Radioligand binding studies indicated that the H4 receptor has a unique pharmacology and binds [3H]histamine (Kd = 44 nM) and [3H]pyrilamine
(Kd = 32 nM) and several psychoactive
compounds (amitriptyline, chlorpromazine, cyproheptadine, mianserin)
with moderate affinity (Ki range of 33-750
nM). Additionally, histamine induced a rapid internalization of
HA-tagged H4 receptors in transfected human embryonic kidney 293 cells.
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