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Vol. 296, Issue 3, 1058-1066, March 2001
Departments of Human Genomics Research (K.L.M., J.B., T.M.L., N.S.,
E.L.G., X.Q., S.W., J.A.H., J.G., M.B., F.J.M.), Allergy (R.E.W.,
S.A.G., J.C.A., S.U., Y.W.), and Immunology (R.W.H., W.G.),
Schering-Plough Research Institute, Kenilworth, New Jersey
Histamine exerts its numerous physiological functions through
interaction with G protein-coupled receptors. Three such
receptors have been defined at both the pharmacological and molecular
level, while pharmacological evidence hints at the existence of further subtypes. We report here the cloning and characterization of a fourth
histamine receptor subtype. Initially discovered in an expressed-sequence tag database, the full coding sequence (SP9144) was
subsequently identified in chromosome 18 genomic sequence. This virtual
coding sequence exhibited highest homology to the H3
histamine receptor and was used to generate a full-length clone by
polymerase chain reaction (PCR). The distribution of mRNA encoding SP9144 was restricted to cells of the immune system as determined by
quantitative PCR. HEK-293 cells transiently transfected with SP9144 and
a chimeric G protein 
-subunit (Gq/i1,2) exhibited increases in intracellular [Ca2+] in response to
histamine but not other biogenic amines. SP9144-transfected cells
exhibited saturable, specific, high-affinity binding of [3H]histamine, which was potently inhibited by
H3 receptor-selective compounds. The rank order and potency
of these compounds at SP9144 differed from the rank order at the
H3 receptor. Although SP9144 apparently coupled to
Gi, HEK-293 cells stably transfected with SP9144 did not
exhibit histamine-mediated inhibition of forskolin-stimulated cAMP
levels. However, both [35S]GTP
S binding and
phosphorylation of mitogen-activated protein kinase were stimulated by
histamine via SP9144 activation. In both of these assays, SP9144
exhibited evidence of constitutive activation. Taken together, these
data demonstrate that SP9144 is a unique, fourth histamine receptor subtype.
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