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Vol. 293, Issue 3, 771-778, June 2000
R. W. Johnson Pharmaceutical Research Institute, San Diego,
California
The recent cloning and characterization of the human histamine
H3 receptor cDNA marked a significant step toward a greater understanding of the role of this receptor in the central nervous system. We now report the cloning of the rat histamine H3
receptor cDNA and demonstrate distinct pharmacological species
differences. The rat cDNA clone encodes a putative 445-amino acid
protein with 93% identity to the human H3 receptor.
Northern blot analysis revealed a major single entity of 2.7-kb in
length expressed only in brain. Transfection of the rat receptor cDNA
into SK-N-MC cells conferred an ability to inhibit forskolin-stimulated
cAMP formation in response to histamine and other H3
agonists. N-[3H]methylhistamine saturably
bound to transfected cells with high affinity
(Kd = 0.8 nM). All agonists tested had
low or subnanomolar Ki values similar to
that for the human recombinant receptor. The antagonists thioperamide
and clobenpropit also bound with high affinity
(Ki = 4 and 0.4 nM, respectively). This
is in contrast to the antagonist profile obtained for the human
recombinant receptor that showed Ki values
of 58 and 0.6 nM for thioperamide and clobenpropit, respectively. These
data suggest that the low affinity of thioperamide for the human
H3 receptor represents a species difference in pharmacology and not a unique pharmacological subtype. It also was found that chloroproxyfan behaved as a full agonist at the rat recombinant receptor. These findings highlight the significance of validating the
pharmacology of experimental compounds at both the rat and human
H3 receptors.
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