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Vol. 299, Issue 1, 121-130, October 2001
The R. W. Johnson Pharmaceutical Research Institute, San
Diego, California
The recently identified histamine H4 receptor has revealed
a potential new complexity for the role of histamine in the immune system. To begin to understand the role of this receptor in humans, one
must first determine whether homologs exist and can be studied in lower
species. To address this, we cloned the rat, mouse, and guinea pig
cDNAs corresponding to the recently identified human histamine
H4 receptor. The rat, mouse, and guinea pig H4
sequences are significantly different from the human H4
sequence at 69, 68, and 65% homology, respectively. The tissue
distribution of the rat, mouse, and guinea pig H4 receptors
is similar to human in that bone marrow and spleen are the most
abundant sources of expression. The human and guinea pig H4
receptors display the highest binding affinity for
[3H]histamine (KD = 5 nM
each), whereas the affinities for rat and mouse receptors are
substantially lower at 136 and 42 nM, respectively. With respect to the
pharmacological profile of known H3/H4 ligands, even greater differences in binding affinities exist among the species
homologs. There are also substantial differences in the signal
transduction response to each of the four species of H4 receptor. This work demonstrates the existence of histamine
H4 receptors in lower species and demonstrates that a clear
knowledge of each species pharmacological profile will be essential to
elucidate the role of this receptor subtype in vivo.
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