Title: Molecular and pharmacological characterization of the mouse histamine H3 receptor
Abstract: Human, guinea pig and rat histamine H3 receptors have been investigated at both pharmacological and molecular levels in recent years. Here we report the cloning, molecular, and pharmacological characterization of the mouse histamine H3 receptor. The amino acid sequence of the mouse histamine H3 receptor exhibits high homology to rat, guinea pig and human histamine H3 receptors with 98%, 95%, 94% identities, respectively. The distribution of the mRNA encoding the mouse histamine H3 receptor was predominant in the brain as detected by Reverse Transcription-Polymerase Chain Reaction (RT-PCR) and RNase protection assay. Although several splice forms have been reported for human, guinea pig and rat histamine H3 receptor mRNAs, we did not detect equivalent isoforms in the mouse in several tissues by either RNase protection assay or robust Polymerase Chain Reaction (PCR) amplifications. Human embryonic kidney (HEK)-293 cells transiently transfected with mouse histamine H3 receptor cDNA and Gqi5 exhibited increases of intracellular Ca2+ in response to histamine and several histamine H3 receptor agonists. COS-7 (African green monkey kidney) cells transfected with mouse histamine H3 receptor cDNA showed high affinity binding for histamine H3 receptor ligands in competition binding assays. The pharmacological comparison of human, guinea pig, rat and mouse histamine H3 receptors indicated that, as expected, the mouse histamine H3 receptor exhibited a more similar pharmacological profile to the rat histamine H3 receptor than to either the human or the guinea pig histamine H3 receptor. Taken together, these findings allow a further appreciation of the histamine H3 receptor at the molecular level and provide an additional species to assist in the pharmacological assessment of histamine H3 receptor function.
Publication Year: 2003
Publication Date: 2003-04-01
Language: en
Type: article
Indexed In: ['crossref', 'pubmed']
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Cited By Count: 75
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