Identification and characterization of histamine H4 receptor
| Autor: | Shunichiro Matsumoto, Tamaki Oda |
|---|---|
| Rok vydání: | 2001 |
| Předmět: |
Clobenpropit
Databases Factual Molecular Sequence Data Pharmacology Receptors G-Protein-Coupled chemistry.chemical_compound GTP-Binding Proteins medicine Animals Humans Tissue Distribution Amino Acid Sequence Histamine H4 receptor Receptor Receptors Histamine H4 Thioperamide Chemistry Histaminergic Receptors Histamine Histamine H3 receptor H3 receptor antagonist Sequence Alignment Histamine medicine.drug |
| Zdroj: | Folia Pharmacologica Japonica. 118:36-42 |
| ISSN: | 1347-8397 0015-5691 |
| Popis: | Recently, we and other groups have identified cDNA encoding the novel histamine H4 receptor. All of the groups have initially found a clue for the H4 receptor-nucleotides sequence in the human draft genomic DNA database. The primary structure of H4 receptor reveals the highest homology with H3 receptor among known G-protein coupled receptors (37.4%). H4 receptor binds to histamine with high affinity, which results in the down-regulation of intracellular cAMP level. H4 receptor is activated not only by histamine, but also R-(alpha)-methylhistamine (H3 receptor agonist), clobenpropit (H3 receptor antagonist), clozapine (neuroleptic) and other histaminergic compounds, while it is antagonized by thioperamide (H3 receptor antagonist). The H4 receptor is localized in the peripheral blood leukocytes, spleen, thymus, small intestine, colon, bone marrow and so on. The tissue distribution of the H4 receptor and known physiological function of histamine tempts us to speculate about its function as an immune modulator. Although there needs much additional work on characterization of the H4 receptor, the discovery of this receptor subtype will unveil a new phase for determining the physiological role of histamine. |
| Databáze: | OpenAIRE |
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