ArticleThe Biochemical journal2001
Genomic organization and characterization of splice variants of the human histamine H3 receptor.
Article in The Biochemical journal, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 24 papers.
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Who cites it
24 citing papers in PubMed, 125 citations in OpenAlex.
- Binding affinities for histamine receptors 1 to 4: Systematic comparison of ligands from the Psychoactive Drug Screening Program KMolecular pharmacology · 2026Review
- Decoding ligand recognition and constitutive activation of histamine H3 and H4 receptors.Acta pharmacologica Sinica · 2026Article
- Histamine HBiomolecules · 2024Review
- Histamine-3 Receptor Availability and Glutamate Levels in the Brain: A PET-1H-MRS Study of Patients With Schizophrenia and Healthy Controls.The international journal of neuropsychopharmacology · 2024Article
- Functional histamine HPharmacological research · 2018Article
- Inhibition of histamine receptor 3 suppresses glioblastoma tumor growth, invasion, and epithelial-to-mesenchymal transition.Oncotarget · 2015Article
- International Union of Basic and Clinical Pharmacology. XCVIII. Histamine Receptors.Pharmacological reviews · 2015Review
- The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.British journal of pharmacology · 2013Article
- A single-point mutation (Ala280Val) in the third intracellular loop alters the signalling properties of the human histamine H₃ receptor stably expressed in CHO-K1 cells.British journal of pharmacology · 2013Article
- Article
- The histamine autoreceptor is a short isoform of the H₃ receptor.British journal of pharmacology · 2012Article
- Development of time-resolved fluorescent based [EU]-GTP binding assay for selection of human Histamine 3 receptor antagonists/inverse agonist: a potential target for Alzheimer's treatment.Annals of neurosciences · 2012Article
- Histaminergic mechanisms for modulation of memory systems.Neural plasticity · 2011Review
- Molecular and biochemical pharmacology of the histamine H4 receptor.British journal of pharmacology · 2009Review
- Altered histamine H3 receptor radioligand binding in post-mortem brain samples from subjects with psychiatric diseases.British journal of pharmacology · 2009Article
- The histamine H4 receptor is functionally expressed on neurons in the mammalian CNS.British journal of pharmacology · 2009Article
- The histamine H3 receptor: an attractive target for the treatment of cognitive disorders.British journal of pharmacology · 2008Review
- Article
- Compared pharmacology of human histamine H3 and H4 receptors: structure-activity relationships of histamine derivatives.British journal of pharmacology · 2006Article
- The histamine H3 receptor: from gene cloning to H3 receptor drugs.Nature reviews. Drug discovery · 2005Review
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11 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
In the present paper we report the genomic organization of the human histamine H3-receptor gene, which consists of four exons spanning 5.5 kb on chromosome 20. Using PCR, six alternative splice variants of the H3 receptor were cloned from human thalamus. These variants were found to be coexpressed in human brain, but their relative distribution varied in a region-specific manner. These isoforms displayed either a deletion in the putative second transmembrane domain (TM), H3(DeltaTM2, 431aa) or a variable deletion in the third intracellular loop (i3), H3(Deltai3, 415aa), H3(Deltai3, 365aa), H3(Deltai3, 329aa) and H3(DeltaTM5+Deltai3, 326aa). In order to determine the biological role of the H3 receptor variants compared with the 'original' H3(445aa) receptor, three isoforms, namely H3(445aa), H3(DeltaTM2, 431aa) and H3(Deltai3, 365aa), were expressed in CHO cells and their pharmacological properties were investigated. Binding studies showed that H3(DeltaTM2, 431aa) transiently expressed in CHO cells was unable to bind [125I]iodoproxyfan, whereas both the H3(445aa) and H3(Deltai3, 365aa) receptors displayed a high affinity for [125I]iodoproxyfan [K(d)=28+/-5 pM (n=4) and 8+/-1 pM (n=5) respectively]. In addition, H3(Deltai3, 365aa) possessed the same pharmacological profile as the H3(445aa) receptor. However, in CHO cells expressing H3(Deltai3, 365aa), H3 agonists did not inhibit forskolin-induced cAMP production, stimulate [35S]guanosine 5'-[gamma-thio]triphosphate ([35S]GTP[S]) binding or stimulate intracellular Ca(2+) mobilization. Therefore the 80-amino-acid sequence located at the C-terminal portion of i3 plays an essential role in H3 agonist-mediated signal transduction. The existence of multiple H3 isoforms with different signal transduction capabilities suggests that H3-mediated biological functions might be tightly regulated through alternative splicing mechanisms.
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