Histamine H1 receptor

UniProt P35367 Organism Homo sapiens Gene HRH1

Also known as: HRH1

Function

G protein-coupled receptor for histamine, a biogenic amine that functions as an immune modulator and a neurotransmitter. Through the H1 receptor, histamine mediates the contraction of smooth muscles and increases capillary permeability due to contraction of terminal venules. Also mediates neurotransmission in the central nervous system and thereby regulates circadian rhythms, emotional and locomotor activities as well as cognitive functions (By similarity).

Classification

Family (Pfam): PF00001 7tm_1
InterPro: GPCR_Rhodpsn, GPCR_Rhodpsn_7TM, Histamine_H1_rcpt
Functional cluster: G Protein-Coupled Receptors

Experimental structures · PDB · 9

3RZE X-ray 3.10A
7DFL EM 3.30A
8X5X EM 3.50A
8X5Y EM 3.00A
8X63 EM 3.20A
8X64 EM 3.40A
8YN2 EM 2.66A
9LRB EM 2.77A
9LRD EM 3.23A

A predicted model is available from AlphaFold.

Gene Ontology · 12

Drugs targeting this protein · 71

DESLORATADINE antagonist
DOXYLAMINE SUCCINATE antagonist
ORPHENADRINE CITRATE antagonist
DIMENHYDRINATE antagonist
TRIPELENNAMINE HYDROCHLORIDE antagonist
HYDROXYZINE PAMOATE antagonist
EPINASTINE HYDROCHLORIDE antagonist
CYCLIZINE LACTATE antagonist
METHDILAZINE HYDROCHLORIDE antagonist
ANTAZOLINE PHOSPHATE antagonist
FEXOFENADINE HYDROCHLORIDE antagonist
DEXBROMPHENIRAMINE MALEATE antagonist
PROMETHAZINE HYDROCHLORIDE antagonist
TRIPELENNAMINE CITRATE antagonist
CLEMASTINE FUMARATE antagonist
AZELASTINE HYDROCHLORIDE antagonist
DEXCHLORPHENIRAMINE MALEATE antagonist
TRIMIPRAMINE MALEATE antagonist
METHDILAZINE antagonist
BROMPHENIRAMINE MALEATE antagonist
BROMODIPHENHYDRAMINE HYDROCHLORIDE antagonist
CARBINOXAMINE MALEATE antagonist
PYRILAMINE MALEATE antagonist
ORPHENADRINE HYDROCHLORIDE antagonist
PROPIOMAZINE HYDROCHLORIDE antagonist
DIPHENHYDRAMINE CITRATE antagonist
LEVOCETIRIZINE DIHYDROCHLORIDE antagonist
ALCAFTADINE antagonist
BEPOTASTINE BESYLATE antagonist
ACRIVASTINE antagonist
LEVOCABASTINE HYDROCHLORIDE antagonist
METHAPYRILENE HYDROCHLORIDE antagonist
OXATOMIDE antagonist
DIBENZEPIN antagonist
DIPHENYLPYRALINE HYDROCHLORIDE antagonist
CETIRIZINE HYDROCHLORIDE antagonist
DIPHENHYDRAMINE HYDROCHLORIDE antagonist
DOXEPIN antagonist
KETOTIFEN FUMARATE antagonist
PHENIRAMINE MALEATE antagonist
CHLORPHENIRAMINE MALEATE antagonist
TOLAZOLINE HYDROCHLORIDE agonist
TERFENADINE antagonist
CYPROHEPTADINE HYDROCHLORIDE antagonist
OLOPATADINE HYDROCHLORIDE antagonist
BILASTINE inverse agonist
GSK-1004723 antagonist
EMEDASTINE DIFUMARATE antagonist
THENALIDINE antagonist
ESMIRTAZAPINE MALEATE antagonist
CHLORPHENOXAMINE antagonist
DIMETHINDENE antagonist
BUCLIZINE HYDROCHLORIDE antagonist
BETAHISTINE agonist
PHENINDAMINE antagonist
ASTEMIZOLE antagonist
EBASTINE inverse agonist
HYDROXYZINE HYDROCHLORIDE antagonist
METHAPYRILENE FUMARATE antagonist
TRIPROLIDINE HYDROCHLORIDE antagonist
AZATADINE MALEATE antagonist
HISTAMINE PHOSPHATE agonist
MECLIZINE HYDROCHLORIDE antagonist
TRIMEPRAZINE TARTRATE antagonist
CINNARIZINE antagonist
LY2624803 antagonist
VAPITADINE DIHYDROCHLORIDE antagonist
MEQUITAZINE antagonist
RUPATADINE antagonist
MIZOLASTINE antagonist
LORATADINE antagonist

Related proteins · sequence + function similarity

Histamine H1 receptor 1.00
Histamine H1 receptor 1.00
Histamine H1 receptor 1.00
Histamine H1 receptor 0.98
Histamine H1 receptor 0.98
Histamine H1 receptor 0.96
Histamine H1 receptor 0.96
Alpha-2 adrenergic receptor 0.88
Muscarinic acetylcholine receptor M5 0.88
Muscarinic acetylcholine receptor M5 0.88
5-hydroxytryptamine receptor 1A-beta 0.88
Alpha-2Db adrenergic receptor 0.88

Co-cited proteins · studied together in the literature

Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2 1 shared papers
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1 1 shared papers

Literature · 13 cited papers

Cryo-EM structure of the human histamine H1 receptor/Gq complex. Nat. Commun. · 2021
Toward a comprehensive characterization of a human cancer cell phosphoproteome. J. Proteome Res. · 2013
Structure of the human histamine H1 receptor complex with doxepin. Nature · 2011
Kinase-selective enrichment enables quantitative phosphoproteomics of the kinome across the cell cycle. Mol. Cell · 2008
A quantitative atlas of mitotic phosphorylation. Proc. Natl. Acad. Sci. U.S.A. · 2008
The consensus coding sequences of human breast and colorectal cancers. Science · 2006
The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC). Genome Res. · 2004
Two threonine residues and two serine residues in the second and third intracellular loops are both involved in histamine H1 receptor downregulation. FEBS Lett. · 2004
Human-specific amino acid changes found in 103 protein-coding genes. Mol. Biol. Evol. · 2004
Complete sequencing and characterization of 21,243 full-length human cDNAs. Nat. Genet. · 2004
Genomic cloning, heterologous expression and pharmacological characterization of a human histamine H1 receptor. Biochem. Biophys. Res. Commun. · 1993
Molecular cloning of the human histamine H1 receptor gene. Biochem. Biophys. Res. Commun. · 1994
… and 1 more in the literature graph

A document in the lmmol reference corpus — open public data (UniProt, GO, PDB, the literature graph) rendered as a single cross-linked page. Hover any link to preview its target.