H1 Receptor
Histamine H1 receptor (H1R) is a rhodopsin-like G protein-coupled receptor that mediates cellular responses to histamine in vascular endothelial cells, smooth muscle cells, immune cells, and the central nervous system[1][2]. H1R primarily couples to Gq proteins and activates phospholipase C-dependent signaling, leading to inositol trisphosphate generation, intracellular calcium mobilization, and downstream inflammatory responses[1][3]. Mechanistically, H1R signaling promotes activation of the transcription factor NF-κB, linking receptor stimulation to the expression of pro-inflammatory mediators and immune-regulatory pathways involved in allergic inflammation[4][5]. Consequently, H1R is a central mediator of allergic diseases, contributing to vascular permeability, pruritus, bronchoconstriction, and inflammatory cell recruitment in experimental and clinical settings[2][6]. In disease models, histamine released from mast cells acts through H1R to coordinate leukocyte activation and migration, thereby sustaining chronic inflammatory responses[7]. Compared with related histamine receptor isoforms, H1R is primarily associated with allergic and inflammatory signaling, whereas H2 receptors regulate gastric acid secretion, H3 receptors modulate neurotransmitter release, and H4 receptors are more closely linked to immune-cell chemotaxis and immune regulation[8]. For experimental applications, H1R has become a validated pharmacological target, and H1-receptor antagonists or inverse agonists are widely used to suppress receptor-dependent inflammatory signaling and to investigate histamine-driven biological processes in allergy and inflammation research[4][9].
References:
- [1]. Neumann J, et al. Function and Role of Histamine H1 Receptor in the Mammalian Heart. Pharmaceuticals (Basel). 2023 May 11;16(5):734. [Content Brief]
- [2]. Togias A. H1-receptors: localization and role in airway physiology and in immune functions. J Allergy Clin Immunol. 2003 Oct;112(4 Suppl):S60-8. [Content Brief]
- [3]. Simons FE, et al. Histamine and H1-antihistamines: celebrating a century of progress. J Allergy Clin Immunol. 2011 Dec;128(6):1139-1150.e4. [Content Brief]
- [4]. Nakayama A, et al. Identification of the catalytic residues of bifunctional glycogen debranching enzyme. J Biol Chem. 2001 Aug 3;276(31):28824-8. [Content Brief]
- [5]. Adderley SP, et al. Involvement of the H1 Histamine Receptor, p38 MAP Kinase, Myosin Light Chains Kinase, and Rho/ROCK in Histamine-Induced Endothelial Barrier Dysfunction. Microcirculation. 2015 May;22(4):237-48. [Content Brief]
- [6]. Simons FE. Advances in H1-antihistamines. N Engl J Med. 2004 Nov 18;351(21):2203-17. doi: 10.1056/NEJMra033121. PMID: 15548781. et al. Advances in H1-antihistamines. N Engl J Med. 2004 Nov 18;351(21):2203-17. [Content Brief]
- [7]. Thangam EB, et al. The Role of Histamine and Histamine Receptors in Mast Cell-Mediated Allergy and Inflammation: The Hunt for New Therapeutic Targets. Front Immunol. 2018 Aug 13;9:1873. [Content Brief]
- [8]. Eisenhofer G, et al. Catecholamine metabolism: a contemporary view with implications for physiology and medicine. Pharmacol Rev. 2004 Sep;56(3):331-49. [Content Brief]
- [9]. Kiros M, et al. Trends in HIV-1 pretreatment drug resistance and HIV-1 variant dynamics among antiretroviral therapy-naive Ethiopians from 2003 to 2018: a pooled sequence analysis. Virol J. 2023 Oct 25;20(1):243. [Content Brief]
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H1 Receptor Related Products (187)
Related Products (187)
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Epinastine hydrochloride
0 ImagesSynonyms: WAL801 hydrochlorideEpinastine hydrochloride (WAL801 hydrochloride) is a selective and orally active histamine H1 receptor antagonist, CD96/PVR inhibitor and mast cell stabilizer. Epinastine hydrochloride has high affinity for neuronal octopamine receptors in locusts (Ki = 2 nM) and honeybees (Ki = 1.1 nM). Epinastine hydrochloride inhibits TARC, IL-8, and IL-4. Epinastine hydrochloride activates anti-colon cancer immunity and inhibits Substance P (HY-P0201)-induced scratching behavior and increased vascular permeability. Epinastine hydrochloride can be used in the research of allergic diseases.
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Pheniramine maleate
0 ImagesSynonyms: Prophenpyridamine maleate; Tripoton maleatePheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects.
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UNC9994
0 ImagesUNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.
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Brompheniramine maleate
0 ImagesBrompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the alkylamine class. Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate can block the hERG channels, calcium channels, and sodium channels with IC50s of 0.90 μM, 16.12 μM and 21.26 μM, respectively. Brompheniramine maleate has anticholinergic, antidepressant and anesthetic properties and can be used for allergic rhinitis research.
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Thiethylperazine dimaleate
0 ImagesThiethylperazine dimaleate, a phenothiazine derivate, is an orally active and potent dopamine D2-receptor and histamine H1-receptor antagonist. Thiethylperazine dimaleate is also a selective ABCC1activator that reduces amyloid-β (Aβ) load in mice. Thiethylperazine dimaleate has anti-emetic, antipsychotic and antimicrobial effects.
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Cyproheptadine hydrochloride sesquihydrate
0 ImagesCyproheptadine hydrochloride sesquihydrate acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride sesquihydrate mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride sesquihydrate induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride sesquihydrate inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride sesquihydrate can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.
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HTMT dimaleate
0 ImagesHTMT (dimaleate) is a potent histamine H1 and H2 receptor agonist. HTMT (dimaleate) is 4 x 104 times more active than histamine in H2-mediated effects in natural suppressor cells.
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Carbinoxamine maleate salt
0 ImagesCarbinoxamine maleate salt is a blood-brain barrier-permeable histamine H1 receptor antagonist. Carbinoxamine maleate salt blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. Carbinoxamine maleate salt inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. Carbinoxamine maleate salt can be used in research on allergic rhinitis, influenza, etc.
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HY-078020
0 ImagesHY-078020 (compound III-4) is a selective, orally active antagonist for histamine H1 receptor with an IC50 of 24.12 nM. HY-078020 exhibits an anti-inflammatory effect in allergic diseases.
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Diphenylpyraline hydrochloride
0 ImagesSynonyms: 4-Diphenylmethoxy-1-methylpiperidine hydrochlorideDiphenylpyraline hydrochloride is a potent histamine H1?receptor antagonist. Diphenylpyraline hydrochloride acts as an orally active antihistamine agent?with antimuscarinic and antiallergic effects. Diphenylpyraline hydrochloride can be used for the relief of allergic conditions including rhinitis and hay fever, and in pruritic skin disorders in vivo.
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Cetirizine-d8
0 ImagesCat. No.: HY-17042S1CAS No.: 774596-22-4Cetirizine-d8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
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AVN-101 hydrochloride
0 ImagesAVN-101 hydrochloride is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (Ki of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively). AVN-101 hydrochloride also exhibits a rather high affinity toward histamine H1 (Ki of 0.58 nM) and adrenergic α2A, α2B, and α2C (Ki= 0.41-3.6 nM) receptors. AVN-101 hydrochloride can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.
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Loratadine-d5
0 ImagesSynonyms: Loratidine-d5; SCH 29851-d5Loratadine-d5 is the deuterium labeled Loratadine. Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.
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Dexbrompheniramine
0 ImagesSynonyms: (+)-Brompheniramine; (S)-BrompheniramineDexbrompheniramine ((+)-Brompheniramine; (S)-Brompheniramine) is a dual inhibitor of histamine H1 receptor and TRPV1 receptor that can cross the blood-brain barrier. Dexbrompheniramine exerts its effects by functionally blocking H1 receptor activity and dose-dependently inhibiting TRPV1-mediated calcium responses, including Capsaicin (HY-10448)-induced responses. The combination of Dexbrompheniramine with Cimetidine (HY-14289) eliminates histamine-induced and sham-feeding-induced drinking behavior, whereas Dexbrompheniramine alone does not induce thirst or alter sham-feeding behavior in rats. Dexbrompheniramine can be used in the research of chronic cough and related pathological mechanisms.
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Antazoline
0 ImagesAntazoline (Phenazoline) is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC50 of 2.910 μmol/L in HepAD38 cells. Antazoline also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC50 = 2.349 μmol/L). Antazoline has anti-arrhythmic effect in acute myocardial infarctions. Antazoline can be studied in research for cardiovascular diseases, and HBV.
