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 (178)
Related Products (178)
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Loratadine
0 ImagesSynonyms: Loratidine; SCH 29851Loratadine (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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Clemastine fumarate
0 ImagesSynonyms: HS-592 fumarate; Meclastine fumarateClemastine (HS-592; Meclastine) fumarate is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine fumarate also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine fumarate exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation .
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Desloratadine
0 ImagesSynonyms: Sch34117Desloratadine (Sch34117) is an orally active and selective H1 receptor antagonist (Ki=0.9 nM) with anti-inflammatory and anti-allergic activities. Desloratadine inhibits the release of histamine and LTC4 from human basophils and targets the regulatory signals of IL-4 and IL-13 production in basophils. Desloratadine significantly alleviates SAR symptoms in patients with concurrent asthma and can be used in the study of seasonal allergic rhinitis and chronic idiopathic urticaria.
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Astemizole
0 ImagesSynonyms: R 43512Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects.
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Terfenadine
0 ImagesSynonyms: (±)-Terfenadine; MDL-991Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9.
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YM-344484
0 ImagesCat. No.: HY-182736CAS No.: 671205-14-4YM-344484 is an orally active dual antagonist of chemokine CCR3 receptor and histamine histamine H1 receptor. YM-344484 inhibits ligand-induced Ca2+ influx, chemotaxis of CCR3-expressing cells, histamine-induced Ca2+ influx, increased vascular permeability and eosinophil accumulation. YM-344484 suppresses vascular permeability and inhibits eosinophil infiltration in a mouse asthma model. YM-344484 can be used in research related to asthma, allergic rhinitis and atopic dermatitis.
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Terfenadine N-oxide
0 ImagesCat. No.: HY-133727CAS No.: 634901-83-0Terfenadine N-oxide, an N-oxide derivative of Terfenadine (HY-B1193), is a histamine H1 receptor antagonist (IC50 = 2.73 μM) and an hERG potassium channel inhibitor (IC50 = 0.698 μM). Terfenadine N-oxide is can be used for the research of histamine-related allergic diseases and hERG channel-associated arrhythmias.
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AZD3778
0 ImagesCat. No.: HY-182439CAS No.: 485391-80-8AZD3778 (Compound 8) is an inhibitor of CCR3 and histamine H1 receptor (histamine H1 receptor), with IC50 values of 8.1 nM and 40 nM, respectively. AZD3778 inhibits the binding of eosinophil chemokines to CCR3, as well as the binding of histamine to histamine H1 receptor. AZD3778 exhibits anti-eosinophilic activity. AZD3778 alleviates symptoms associated with allergic rhinitis. AZD3778 can be used in research related to allergic rhinitis and asthma.
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Fexofenadine
0 ImagesSynonyms: MDL-16455; Terfenadine carboxylateFexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research.
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Ritanserin
0 ImagesSynonyms: R 55667Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.
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Amitriptyline hydrochloride
0 ImagesAmitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity.
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Ebastine
0 ImagesSynonyms: LAS-W 090; RP64305Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research.
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Mirtazapine
0 ImagesSynonyms: Org3770; 6-AzamianserinMirtazapine (Org3770) is a potent and orally active noradrenergic and specific serotonergic antidepressant (NaSSA) agent. Mirtazapine is also a 5-HT2, 5-HT3, histamine H1 receptor and α2-adrenoceptor antagonist with pKi values of 8.05, 8.1, 9.3 and 6.95, respectively.
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(S)-(+)-Dimethindene maleate
0 Images(S)-(+)-Dimethindene maleate, an enantiomer, is a potent M2-selective muscarinic receptor antagonist (pA2 = 7.86/7.74; pKi = 7.78). (S)-(+)-Dimethindene maleate shows lower affinities for the muscarinic M1 (pA2 = 6.83/6.36; pKi = 7.08), the M3 (pA2 = 6.92/6.96; pKi = 6.70) and the M4 receptors (pKi = 7.00), respectively. (S)-(+)-Dimethindene maleate also is a histamine H1 receptor antagonist (pA2 = 7.48).
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Fexofenadine hydrochloride
0 ImagesSynonyms: MDL-16455 hydrochloride; Terfenadine carboxylate hydrochlorideFexofenadine (MDL-16455) hydrochloride is an orally active and nonsedative H1 receptor antagonist. Fexofenadine hydrochloride can be used in allergic rhinitis and chronic idiopathic urticarial research.
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Meclizine dihydrochloride
0 ImagesMeclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR.
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Mepyramine maleate
0 ImagesMepyramine maleate (Pyrilamine maleate) is a selective histamine H1 receptor antagonist and KCNQ channel inhibitor, with an IC50 of 12.5 μM against KCNQ2/Q3. Mepyramine maleate shows no activity against allergic asthma in mice when used alone, but modulates the effect of JNJ 7777120 (HY-13508) on allergic asthma in mice; it inhibits the development of morphine physical dependence and increases histamine levels in mouse brains. Mepyramine maleate can be used in studies related to seizures, convulsions, allergic asthma and morphine physical dependence.
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Ketotifen
0 ImagesSynonyms: HC 20-511Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.
