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 G_q 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]

H₁ Receptor 관련 제품 (173):

By Type:	Pan (30) Selective (26)
By Effects:	Inhibitors (25) Agonists (8) Antagonists (130) Modulators (6) Ligand (1)

Cat. No.	상품명	효과	Purity

HY-B0298

Clemastine	Antagonist	99.26%
Clemastine (HS-592; Meclastine) is an orally active, blood-brain barrier-permeable H1 histamine receptor (H1 histamine receptor) antagonist with potent antiallergic effects. Clemastine also antagonizes muscarinic acetylcholine receptors (mAChR), particularly the M1 and M4 subtypes. In addition to antihistamine effects, Clemastine exhibits multiple pharmacological activities, especially in promoting central nervous system remyelination, activating autophagy and pyroptosis, exerting anti-apoptotic and neuroprotective effects, and suppressing inflammation.

HY-B0274A

Chlorprothixene hydrochloride	Antagonist	99.91%
Chlorprothixene hydrochloride is a dopamine and histamine receptors antagonist with K_is of 18 nM, 2.96 nM, 4.56 nM, 9 nM and 3.75 nM for hD1, hD2, hD3, hD5 and hH1 receptors, respectively. Antipsychotic activity.

HY-B0426A

Olopatadine hydrochloride	Antagonist	99.83%
Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4⁺ and CD8⁺ T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis.

HY-B0548

Hydroxyzine	Antagonist	99.72%
Hydroxyzine, a benzodiazepine antihistamine agent, acts as an orally active histamine H1-receptor and serotonin antagonist. Hydroxyzine has anxiolytic effect and can be used for the research of generalised anxiety disorder.

HY-10121

Asenapine	Antagonist	99.62%
Asenapine (Org 5222), an atypical antipsychotic, is an antagonist of serotonin receptors (pK_i: 8.4-10.5), adrenoceptors (pK_i: 8.9-9.5), dopamine receptors (pK_i: 8.9-9.4) and histamine receptors (pK_i: 8.2-9.0). Asenapine can be used in the research of schizophrenia and bipolar disorder.

HY-B1215

Dimenhydrinate	Inhibitor	99.89%
Dimenhydrinate is an orally active H1-antihistamine consisting of Diphenhydramine (HY-B0303) and 8-Chlorotheophylline. Dimenhydrinate is used to prevent nausea, vomiting, dizziness, and vertigo associated with motion sickness.

HY-A0069

Doxylamine succinate	Inhibitor	99.76%
Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia.

HY-B0188

Mianserin	Inhibitor	99.42%
Mianserin (Mianserine) is an orally active H1 receptor antagonist. Mianserin can activate κ-opioid receptor and octopamine receptor. Mianserin increases ERK1/2 and CREB phosphorylation, and antagonizes full κ-opioid agonist and Dynorphin A (HY-P1333)-induced MAPK phosphorylation. Mianserin modulates social and exploratory behaviour, raises electroconvulsive thresholds. Mianserin can be used for the research of neurological disease, such as depression and epilepsy.

HY-A0075

Decloxizine dihydrochloride	Antagonist	99.69%
Decloxizine (UCB-1402; NSC289116) dihydrochloride is an orally active bronchodilator that can penetrate the blood-brain barrier. Decloxizine dihydrochloride is a piperazine-type H₁ histamine receptor antagonist. Decloxizine dihydrochloride selectively blocks H1 histamine receptors, inhibiting histamine-induced capillary dilation, edema, and itching. Decloxizine dihydrochloride has some 5-HT₂ receptor antagonistic activity. Decloxizine dihydrochloride can be used in studies of urticaria, allergic rhinitis, and bronchial asthma.

HY-14277A

Levocabastine hydrochloride	Antagonist	99.37%
Levocabastine (R 50547) hydrochloride is a potent and selective histamine H1-receptor antagonist. Levocabastine hydrochloride is also a selective, high affinity neurotensin receptor subtype 2 (NTR2) antagonist, with a K_i of 17 nM for mNTR2. Levocabastine hydrochloride can act as a VLA-4 antagonist, interferes with conjunctival eosinophil infiltration in allergic conjunctivitis (AC).

HY-148825

NP10679	Antagonist	98.40%
NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC₅₀s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC₅₀s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.

HY-13511A

Rupatadine Fumarate	Antagonist	99.99%
Rupatadine (UR-12592) Fumarate is a potent, orally active and long-lasting dual PAF/H1 antagonist, with K_is of 0.55 μM and 0.1 μM, respectively. Rupatadine Fumarate can be used for the research of allergic rhinitis and urticaria.

HY-108411

Emedastine	Antagonist	98.02%
Emedastine is an orally active, selective and high affinity histamine H₁ receptor antagonist with a K_i value of 1.3 nM. Emedastine is a benzimidazole derivative with potent antiallergic properties and used for allergic rhinitis, allergic skin diseases and allergic conjunctivitis.

HY-B0303AS1

Diphenhydramine-d₅ hydrochloride	Antagonist	99.84%
Diphenhydramine-d₅ (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB).

HY-14447

Bilastine	Antagonist	99.91%
Bilastine is an oral histamine H1-receptor antagonist. Bilastine can be used for allergic rhinitis and urticaria studies, and it also improves diabetic nephropathy in mice, showing safety for the central nervous system.

HY-B1301

Triprolidine hydrochloride monohydrate	Antagonist	99.92%
Triprolidine hydrochloride monohydrate, a first-generation antihistamine, is an oral active histamine H1 antagonist. Triprolidine hydrochloride monohydrate can be used for the research of allergic rhinitis. Triprolidine hydrochloride monohydrate exhibits spinal motor and sensory block in rats.

HY-B0538A

Pemirolast potassium	Antagonist	99.99%
Pemirolast potassium is an orally active antiallergic agent. Pemirolast potassium attenuates Paclitaxel (HY-B0015) hypersensitivity reactions. Pemirolast potassium can be used for bronchial asthma and conjunctivitis research^-.

HY-B1483

Methapyrilene hydrochloride	Inhibitor	99.88%
Methapyrilene (Thenylpyramine) hydrochloride is an orally active H1-receptor antihistamine and an anticholinergic agent of the pyridine chemical class. Methapyrilene hydrochloride has hepatotoxicity and can be used as a hepatotoxin that cause periportal hepatic necrosis in vivo

HY-B0303AS

Diphenhydramine-d₆ hydrochloride	Antagonist	99.30%
Diphenhydramine-d₆ (hydrochloride) is the deuterium labeled Diphenhydramine hydrochloride. Diphenhydramine hydrochloride is a first-generation histamine H1-receptor antagonist with anti-cholinergic effect. Diphenhydramine hydrochloride can across the ovine blood-brain barrier (BBB).

HY-B0895

Hydroxyzine pamoate	Antagonist	99.85%
Hydroxyzine pamoate is a histamine receptor H1 antagonist, one of the salt forms of Hydroxyzine, soluble in dimethyl formamide and chloroform but insoluble in water and alcohol.

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H1 Receptor

H1 Receptor 관련 제품 (173):

H₁ Receptor

H₁ Receptor 관련 제품 (173):