2. GPCR/G Protein
    Immunology/Inflammation
    Neuronal Signaling
  3. Histamine Receptor

Histamine Receptor

Histamine Receptors are a class of G protein-coupled receptors with histamine as their endogenous ligand. There are four known histamine receptors: H1 receptor, H2 receptor, H3 receptor, H4 receptor. The H1 receptor is a histamine receptor belonging to the family of Rhodopsin-like G-protein-coupled receptors. This receptor, which is activated by the biogenic amine histamine, is expressed throughout the body, to be specific, in smooth muscles, on vascular endothelial cells, in the heart, and in the central nervous system. H2 receptors are positively coupled to adenylate cyclase via Gs. It is a potent stimulant of cAMP production, which leads to activation of Protein Kinase A. Histamine H3 receptors are expressed in the central nervous system and to a lesser extent the peripheral nervous system, where they act asautoreceptors in presynaptic histaminergic neurons, and also control histamine turnover by feedback inhibition of histamine synthesis and release. The Histamine H4 receptor has been shown to be involved in mediating eosinophil shape change and mast cell chemotaxis.

Histamine Receptor Related Products (362):

Cat. No. Product Name Effect Purity
  • HY-B0527A
    Amitriptyline hydrochloride Inhibitor 98.91%
    Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].
  • HY-12532
    Astemizole Antagonist
    Astemizole (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[1][2].
  • HY-B0298A
    Clemastine fumarate Antagonist 99.97%
    Clemastine (HS-592) fumarate is a selective histamine H1 receptor antagonist. Clemastine fumarate is an antihistamine mainly used for relieving symptoms of allergic reactions primarily by competing with histamine to bind H1 receptors. Anti-inflammatory effects[1][2].
  • HY-B1193
    Terfenadine Antagonist 99.91%
    Terfenadine ((±)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM[1]. 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[2].
  • HY-B1204
    Histamine Activator
    Histamine is an organic nitrogenous compound involved in local immune responses as well as regulating physiological function in the gut and acting as a neurotransmitter.
  • HY-B1204R
    Histamine (Standard) Activator
    Histamine (Standard) is the analytical standard of Histamine. This product is intended for research and analytical applications.
  • HY-W010841R
    Levocetirizine dihydrochloride (Standard) Antagonist
    Levocetirizine (dihydrochloride) (Standard) is the analytical standard of Levocetirizine (dihydrochloride). This product is intended for research and analytical applications. Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
  • HY-B1062R
    Dexchlorpheniramine maleate (Standard) Inhibitor
    Dexchlorpheniramine (maleate) (Standard) is the analytical standard of Dexchlorpheniramine (maleate). This product is intended for research and analytical applications. Dexchlorpheniramine maleate is an antihistamine with anticholinergic properties used in the study of allergic diseases.
  • HY-101188
    INCB38579 Antagonist 99.97%
    INCB38579 is an orally active, highly brain penetrable, and selective histamine H4 receptor (HH4R) antagonist (hH4R IC50=4.8 nM, mH4R IC50=42 nM, rH4R IC50=32 nM). INCB38579 shows anti-inflammatory pain and anti-pruritic activities[1].
  • HY-B1510S
    Acrivastine D7 Antagonist
    Acrivastine-d7 is a deuterium labeled Acrivastine. Acrivastine is a short acting histamine 1 receptor antagonist.
  • HY-13448
    Nedocromil Inhibitor
    Nedocromil suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  • HY-B0188A
    Mianserin hydrochloride Inhibitor 99.87%
    Mianserin hydrochloride (Org GB 94) is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.
  • HY-107563
    ROS 234 Antagonist
    ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access[1][2].
  • HY-W281862
    Sequifenadine Inhibitor
    Sequifenadine is a H1-antihistamine. Sequifenadine has the potential for the research of inflammatory eye disease with allergic symptoms[1][2].
  • HY-B0527AS
    Amitriptyline-d6 hydrochloride Inhibitor 99.65%
    Amitriptyline-d6 (hydrochloride) is the deuterium labeled Amitriptyline hydrochloride. Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with Kis of 3.45 nM and 13.3 nM for human SERT and NET, respectively. Amitriptyline hydrochloride also weakly binds to dopamine reuptake transporter (DAT) with a Ki of 2.58 μM. Amitriptyline hydrochloride also inhibits adrenergic, muscarinic, histamine and 5-HT receptors. Amitriptyline hydrochloride is a TrkA and TrkB receptors agonist with potent neurotrophic activity. Amitriptyline hydrochloride has antidepressant activity[1][2][3].
  • HY-16344
    Nedocromil sodium Inhibitor
    Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2).
  • HY-B1808A
    Triprolidine hydrochloride Antagonist
    Triprolidine hydrochloride is an orally active histamine H1 antagonist. Triprolidine hydrochloride has the function of spinal cord motor and sensory block. Triprolidine hydrochloride can be used for the research of allergic rhinitis[1][2][3].
  • HY-W010841
    Levocetirizine dihydrochloride Antagonist
    Levocetirizine dihydrochloride ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].
  • HY-146035
    AChE-IN-14 Inhibitor
    AChE-IN-14 (compound 5) is a potent cholinesterase inhibitor with IC50s of 0.46 , 0.48, and 0.44 μM for electric eel acetylcholinesterase (eeAChE), human recombinant acetylcholinesterase (hAChE), and equine serum butyrylcholinesterase (eqBuChE), respectively. AChE-IN-14 exhibits high affinity toward human H3 receptor (H3R; Ki= 159.8 nM). AChE-IN-14 can be used for the research of Alzheimer’s disease[1].
  • HY-101373A
    Zolantidine dimaleate Antagonist 99.88%
    Zolantidine dimaleate (SKF 95282 dimaleate) is a potent, selective and cross the blood-brain barrier histamine H2 antagonist. Zolantidine dimaleate induces antinociception[1][2].