Histamine Receptor Inhibitor

TEI-6472, a naphthalene derivative, can suppress IgE responses both in vitro and in vivo. TEI-6472 causes significant inhibition of FceRI-mediated histamine release.

Azatadine is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine induces sedation and exhibits topical anesthetic properties. Azatadine can be used for the research of allergic rhinitis.

Proxibarbal is a barbiturate derivative. Proxibarbal has anti-anxiety properties and is also used for the study of migraine headaches.

Bamirastine inhibits ligand binding to recombinant human histamine H₁ receptors (rhH₁R) with an IC₅₀ value of 17.3 nM.

Rocastine (AHR-11325 ) is an orally active H₁-histamine receptor inhibitor that selectively binds to and functionally inhibits H1-histamine receptors. Rocastine protects guinea pigs from the lethal effect induced by Histamine (HY-B1204), prevents histamine-induced collapse, and protects guinea pigs from the falling reaction induced by nebulized antigens. Rocastine can be used in the research of allergic diseases.

Pitolisant-d₁₀ (Tiprolisant-d₁₀) is deuterium labeled Pitolisant. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (K_i=0.16 nM).

KF-17625 is an orally active bronchodilator. KF-17625 can inhibit bronchoconstriction induced by Carbachol (HY-B1208), Histamine (HY-B1204), or Leukotriene D4 (HY-113456). KF-17625 can inhibit canine tracheal phosphodiesterase (PDE) IV (IC₅₀ = 12 μM) and Concanavalin-A (HY-P2149)-induced histamine release from rat mast cells (44% inhibition at 10 mM). KF-17625 can be used for the researches of immunology and inflammation.

(S)-Azelastine ((+)-Azelastine) is an antihistamine with antiallergic and antiasthmatic activity. (S)-Azelastine has been shown to downregulate H1R, M1R, and M3R levels. (S)-Azelastine also has the property of inhibiting HNEpC proliferation.

Elbanizine inhibits histamine, bradykinin, histamin-release from rat mast cells (IC₅₀ of 0.26 μM) and the IgE-mediated passive cutaneous anaphylaxis (PCA) reaction. Elbanizine exhibits antiallergic and antiasthmatic in guinea pig model.

Mianserin-d₃ hydrochloride is the deuterium labeled Mianserin. 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.

Antihistamine-1 (Standard) is the analytical standard of Antihistamine-1 (HY-100238). This product is intended for research and analytical applications. Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.

Azatadine dimaleate (Standard) is the analytical standard of Azatadine dimaleate. This product is intended for research and analytical applications. Azatadine dimaleate (Azatadine maleate) is an orally active histamine H₁ receptor inhibitor, cetylcholine receptor inhibitor, and serotonin receptor inhibitor. Azatadine dimaleate induces sedation and exhibits topical anesthetic properties. Azatadine dimaleate can be used for the research of allergic rhinitis.

Undecane (Standard) is an analytical standard of Undecane (HY-N8593).Undecane is a potent cAMP agonist with anti-allergic and anti-inflammatory activities. Undecane inhibits degranulation and the secretion of histamine and TNF-α. Undecane reverses the increased levels of p38 phosphorylation, NF-κB transcriptional activity and target cytokine/chemokine genes, including thymus and activation-regulated chemokine (TARC), macrophage-derived chemokine (MDC) and interleukin-8 (IL-8). Undecane can be used for the study of skin inflammatory disorders, such as atopic dermatitis.

Ketotifen (fumarate) (Standard) is the analytical standard of Ketotifen (fumarate). This product is intended for research and analytical applications. Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.

(R)-(+)-Mequitazine is a histamine H1 receptor antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases.

D18024 is a phthalazinonderivat antiallergic and antihistaminic activity.

Embramine is a monoethanolamine used as an antihistamine and anticholinergic.

CI-949 is an allergic mediator release inhibitor, which inhibits histamine, leukotriene C₄/D₄ (LTC₄/LTD₄), and thromboxane B₂ (TXB₂) release with IC₅₀s of 11.4 μM, 0.5 μM and 0.1 μM, respectively.

KP136 (AL136) is an orally effective antiallergic agent. The IC₅₀ is 76.1 μg/mL for histamine release and 63 ug/mL for degranulation.