Histamine Receptor Inhibitor

Tiaramide (RHC 2592-A) hydrochloride is an analgesic agent with antiallergic activity, and is also a non-steroidal, anti-inflammatory compound. Tiaramide hydrochloride inhibits histamine release.

H3R antagonist 1 hydrochloride is a histamine receptor 3 (H3R) inverse agonist. H3R antagonist 1 hydrochloride increases the expression levels of myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes. H3R antagonist 1 hydrochloride can be used for the study of multiple sclerosis.

Propiomazine is an orally active antihistamine agent. Propiomazine is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.

(Rac)-Bepotastine (besilate) is the isomer of Bepotastine (besilate) (HY-A0015), and can be used as an experimental control. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research.

Nesosteine (CO-1177) is a bronchitis inhibitor that improves the rheology and production of airway bronchial mucus in rabbits. Nesosteine significantly reduced the viscosity of airway bronchial mucus in animals with sulfuric acid nebulized bronchitis and increased mucus production in healthy animals. Nesosteine is more active than mucus-regulating drugs such as Sobrerol, N-acetylcysteine, bromhexine, ambroxol, S-carboxymethylcysteine, and mercaptoalanine. Nesosteine also reduced the content of total proteins in airway bronchial mucus, such as albumin, α1, α2, β, and γ mucins.

JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC₅₀ of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research.

Dimethindene is a potent, selective histamine H1 antagonist. Dimethindene impairs cutaneous wound healing (WH). Dimethindene can block K⁺ currents.

Bufrolin is a Cromoglycate (histamine release inhibitor) analog and a high potency agonist of GPR35. Bufrolin promotes interactions between β-arrestin-2 and either human GPR35a or rat GPR35. Bufrolin also serves as antiallergic mast cell stabilizer and inhibit an anti-inflammatory response inducible by the internalization peptide. Bufrolin acts as an anti-inflammatory agent to be used in research of delivering pharmacol linked with internalization peptide.

Setastine (EGIS-2062 (free acid); EGYT-2062 (free acid) is an orally effective, non-sedative and long acting anti-allergic agent. Setastine possesses potent histamine Hi-receptor blocking properties and can be used for allergies and rhinitis research^[1]<.

Chlorphenoxamine, an antihistamine and anticholinergic agent is a GPCR antagonist. Chlorphenoxamine inhibits multiple lethal viral diseases, such as SARS-CoV, MERS-CoV, EBOV and malaria. Chlorphenoxamine shows anti-filovirus activity against both EBOV and Marburg virus (MARV) with IC₅₀s of 1.1 μM and 6.2 μM, respectively. Chlorphenoxamine is used for allergic conditions, urticaria, viral diseases and Parkinson’s disease.

Ketotifen-d₃ (fumarate) is the deuterium labeled Ketotifen fumarate. Ketotifen (HC 20511) fumarate is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks.

Amitriptyline-d3 hydrochloride is the deuterium labeled Amitriptyline (hydrochloride). Amitriptyline hydrochloride is an inhibitor of serotonin reuptake transporter (SERT) and noradrenaline reuptake transporter (NET), with K_is 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 K_i 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.

Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C₄ (LTC₄), and prostaglandin D₂ (PGD₂).

Osthole (Standard) is the analytical standard of Osthole. This product is intended for research and analytical applications. Osthole (Osthol) is a natural antihistamine alternative. Osthole may be a potential inhibitor of histamine H1 receptor activity. Osthole also suppresses the secretion of HBV in cells.

H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC₅₀ of 19 nM.

Bromodiphenhydramine hydrochloride is a potent antihistamine with antimicrobial property. Bromodiphenhydramine hydrochloride inhibits a large number of Gram negative and Gram positive bacteria. Bromodiphenhydramine hydrochloride can be used for cutaneous allergies research.

Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease.

Nimbin is an orally active intermediate limonoid found in Azadirachta. Nimbin prevents tau aggregation and increases cell viability. Nimbin is effective inhibits the envelope protein of dengue virus. Nimbin has anti-inflammatory, antipyretic, antifungal, antihistamine, antiseptic, antioxidant, anti-cancer and anti-viral properties. Nimbin is promising for research of neurodegenerative diseases and viral infections.

Mianserin-d3 is the deuterium labeled Mianserin (HY-B0188). 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.

Acitazanolast is an orally active antiallergic agent, can inhibit histamine release. Acitazanolast can be used in study of type I anaphylaxis (immediate) caused by IgE antibodies.