Histamine Receptor Inhibitor

Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area.

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.

C-Type Natriuretic Peptide (CNP) (1-22), human, a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor.

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

Cinnarizine is an orally active, effective and selective inhibitor of L-type calcium channel Cav1.3 with an IC₅₀ of 1.5 μM (in vestibular hair cells). Cinnarizine can cross the blood-brain barrier and regulate calcium homeostasis and dopamine neurotransmission. Cinnarizine inhibits the influx of calcium ions into smooth muscle cells by blocking L-type calcium channels, thereby relaxing vascular smooth muscle, improving cerebral circulation and reducing blood viscosity, while antagonizing dopamine receptors. Cinnarizine can be used in the study of vestibular vertigo, Meniere's disease and cerebrovascular diseases.

C-Type Natriuretic Peptide (CNP) (1-22), human (TFA),a 1-22 fragment of CNP, is a natriuretic peptide receptor B (NPR-B) agonist. C-Type Natriuretic Peptide (CNP) (1-22), human (TFA) inhibits cAMP synthesis stimulated by the physiological agonists histamine and 5-HT or directly by Forskolin. CNP is a potent, endothelial-derived relaxant and growthinhibitory factor.

Lodoxamide (U-42585E free acid) is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.

Spinacetin is a natural product that can be isolated from Inula japonica. Spinacetin inhibits the release of histamine. Spinacetin has anti-inflammatory activity.

Dexchlorpheniramine maleate is an orally taken anti-histamine that has anti-inflammatory, anti-irritant, anti-allergic, and skin barrier effects. Dexchlorpheniramine maleate inhibits myocardial contraction in rats. Dexchlorpheniramine maleate can be used in studies of allergic rhinitis.

Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.

Azacyclonol (γ-pipradol), a metabolite of Terfenadine, is a central depressant agent. Azacyclonol is a ganglion-blocking agent. Azacyclonol can be used to diminish psychoses-induced hallucinations.

Lodoxamide tromethamine (U-42585E) is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.

XmAb-7195 (AIMab-7195) is a human monoclonal antibody (mAb) targeting IGHE. XmAb-7195 can be used in Food hypersensitivity, Allergic asthma, Allergic rhinitis, Atopic dermatitis and Conjunctivitis research.

Antazoline hydrochloride is a histamine H1 receptor antagonist with anticholinergic and antiviral properties. Antazoline hydrochloride can prevent histamine from acting on target cells through a reversible competition effect on histamine receptor sites of these cells. Antazoline hydrochloride can exert an antiallegic effect and prevent the occurrence of physiological reactions from the effect of blocking as well as inhibiting H1 receptor. Antazoline hydrochloride can effectively reduce HBV DNA in the extracellular supernatant in a dose-dependent manner, with EC₅₀ of 2.910 μmol/L in HepAD38 cells. Antazoline hydrochloride also has a significant inhibitory effect on HBV DNA in the extracellular supernatant of Huh7 cells (EC₅₀ = 2.349 μmol/L). Antazoline hydrochloride has anti-arrhythmic effect in acute myocardial infarctions. Antazoline hydrochloride can be studied in research for cardiovascular diseases, and HBV.

Dothiepin (Dosulepin; Dothep) is an antidepressant agent with sedative/anxiolytic activity. Dothiepin is an inhibitor preferring of noradrenaline uptake than serotonin uptake. Dothiepin facilitates noradrenergic neurotransmission via inhibiting the neuronal uptake. Dothiepin is also an antagonist of histamine H1-receptor without cardiotoxicity. Dothiepin exhibits significant analgesic activity in psychogenic facial pain，idiopathic fibromyalgia syndrome or rheumatoid arthritis.

Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma.

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.

Buclizine dihydrochloride is an orally active antihistamine antiallergic compound. Buclizine dihydrochloride is a potent teratogen in the rat and shows anti-tumor activity.

Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.

Marmin is a histamine receptor inhibitor and tracheal smooth muscle relaxant. Marmin antagonizes histamine- and methacholine-induced contraction of tracheal smooth muscle. Marmin inhibits histamine release from mast cells, and also blocks extracellular calcium influx via voltage-dependent calcium channels as well as calcium release from intracellular calcium stores, thereby effectively inhibiting calcium-mediated smooth muscle contraction. Marmin slightly enhances the relaxant effect of isoprenaline, and induces epithelial-dependent tracheal smooth muscle relaxation independent of nitric oxide, cGMP or β₂-adrenergic pathways through the release of prostaglandin E₂.