Histamine Receptor Inhibitor

Propiomazine hydrochloride is an orally active antihistamine agent. Propiomazine hydrochloride 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 hydrochloride is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.

(R)-Meclizine is the enantiomer of Meclizine. Meclizine is an antihistamine agent.

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

Doxylamine-d₅ succinate is deuterium labeled Doxylamine succinate (HY-A0069A). 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.

Propiomazine maleate is an orally active antihistamine agent. Propiomazine maleate 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 maleate is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.

BRL 22321 free base is a stabilizer with similar mast cell stabilizing activity to Cromolyn sodium (HY-B0320A) and also has some smooth muscle relaxant activity. BRL 22321 free base is more potent than Cromolyn sodium (HY-B0320A) in inhibiting rat passive cutaneous and peritoneal anaphylaxis and antigen-induced histamine release from passively sensitized rat peritoneal cells.

Loratadine n-oxide is a metabolite of Loratadine. Loratadine n-oxide shows antihistamine activity.

Cyproheptadine hydrochloride-d₃ (Cyproheptadine HCl-d₃) is the d₃-labeled Cyproheptadine (hydrochloride) (HY-B0366A). Cyproheptadine hydrochloride (Cyproheptadine HCl) acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine hydrochloride mediates cell cycle arrest via G1 phase arrest, G1/S transition arrest, G0/G1 phase arrest, reduced expression of cyclins D1/D2/D3, upregulated expression of HBP1, p16, p21, p27, and decreased phosphorylation of retinoblastoma protein. Cyproheptadine hydrochloride induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine hydrochloride inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine hydrochloride can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.

VUF14738 (compound 28) is a bidirectional photoswitch antagonist that can rapidly and reversibly photoisomerize at the histamine H3 receptor, with binding affinity increased or decreased upon illumination, and can be used in real-time electrophysiological experiments to study the activity of dynamic light modulation of receptor activation.

Traxanox is an orally available diuretic that enhances phagocytosis of yeast granules by mouse peritoneal macrophages and rat peritoneal polymorphonuclear leukocytes in vitro. Traxanox inhibits IgE-mediated histamine release and cyclic AMP phosphodiesterase activity.Traxanox exhibits anti-inflammatory activity, as it inhibits the anaphylactoid reaction and reduces pleural fluid accumulation in experimental models of inflammation. Traxanox also demonstrates a synergistic effect when combined with hydrocortisone or indomethacin in suppressing adjuvant arthritis in rats.

Propiomazine-d₆ hydrochloride is deuterium labeled Propiomazine hydrochloride. Propiomazine hydrochloride is an orally active antihistamine agent. Propiomazine hydrochloride 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 hydrochloride is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia.

Tribenoside (Standard) is the analytical standard of Tribenoside. This product is intended for research and analytical applications. Tribenoside is a vasoprotective agent, can be used for the research of hemorrhoids. Tribenoside has mild anti-inflammatory, analgesic, and wound healing properties.

Papaveraldine (Xanthaline) is a benzylisoquinoline alkaloid that shows antispasmodic and protective activity against histamine-induced bronchospasm in rats. Papaveraldine is an active ingredient of a hair tonic preparation that promotes melanin formation for grey hair.

Mequitamium iodide (LG 30435) is an antihistamine drug with antiallergic and bronchodilatory activity. Mequitamium iodide can effectively antagonize airway contraction and inflammatory responses induced by histamine and antigens. Mequitamium iodide has nanomolar affinity for the H1 and smooth muscle receptors of histamine and mequitin. Mequitamium iodide, when administered in aerosol form, significantly inhibits histamine- and antigen-induced increases in airway pressure in allergic mice. Mequitamium iodide reduces antigen-induced eosinophil accumulation in the airways. Mequitamium iodide also exhibits inhibitory effects on PAF-induced platelet aggregation and bronchoconstriction, and can be used in the study of allergic diseases such as rhinitis and asthma.

Dalcotidine (KU-1257) is an orally active and competitive histamine H2 receptor antagonist. Dalcotidine promotes the healing of chronic ulcers and inhibits gastric acid secretion.

Tixanox sodium (RS-7540), an anti-allergic compound, is a potent inhibitor of mediator release in the IgE-mediated passive cutaneous anaphylaxis (PCA) reaction.

Fepradinol is an orally active nonsteroidal anti-inflammatory agent. Fepradinol inhibits the increase in vascular permeability induced by histamine, 5-hydroxytryptamine, and bradykinin, reduces exudate volume, prevents leukocyte migration, and suppresses acute inflammation models. Fepradinol also induces thrombotic vasculopathy with epidermal necrosis, without leukocytoclastic vasculitis; triggers occlusive contact dermatitis presenting as purpuric papulonecrotic lesions, and causes strongly positive patch test reactions. Fepradinol can be used in research related to occlusive contact dermatitis and acute inflammation.

Dibenamine is an alpha-adrenergic antagonist that exhibits the ability to block both basal and histamine-stimulated gastric acid secretion, making it therapeutically relevant in conditions involving excessive gastric acid production.

Nivimedone (BRL 10833 free base) is an orally active antiallergic agent. Nivimedone inhibits IgE-mediated passive cutaneous anaphylaxis in rats. Nivimedone suppresses antigen-induced histamine release from lung tissues passively sensitized with atopic serum. Nivimedone can be used in research related to bronchial asthma.

4'-O-Methylnyasol is an inhibitor of β-hexosaminidase. 4'-O-Methylnyasol inhibits β-hexosaminidase release from rat basophilic leukemia-2H3 cells with an IC₅₀ of 52.67 μM.