Histamine Receptor Inhibitor

Pitolisant (Standard) is the analytical standard of Pitolisant. This product is intended for research and analytical applications. Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).

Cyproheptadine (Standard) is the analytical standard of Cyproheptadine (HY-B1622). This product is intended for research and analytical applications. Cyproheptadine acts as a p38 MAP kinase activator, CHK2 activator, histamine H1 receptor inhibitor and serotonin receptor inhibitor. Cyproheptadine 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 induces Apoptosis by increasing PARP and cleaved PARP, as well as activating the mitochondrial caspase pathway. Cyproheptadine inhibits tumor growth with extremely low toxicity to normal cells. Cyproheptadine can be used in research related to hepatocellular carcinoma, multiple myeloma and acute myeloid leukemia.

Repirinast (Standard) is the analytical standard of Repirinast (HY-109544). This product is intended for research and analytical applications. Repirinast (MY-5116) is an orally active anti-allergic agent. Repirinast inhibits histamine release. Repirinast can be used in the research of bronchial asthma.

Azapetine phosphate is an antagonist of α₁-adrenoceptor, with an IC₅₀ of 0.205 μM at rat α₁-adrenoceptor and an IC₅₀ of 1.3 μM at rat α₂-adrenoceptor, and exhibits higher selectivity for α₁-adrenoceptor than for α₂-adrenoceptor. Azapetine phosphate functionally blocks postsynaptic α₁-adrenoceptors, and at higher concentrations, it blocks presynaptic α₂-adrenoceptors, central α-adrenoceptors, and H₂ histamine receptors. Azapetine phosphate is used in related research on hypotension.

FR-A-19 is a potent histamine H2-agonist with IC₅₀ values of 0.02, 0.015, and 0.008 μM targets arpromidine, BUA-75, and FRA-19 respectively. FR-A-19 has potent anti-allergic properties.

Dimenhydrinate (Standard) is the analytical standard of Dimenhydrinate. This product is intended for research and analytical applications. Dimenhydrinate is an orally active H1-antihistamine consisting of Diphenhydramine (HY-B0303) and 8-Chlorotheophylline. Dimenhydrinate is used to prevent nausea, vomiting, dizziness, and vertigo associated with motion sickness.

Dioxopromethazine hydrochloride (Standard) is the analytical standard of Dioxopromethazine hydrochloride. This product is intended for research and analytical applications. Dioxopromethazine is an orally active antihistamine. Dioxopromethazine inhibits asthmatic symptoms and can be used for relevant research.

Cyprolidol is an orally active inhibitor of acetylcholine receptor and histamine receptor with potential antidepressant activity. Cyprolidol inhibits acetylcholine-induced hypotensive response, histamine-induced systolic blood pressure decrease, tyramine-induced systolic blood pressure increase, serotonin-induced systolic blood pressure response in anesthetized animals, and bretylium-induced systolic blood pressure increase in anesthetized cats. Cyprolidol potentiates norepinephrine-induced systolic blood pressure increase, slightly potentiates epinephrine-induced systolic blood pressure increase, and enhances the anesthetic depth of barbiturates. Cyprolidol can be used in the research of depression.

CI-624 decrease secretion volumes and outputs of hydrogen, sodium and potassium ions and of pepsin. CI-624 can be used in the research of cancer and autoimmune diseases.

Bromodiphenhydramine (hydrochloride) (Standard) is the analytical standard of Bromodiphenhydramine (hydrochloride). This product is intended for research and analytical applications. 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.

Acrivastine (Standard) is the analytical standard of Acrivastine. This product is intended for research and analytical applications. Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.

Cinnarizine (Standard) is the analytical standard of Cinnarizine. This product is intended for research and analytical applications.

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

Lodoxamide (tromethamine) (Standard) is the analytical standard of Lodoxamide (tromethamine). This product is intended for research and analytical applications. Lodoxamide tromethamine (U-42585E) is a medication for the treatment of prophylaxis of mast cell-mediated allergic disease.

Clemizole penicillin is a composite preparation containing two active components, Clemizole (HY-30234) and penicillin, with antihistamine, anti-inflammatory, and bactericidal activities. The Clemizole component of Clemizole penicillin targets the H₁ receptor, CrtN, and TRPC5 calcium channel, while penicillin exerts antibacterial effects. The clemizole contained in Clemizole penicillin acts as a reversible competitive inhibitor of the TRPC5 calcium channel; it also competitively targets the CrtN enzyme of Staphylococcus aureus to block staphyloxanthin biosynthesis. Clemizole penicillin can be used in research on lobar pneumonia and syphilis.

Lodoxamide (Standard) is the analytical standard of Lodoxamide. This product is intended for research and analytical applications. Lodoxamide (U-42585E free acid) is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.

Psoralenoside is a benzofuran glycoside from Psoralea corylifolia. Psoralenoside exhibits high binding affinities against histaminergic H1, calmodulin, and voltage-gated L-type calcium channels (E-value≥-6.5 Kcal/mol). Psoralenoside shows estrogen-like activity, osteoblastic proliferation accelerating activity, antitumor effects and antibacterial activity.

Levodropropizine-d₅ ((S)-(-)-Dropropizine-d₅) is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is an orally active histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.

Pitolisant-d₆ (Tiprolisant-d₆) 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).

Chlorphenoxamine (Standard) is the analytical standard of Chlorphenoxamine (HY-B1607). This product is intended for research and analytical applications. 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.