Histamine Receptor Inhibitor

Buclizine (dihydrochloride) (Standard) is the analytical standard of Buclizine (dihydrochloride). This product is intended for research and analytical applications. Buclizine dihydrochloride is an orally active antihistamine antiallergic compound. Buclizine dihydrochloride is a potent teratogen in the rat and shows anti-tumor activity.

Doxylamine succinate (Standard) is the analytical standard of Doxylamine succinate (HY-A0069). This product is intended for research and analytical applications. 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.

Impentamine dihydrobromide (VUF 4702 dihydrobromide) is a histamine H3 receptor antagonist with potential antihistamine activity. Impentamine dihydrobromide shows the strongest selective H3 antagonism among a series of 4(5)-(ω-aminoalkyl)-1H-imidazole compounds. The pA2 value of impentamine dihydrobromide is 8.4, showing its high efficacy in guinea pig jejunum. Impentamine dihydrobromide has a specific antagonistic binding site with the H3 receptor.

Phenyltoloxamine (Bistrimin) is an antihistamine agent with sedative and analgesic effects. Phenyltoloxamine also has potent Sigma-1 receptor binding affinity (K_i: 160 nM).

Pheniramine-d₆ (maleate) is the deuterium labeled Pheniramine maleate. Pheniramine Maleate ia an antihistamine and vasoconstrictor.

Dexchlorpheniramine (maleate) (Standard) is the analytical standard of Dexchlorpheniramine (maleate). This product is intended for research and analytical applications. Dexchlorpheniramine maleate is an antihistamine with anticholinergic properties used in the study of allergic diseases.

Dimephosphon is an anti-inflammatory agent with antihistamine and antiserotonin activities. Dimephosphon helps maintain the conduction function of the spinal cord and reduces the excitability of spinal motor neurons in the area surrounding the lesion. Dimephosphon directly activates lymphatic vessel movement and improves lymphatic circulation. Dimephosphon can be used for the study of inflammatory edema, acute spinal cord injury and lymphatic circulation disorders.

UK-9040, a derivative of the antihistamine Triprolidine (HY-B1808), is an orally active inhibitor of gastric secretory. UK-9040 reduces gastric acid, pepsin, and volume output in response to food, Insulin (HY-P0035), Histamine (HY-B1204), N-methyl histamine, and Pentagastrin (HY-A0261).

Norzotepine is the major human metabolite of Zotepine (HY-103093) and also a NET inhibitor (human IC₅₀ = 4.2 nM). Norzotepine exerts antipsychotic-like and antidepressant-like effects by inhibiting Norepinephrine (HY-13715) reuptake and blocking dopamine D₂ (Dopamine D₂), histamine H₁ (Histamine H₁), and 5-HT₂ receptors. Norzotepine can be used for research on schizophrenia.

KY 234 is an orally effective inhibitor that targets thromboxane A2 production, with an IC₅₀ of 5 μM. KY 234 significantly inhibits leukotriene D4 (LTD4), histamine, and antigen-induced bronchoconstriction in guinea pigs, with IC₅₀ values of 6.0 mg/kg, 2.5 mg/kg, and 6.3 mg/kg, respectively.

Hetramine is a compound with antihistamine and antiallergic activity that prevents histamine-induced intestinal contractions as well as allergy and anaphylactic shock in guinea pigs.

ONO-8809 is a Thromboxane A2 receptor antagonist. ONO-8809 inhibits the LTC4-induced airway hyperresponsiveness to histamine in a dose-dependent manner.

HDAC6-IN-49 (Compound 3) is an inhibitor for HDAC with IC₅₀ of 0.012 and 0.735 μM for HDAC6 and HDAC1. HDAC6-IN-49 also exhibits inhibitory activities against MAO-B, cholinesterase (ChE), histamine receptor (H3R) and serotonin 6 receptor (5-HT6R). HDAC6-IN-49 exhibits neuroprotective efficacy on SH-SY5Y cell. HDAC6-IN-49 improves cognitive function and locomotor ability in Drosophila Parkinson's disease models and in C. elegans Alzheimer's disease models.

Perphenazine-d₈ (dihydrochloride) is the deuterium labeled Perphenazine, which is a typical antipsychotic agent(5-HT, Dopamine receptor ligand).

Arbortristoside A is an orally active inhibitor of prostaglandin (prostaglandin), histamine (histamine) and serotonin (serotonin). Arbortristoside A mediates anti-inflammatory, analgesic, anti-allergic, immunomodulatory, antiviral and anti-ulcerogenic effects, and also exhibits in vitro anticancer activity. Arbortristoside A can be used in research related to human hepatocellular carcinoma, breast cancer, fibrosarcoma, leishmaniasis, allergic diseases, viral infections and gastric ulcers.

(R)-Azelastine is an antihistamine compound with antiallergic activity. (R)-Azelastine can downregulate the levels of H1R, M1R, and M3R. (R)-Azelastine has also been shown to inhibit the proliferation of HNEpC.

Azapetine hydrochloride 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 hydrochloride functionally blocks postsynaptic α₁-adrenoceptors, and at higher concentrations, it blocks presynaptic α₂-adrenoceptors, central α-adrenoceptors, and H₂ histamine receptors. Azapetine hydrochloride is used in related research on hypotension.

Ritanserin (Standard) is the analytical standard of Ritanserin. This product is intended for research and analytical applications. Ritanserin (R 55667) is a highly potent, relatively selective, orally active, long acting antagonist of 5-HT2 receptor, with an IC50 of 0.9 nM, less active on Histamine H1, Dopamine D2, Adrenergic α1, Adrenergic α2 receptors.

Ketotifen-d₃ (HC 20-511-d₃) is deuterium labeled Ketotifen. Ketotifen (HC 20-511) is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention.

VUF-6884 (Compound 7j) is a histamine receptor (Histamine Receptor) ligand with activity toward human H4R and H1R. Its pEC₅₀ and pK_i values against human H4R are 7.70 and 7.55, respectively, while those against human H1R are 8.17 and 8.11, respectively. VUF-6884 competitively binds to the orthosteric binding site of human H4R to displace histamine, and exhibits inverse agonist activity at human H1R.