Histamine Receptor Inhibitor

Cyproheptadine hydrochloride (Standard) (Cyproheptadine HCl (Standard)) is the analytical standard of Cyproheptadine hydrochloride (HY-B0366A). This product is intended for research and analytical applications. 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.

LY2624803 is a 5-HT2A and histamine, H1 receptor antagonist.

Gallocatechin-3-O-(3''-O-methyl)-gallate (GCG3''Me) is a catechin polyphenol. Gallocatechin-3-O-(3''-O-methyl)-gallate inhibits histamine release. Gallocatechin-3-O-(3''-O-methyl)-gallate can be used in allergy-related studies.

Quifenadine hydrochloride is an H1-histamine receptor blocker and can be used in the research of anti-arrhythmia.

Benztropine-¹³C,d₃ (mesylate) is the ¹³C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects.

Undecane-d₂₄ is the deuterium labeled Undecane (HY-N8593).Undecane is a potent cAMP agonist with anti-allergic and anti-inflammatory activities. Undecane inhibits degranulation and the secretion of histamine and TNF-α. Undecane reverses the increased levels of p38 phosphorylation, NF-κB transcriptional activity and target cytokine/chemokine genes, including thymus and activation-regulated chemokine (TARC), macrophage-derived chemokine (MDC) and interleukin-8 (IL-8). Undecane can be used for the study of skin inflammatory disorders, such as atopic dermatitis.

Aceprometazine (1664CB) is an orally active antipsychotic. Aceprometazine can be used in the study of psychiatric disorders, such as depression.

Fenethazine (Phenethazine) is a compound with antihistamine activity. It is an effective antihistamine. Its congeners also have anticholinergic effects and can be used to inhibit Parkinson's disease.

Eukovoside is a cinnamic acid derivative found in Euphrasia regelii with anti-inflammatory, antioxidant, antibacterial, antiallergic, and antihistamine activity. Eukovoside can be used for the research of hyperglycemic diseases, eye inflammation, upper respiratory passages inflammation, hay fever, conjunctivitis, colds, influenza, sinusitis.

(R)-Azelastine hydrochloride, an antihistamine, has been demonstrated to down-regulate the levels of H1R, M1R, and M3R, while also inhibiting the proliferation of HNEpC.

Linadryl is a compound with antihistamine and other effects. It has a variable effect on gastric acid secretion after oral administration, and its effect is about half that of Diphenhydramine (HY-B0303).

Contilisant is a permeable antioxidant and neuroprotectant agent. Contilisant exhibits high nM affinity at H3R. Contilisant inhibits monoamine oxidases and cholinesterases. Contilisant has a binding affinity of 65.23 nM towards hS1R. Contilisant can significantly restore cognitive deficit induced by Aβ_1-42 in the radial maze assay of Alzheimer’s animal model.

Alloclamide is a competitive antihistamine compound targeting the H₁ histamine receptor. Alloclamide‘s core regulatory mechanism involves competitive binding to the H₁ histamine receptor, blocking the activation of the receptor by histamine molecules and inhibiting various allergy-related biological responses mediated by histamine. Alloclamide can be used in allergy-related research.

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

4-AcO-DALT hydrochloride is a tryptamine compound with psychoactive effects. 4-AcO-DALT hydrochloride inhibits 5-HT receptors, alpha receptors, dopamine receptors, histamine receptor 1 (H1), muscarinic M2 receptor and Sigma 2 receptor. 4-AcO-DALT hydrochloride shows K_i values of 582 nM, 2689 nM, 2099 nM, 2116 nM, 958 nM, 137 nM, 824 nM, 479 nM, 406 nM, 874 nM, 4190 nM, 482 nM, 214 nM, 803 nM, 4522 nM, 1907 nM for 5-HT1B, 5-HT1D, 5-HT1E, 5-HT2A, 5-HT2B, 5-HT2C, 5-HT6, 5-HT7A, H1, Sigma 2, α2A, α2B, α2C, D2, D3 receptors.

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

RS-51324 is an oral active antidepressant agent. RS-51324 inhibitts norepinephrine uptake and reverses of Reserpine (HY-N0480)-induced hypothermia.

Quinotolast is an orally active antiallergic agent. Quinotolast inhibits histamine release from rat peritoneal cells. Quinotolast inhibits cutaneous cromoglycate in guinea pig model. Quinotolast has inhibitory effect on histamine and peptide leukotrienes release from guinea pig lung fragments and mouse cultured mast cells. Quinotolast can be studied in allergy-related research.

SUN-1334H free base is an orally active inhibitor for histamine H1 receptor, with an IC₅₀ of 20.3 nM and K_i of 9.7 nM. SUN-1334H free base inhibits histamine-induced contractions of isolated guinea-pig ileum with an IC₅₀ of 0.198 μM. SUN-1334H free base inhibits histamine-induced bronchoconstriction in guinea pigs, histamine-induced skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs.

Rocastine fumarate (AHR-11325 fumarate) is an orally active H₁-histamine receptor inhibitor that selectively binds to and functionally inhibits H1-histamine receptors. Rocastine fumarate protects guinea pigs from the lethal effect induced by Histamine (HY-B1204), prevents histamine-induced collapse, and protects guinea pigs from the falling reaction induced by nebulized antigens. Rocastine fumarate can be used in the research of allergic diseases.