Histamine Receptor Inhibitor

AHR-13268D is an oral active antiallergic and antihistaminic agent, with bioavailable approximately 88%. AHR-13268D is a potent inhibitor of histamine release from rat peritoneal mast cells, with the IC₅₀ of 0.51 nM.

Chloracyzine is an antianginal agent with spasmolytic properties and prevent or relieve spasms of the coronary vessels. Chloracyzine shows a moderate antihistaminic effect.

Cyproheptadine-d₃ is the d₃-labeled Cyproheptadine (HY-B1622). 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.

Mifentidine (DA 4577) is a potent and selective H2 Receptor antagonist. Mifentidine has an anti-secretion effect and can antagonize the acid-promoting activity of histamine with EC₅₀ 3.28 μM.

Dihexyverine hydrochloride is a compound belonging to the amino alcohol ester class. Dihexyverine hydrochloride possesses anticholinergic, smooth muscle relaxant, antihistaminic, and antiemetic effects. Dihexyverine hydrochloride can also shorten the duration of labor. Dihexyverine hydrochloride can be used in research related to gastrointestinal spasms, obstetrics, and other fields.

Levodropropizine-d₈ is deuterium labeled Levodropropizine. Levodropropizine (DF-526) is a histamine receptor inhibitor, Levodropropizine is an effective and very well tolerated peripheral antitussive agent.

Pheniramine (maleate) (Standard) is the analytical standard of Pheniramine (maleate). This product is intended for research and analytical applications. Pheniramine (Prophenpyridamine; Tripoton) maleate is a first-generation histamine H1 receptor antagonist, acts on the central nervous system (CNS) with sedative and hypnotic effect. Pheniramine maleate displays antitumor effect and induces leukemia cells apoptosis. Pheniramine maleate is also a safe and effective local agent that can suppress or relieve pain, with antipruritic effects.

Cassiaside C2 is a naphthopyrone with a strong antiallergic activity. Cassiaside C2 inhibits the histamine release from rat peritoneal exudate mast cells induced by antigen-antibody reaction.

AZD3778 (Compound 8) is an inhibitor of CCR3 and histamine H1 receptor (histamine H1 receptor), with IC₅₀ values of 8.1 nM and 40 nM, respectively. AZD3778 inhibits the binding of eosinophil chemokines to CCR3, as well as the binding of histamine to histamine H1 receptor. AZD3778 exhibits anti-eosinophilic activity. AZD3778 alleviates symptoms associated with allergic rhinitis. AZD3778 can be used in research related to allergic rhinitis and asthma.

Hydroxydione has an effect of general anesthetic. Hydroxydione is a neuroactive steroid it can be used for anaesthesia related research.

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

REV 2871 (Eclazolast; CHBZ) is a potent and oral activity antiallergic agent. REV 2871 also is an irreversibility histamine release (HR) inhibitor.

AM-0466 is a sodium channel inhibitor with nanomolar levels of NaV1.7 inhibitory activity. AM-0466 exhibits potent pharmacodynamic activity in a NaV1.7-dependent histamine-induced itch model. AM-0466 also showed significant analgesic effects in capsaicin-induced pain models. After optimizing its pharmacokinetic properties, AM-0466 was advanced into in vivo targeting and efficacy models for testing.

Fexofenadine-d₁₀ (hydrochloride) is deuterium labeled Fexofenadine (hydrochloride). Fexofenadine hydrochloride (MDL-16455 hydrochloride), a H1R antagonist, is an anti-allergic agent used in seasonal allergic rhinitis and chronic idiopathic urticarial (person aged ≥16 years).

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

(Z)-Olopatadine-d₃ (hydrochloride) is deuterium labeled Olopatadine (hydrochloride).

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

Ketotifen-¹³C,d₃ is deuterium labeled Ketotifen.

H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC₅₀ of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ_1-42 induced by itself and Cu²⁺ (95.48% and 88.63%) , and degraded the Aβ_1-42 fibrils induced by itself and Cu²⁺ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu²⁺, Zn²⁺, Al³⁺, and Fe²⁺. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ_1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .

AVN-101 is a potent, brain-penetrant and orally active 5-HT7 receptor antagonist (K_i of 153 pM), with slightly lesser potency toward 5-HT6, 5-HT2A, and 5HT-2C receptors (K_i values of 2.04 nM, 1.56  nM, and 1.17  nM, respectively). AVN-101 also exhibits a rather high affinity toward histamine H1 (K_i of 0.58 nM) and adrenergic α2A, α2B, and α2C (K_i= 0.41-3.6 nM) receptors. AVN-101 can be studied in such diseases as general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis.