Histamine Receptors



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Catalog No. Product Name Application Product Information
A16472

Cyclizine 2HCl

Histamine H1 receptor antagonist
Cyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity.
A15075

Ebrotidine

H2-receptor antagonist
Ebrotidine is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection.
A15047

Clemizole hydrochloride

H1 histamine receptor antagonist
Clemizole hydrochloride is an antagonist of H1 histamine receptor with an IC50 value of 8 mM for NS4B RNA binding.
A15041

Cetirizine

H1-receptor antagonist
Cetirizine, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.
A14946

Ebastine

H1-histamine receptor antagonist
Ebastine is a H1 antihistamine with low potential for causing drowsiness.
A13442

A 943931 2HCl

Histamine H4 receptor antagonist
A 943931 2HCl is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively).
A13641

Immethridine hydrobromide

histamine H3 receptor agonist
Immethridine hydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively).
A13899

Astemizole

H1-receptor antagonist
Astemizole is a potent antihistamine (H1-receptor antagonist, IC50 = 4 nM) that displays selectivity over dopamine, 5-HT, and muscarinic acetylcholine receptors. This compound has shown potent hERG K+ channel blocking activity (IC50 = 0.9 nM), antimalarial activity in multidrug resistant strains in vitro (IC50 = 227 - 734 nM), and has been used as a chaperone to correct folding defects and restore protein function for some mutated forms of hERG channels.
A14248

Promethazine HCl

Histamine H1 receptor antagonist
Promethazine HCl is a potent histamine H1 receptor antagonist.
A12713 SALE

JNJ7777120

Histamine Antagonist
JNJ7777120 is a potent, selective non-imidazole H4?histamine receptor antagonist.
A15213

Pitolisant hydrochloride

Nonimidazole inverse agonist
Pitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
A15214

Pitolisant oxalate

Nonimidazole inverse agonist
Pitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
A15285

Zaltidine

H2-receptor antagonist
Zaltidine is a H2-receptor antagonist, which has the antisecretory action.
A16418

Azatadine dimaleate

Histamine/cholinergic inhibitor
Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively.
A16411

Antazoline HCl

Histamine H1 receptor inhibitor
Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine.
A16393

Alcaftadine

H1 histamine receptor antagonist
Alcaftadine is a high affinity ligand for the H1 receptor, with a pKi (8.5) that is comparable with that of other H1 antihistamines. Alcaftadine is also an antagonist for H2 and H4 receptors with no affinity for the H3 receptor.
A15666

Buclizine HCl

-
Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
A16169

Cyproheptadine hydrochloride

serotonin/histamine2 antagonist
Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2.
A16132

Lidocaine hydrochloride

Histamine H1-receptor agonist
Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.
A16129

CarbinoxaMine Maleate

histamine-H1 receptor blocking agent
Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties.
A15016

Bavisant dihydrochloride hydrate

H3 receptor antagonist
Bavisant dihydrochloride hydrate is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
A15015

Bavisant dihydrochloride

H3 receptor antagonist
Bavisant dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD.
A13086

Metiamide

Histamine H2-receptor antagonist
Metiamide is a histamine H2-receptor antagonist developed from another H2 antagonist, burimamide. It was an intermediate compound in the development of the successful anti-ulcer drug cimetidine.
A13073

Clemizole

H1 histamine receptor antagonist.
Clemizole is an H1 histamine receptor antagonist.
A10091 SALE

Asenapine maleate

H1 antagonist
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.
A11724

Mizolastine

-
Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H1 receptors.
A11714

Lafutidine

H2 receptor antagonist
Lafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action.
A11712 SALE

Orphenadrine citrate

-
Orphenadrine is known to have the following pharmacology: mACh receptor antagonist (anticholinergic); H1 receptor antagonist (antihistamine); NMDA receptor antagonist; NET blocker (norepinephrine reuptake inhibitor); Nav1.7, Nav1.8, and Nav1.9 sodium channel blocker; HERG potassium channel blocker.
A11709 SALE

Cyproheptadine hydrochloride

-
A11360

Ciproxifan

-
Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist.
A10226 SALE

Clemastine fumarate

Histamine Receptor antagonis
Clemastine is a selective histamine H1 antagonist. It binds to the histamine H1 receptor, thus blocking the action of endogenous histamine, which leads to temporary relief of the negative symptoms caused by histamine.
A11699 SALE

Brompheniramine

-
Brompheniramine is a first-generation antihistamine. Brompheniramine works by acting as an antagonist of histamine H1 receptors. It also functions as a moderately effective anticholinergic agent, and is likely an antimuscarinic agent similar to other common antihistamines such as diphenhydramine.
A10117 SALE

Azelastine HCl (Allergodil)

-
Azelastine is a potent, second-generation, selective, histamine antagonist (histamine-H1-receptor antagonist).
A10195 SALE

Cetirizine Dihydrochloride

-
Cetirizine is a second-generation antihistamine, a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.
A10205 SALE

Chlorpheniramine maleate

-
Chlorpheniramine maleate is a first-generation alkylamine antihistamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticaria.
A10218

Cimetidine

H2-receptor antagonist
Cimetidine is a histamine H2-receptor antagonist that inhibits stomach acid production.
A10671

Olopatadine hydrochloride

-
Olopatadine hydrochloride is a dual acting histamine H1-receptor antagonist and mast cell stabilizer
A12845

Bepotastine

-
Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor.
A12661

Bilastine

-
Bilastine is a novel, nonsedating H1-antihistamine developed for symptomatic treatment of allergic rhinitis and chronic idiopathic urticaria.
A11859 SALE

Fexofenadine HCl

COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist
A10538

Loratadine

-
Loratadine is a non-sedative antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells. Loratadine is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
A11222 SALE

Rupatadine

PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively.
A12356 SALE

Rupatadine Fumarate

PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively.
A11921

Roxatidine acetate hydrochloride

-
Roxatidine Acetate Hydrochloride is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function in vitro.
A11340

Bepotastine Besilate

Histamine Receptor antagonist
Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.
A11117

Ciproxifan maleate

H3-receptor antagonist
Ciproxifan maleate is a potent, selective H3 histamine receptor antagonist.

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