Histamine Receptors
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Decloxizine
Catalog No. A20964 histamine 1 receptor antagonistDecloxizine(UCB-1402; NSC289116) is a histamine 1 receptor antagonist. Learn More -
GSK189254A
Catalog No. A22005 histamine H3 receptor antagonistGSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively. Learn More -
Niperotidine
Catalog No. A21981 histamine H2-receptor antagonistNiperotidine is a histamine H2-receptor antagonist. Learn More -
JNJ-5207852
Catalog No. A21480 histamine H3 receptor antagonistJNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively. Learn More -
PF-03654746 Tosylate
Catalog No. A21434 histamine H3 receptor antagonistPF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. Learn More -
PF-03654746
Catalog No. A21429 histamine H3 receptor antagonistPF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration. Learn More -
Toreforant
Catalog No. A21058 histamine H4 receptor (H4R) antagonistToreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM. Learn More -
Chlorcyclizine hydrochloride
Catalog No. A18025 histamine H1 antagonistChlorcyclizine hydrochloride is a histamine H1 antagonist. Learn More -
H4 Receptor antagonist 1
Catalog No. A18929 histamine H4 receptor inverse agonistH4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM. Learn More -
Buclizine HCl
Catalog No. A15666 Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family. Learn More -
Ebrotidine
Catalog No. A15075 H2-receptor antagonistEbrotidine is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection. Learn More -
Cyproheptadine hydrochloride
Catalog No. A16169 serotonin/histamine2 antagonistCyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2. Learn More -
Lidocaine hydrochloride
Catalog No. A16132 Histamine H1-receptor agonistLidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent. Learn More -
CarbinoxaMine Maleate
Catalog No. A16129 histamine-H1 receptor blocking agentCarbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties. Learn More -
Bavisant dihydrochloride hydrate
Catalog No. A15016 H3 receptor antagonistBavisant 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. Learn More -
Bavisant dihydrochloride
Catalog No. A15015 H3 receptor antagonistBavisant 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. Learn More -
Zaltidine
Catalog No. A15285 H2-receptor antagonistZaltidine is a H2-receptor antagonist, which has the antisecretory action. Learn More -
Pitolisant oxalate
Catalog No. A15214 Nonimidazole inverse agonistPitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). Learn More -
Pitolisant hydrochloride
Catalog No. A15213 Nonimidazole inverse agonistPitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). Learn More -
Clemizole hydrochloride
Catalog No. A15047 H1 histamine receptor antagonistClemizole hydrochloride is an antagonist of H1 histamine receptor with an IC50 value of 8 mM for NS4B RNA binding. Learn More -
Alcaftadine
Catalog No. A16393 H1 histamine receptor antagonistAlcaftadine 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. Learn More -
Antazoline HCl
Catalog No. A16411 Histamine H1 receptor inhibitorAntazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. Learn More -
Azatadine dimaleate
Catalog No. A16418 Histamine/cholinergic inhibitorAzatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. Learn More -
Cyclizine 2HCl
Catalog No. A16472 Histamine H1 receptor antagonistCyclizine 2HCl is a piperazine derivative with Histamine H1 receptor antagonist activity. Learn More -
Terfenadine
Catalog No. A17373 H1 histamine receptor antagonistTerfenadine ((??)-Terfenadine) is a potent open-channel blocker of hERG with an IC50 of 204 nM. Terfenadine, an H1 histamine receptor antagonist, acts as a potent apoptosis inducer in melanoma cells through modulation of Ca2+ homeostasis. Terfenadine induces ROS-dependent apoptosis, simultaneously activates Caspase-4, -2, -9 and induces p73, Noxa. Learn More -
Levocetirizine Dihydrochloride
Catalog No. A17440 Histamine H1 receptor antagonistLevocetirizine dihydrochloride is a L-isomer of cetirizine and histamine H1 receptor antagonist. It incrases levels of CD4+ CD25+ T cells and decreases levels of eosinophils, decreasing allergy symptoms. Learn More -
Hydroxyzine pamoate
Catalog No. A17712 Histamine H1 receptor antagonistHydroxyzine pamoate is an histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. Learn More -
Diphenylpyraline hydrochloride
Catalog No. A17717 antihistamineDiphenylpyraline hydrochloride is a first-generation antihistamine with anticholinergic effects of the diphenylpiperidine class. Learn More -
Acrivastine
Catalog No. A17746 Histamine 1 receptor antagonistAcrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis. Learn More -
Mebhydrolin napadisylate
Catalog No. A17997 histamine H1-receptor antagonistDiazoline is a histamine H1-receptor antagonist. Learn More -
Mequitazine
Catalog No. A18206 Histamine H1 antagonistMequitazine is a potent histamine H1 antagonist or antihistamine. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract. Learn More -
Rupatadine
Catalog No. A11222 PAFR inhibitor/H1 receptor inhibitorRupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. Learn More -
Azelastine HCl (Allergodil)
Catalog No. A10117 Azelastine is a potent, second-generation, selective, histamine antagonist (histamine-H1-receptor antagonist). Learn More -
Brompheniramine
Catalog No. A11699 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. Learn More -
Clemastine fumarate
Catalog No. A10226 Histamine Receptor antagonisClemastine 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. Learn More -
Ciproxifan
Catalog No. A11360 Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist. Learn More -
Cyproheptadine hydrochloride
Catalog No. A11709 Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM. Learn More -
Orphenadrine citrate
Catalog No. A11712 NMDA receptor antagonistOrphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. Learn More -
Lafutidine
Catalog No. A11714 H2 receptor antagonistLafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action. Learn More -
Mizolastine
Catalog No. A11724 Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H1 receptors. Learn More -
Asenapine maleate
Catalog No. A10091 H1 antagonistAsenapine 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. Learn More -
Cetirizine Dihydrochloride
Catalog No. A10195 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. Learn More -
Chlorpheniramine maleate
Catalog No. A10205 Chlorpheniramine maleate is a first-generation alkylamine antihistamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticaria. Learn More -
Cimetidine
Catalog No. A10218 H2-receptor antagonistCimetidine is a histamine H2-receptor antagonist that inhibits stomach acid production. Learn More -
Bepotastine Besilate
Catalog No. A11340 Histamine Receptor antagonistBepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist. Learn More -
Roxatidine acetate hydrochloride
Catalog No. A11921 Roxatidine Acetate Hydrochloride is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function in vitro. Learn More -
Rupatadine Fumarate
Catalog No. A12356 PAFR inhibitor/H1 receptor inhibitorRupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. Learn More -
Ciproxifan maleate
Catalog No. A11117 H3-receptor antagonistCiproxifan maleate is a potent, selective H3 histamine receptor antagonist. Learn More -
Loratadine
Catalog No. A10538 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. Learn More -
Fexofenadine HCl
Catalog No. A11859 COX inhibitor/histamine H1 receptor agonistFexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist Learn More