Catalog No.
Product Name
Application
Product Information
Product Citation
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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.- Keisuke Obara, .et al. , Biol Pharm Bull, 2021, 44, 1140-1150
- Azelastine is a potent, second-generation, selective, histamine antagonist (histamine-H1-receptor antagonist).
- 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.
- Chlorpheniramine maleate is a first-generation alkylamine antihistamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticaria.
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H2-receptor antagonist
Cimetidine is a histamine H2-receptor antagonist that inhibits stomach acid production. -
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. - 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.
- Olopatadine hydrochloride is a dual acting histamine H1-receptor antagonist and mast cell stabilizer
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mast cell stabilizer
Nedocromil is a medication considered as mast cell stabilizer which act to prevent wheezing, shortness of breath, and other breathing problems caused by asthma. It is administered by an inhaler under the brand name Tilade. -
H3-receptor antagonist
Ciproxifan maleate is a potent, selective H3 histamine receptor antagonist. -
PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
Histamine Receptor antagonist
Bepotastine Beslilate (Bepreve) is a histamine H1 receptor anatagonist.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Ciproxifan is an extremely potent histamine H3 inverse agonist/antagonist.
- K Yamamoto, .et al. , Naunyn-Schmiedeberg's Arch Pharmacol, 2019, pp 1-12 PMID: 30919010
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nonimidazole inverse agonist
Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM). - 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.
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histamine receptor antagonist
Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM. -
NMDA receptor antagonist
Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker. -
H2 receptor antagonist
Lafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action. - Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H1 receptors.
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COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist - Roxatidine Acetate Hydrochloride is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function in vitro.
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PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
Histamine Antagonist
JNJ7777120 is a potent, selective non-imidazole H4?histamine receptor antagonist.- K Yamamoto, .et al. , Naunyn-Schmiedeberg's Arch Pharmacol, 2019, pp 1-12 PMID: 30919010
- Yamamoto K, .et al. , Neurosci Lett, 2018, May 29;676:103-107 PMID: 29655943
- Bepotastine is a non-sedating, selective antagonist of the histamine 1 (H1) receptor.
- Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
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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). -
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). - Lodoxamide is an antiallergic compound acting as a mast-cell stabilizer for the treatment of asthma and allergic conjunctivitis.
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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.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Peptide 401, a potent mast cell degranulating factor from bee venom, suppresses the increased vascular permeability due to intradermal injection of various smooth muscle spasmogens (histamine, and 5-HT).
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Histamine H1 receptor antagonist
Promethazine HCl is a potent histamine H1 receptor antagonist. -
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. -
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. -
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. -
H1 histamine receptor antagonist
Clemizole hydrochloride is an antagonist of H1 histamine receptor with an IC50 value of 8 mM for NS4B RNA binding. -
H2-receptor antagonist
Ebrotidine is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection. -
Nonimidazole inverse agonist
Pitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). -
Nonimidazole inverse agonist
Pitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). - Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
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histamine-H1 receptor blocking agent
Carbinoxamine maleate is a histamine-H1 receptor blocking agent with antihistamine and anticholinergic properties. -
Histamine H1-receptor agonist
Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent. -
serotonin/histamine2 antagonist
Cyproheptadine hydrochloride sesquihydrate is an antihistamine and is an antagonist of serotonin and histamine2. -
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. -
Histamine H1 receptor inhibitor
Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine.
