Catalog No.
Product Name
Application
Product Information
Citations
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H2-receptor antagonist
Cimetidine is a histamine H2-receptor antagonist that inhibits stomach acid production.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
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Histamine H2-receptor antagonist
Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion.- Jingyeong Shin, .et al. , Chemical Engineering Journal, 2023, December
- 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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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
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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 PMID: 34334499
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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
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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
- 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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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. -
histamine H1 receptor agonist and H3 receptor antagonist
Betahistine EP Impurity C (NSC19005) is an impurity of Betahistine. Betahistine is a potent, orally active and well-tolerated histamine H1 receptor agonist and H3 receptor antagonist used for the study of rheumatoid arthritis (RA). -
antagonist of histamine H1
Cyclizine is an antagonist of histamine H1. Cyclizine is an antihistamine drug that can be used to treat nausea, vomiting and dizziness associated with motion sickness, vertigo and post-operatively following administration of general anaesthesia and opioids. -
Histamine H1 Receptor Antagonist
Epinastine is a selective histamine H1 receptor antagonist, known for its effectiveness as a mast cell stabilizer. It exhibits high affinity for neuronal octopamine receptors in various insects, demonstrating potential roles in modulating immune responses. Epinastine also inhibits pro-inflammatory cytokines such as TARC, IL-8, and IL-4, making it valuable for research into allergic diseases and anti-cancer immunity mechanisms. Its ability to reduce scratching behavior and vascular permeability further underscores its relevance in studying allergic and inflammatory conditions. -
Histamine H1 Receptor Antagonist
Mebhydrolin is a selective antagonist of the histamine H1 receptor, primarily known for its role in mediating allergic responses. This compound exhibits significant antihistaminic activity, making it valuable for research in allergy and immunology. Its effectiveness in blocking histamine-induced physiological effects allows for the exploration of H1 receptor pathways and the development of related therapeutic strategies. -
Stable Isotope
Terfenadine-d3 is the deuterated form of Terfenadine, which primarily targets the hERG potassium channel as a potent open-channel blocker with an IC50 of 204 nM. As an H1 histamine receptor antagonist, Terfenadine-d3 demonstrates significant biological activity by inducing apoptosis in melanoma cells through the modulation of calcium homeostasis. Its mechanism includes the generation of reactive oxygen species (ROS) and the subsequent activation of caspases -4, -2, and -9, making it valuable for research in cancer biology and apoptosis pathways. -
Neurotransmitter
Histamine dihydrochloride acts as an agonist for histamine receptors and functions as a vasodilator. This organic nitrogen compound plays a crucial role in local immune responses and regulates intestinal physiological functions while also serving as a neurotransmitter. Histamine dihydrochloride influences the p38 MAPK/Akt signaling pathway and demonstrates notable antitumor, antioxidant, and anti-inflammatory properties. It is valuable in research applications related to acute myeloid leukemia, malignant melanoma, and renal cell carcinoma. -
Neurotransmitter
Histamine phosphate is an agonist of the histamine receptor and functions as a potent vasodilator. This organic nitrogen compound plays a crucial role in local immune responses, modulates intestinal physiological functions, and serves as a key neurotransmitter. Histamine phosphate influences the p38 MAPK/Akt signaling pathway and demonstrates notable antitumor, antioxidant, and anti-inflammatory activities. It is applicable in research related to acute myeloid leukemia, malignant melanoma, and renal cell carcinoma. -
Neurotransmitter
Histamine is a biogenic amine that acts as an agonist for histamine receptors, playing a significant role as a neurotransmitter. It is involved in local immune responses and the regulation of various physiological functions, including vasodilation. Histamine influences the p38 MAPK/Akt signaling pathway and demonstrates notable antitumor, antioxidant, and anti-inflammatory properties. It is commonly utilized in research related to acute myeloid leukemia, malignant melanoma, and renal cell carcinoma. -
Stable Isotope
Histamine-d4 is a deuterium-labeled derivative of histamine, functioning primarily as a stable isotope for metabolic and pharmacokinetic studies. This compound acts as an agonist at histamine receptors and serves as a notable vasodilator, playing a critical role in local immune responses, intestinal physiological regulation, and neurotransmission. Histamine influences several signaling pathways, including p38 MAPK and Akt, and exhibits diverse biological activities such as anti-inflammatory, antioxidant, and potential antitumor effects. Its applications in research extend to the study of acute myeloid leukemia, malignant melanoma, and renal cell carcinoma, facilitating a deeper understanding of these conditions. -
Stable Isotope
Histamine-13C5 is a stable isotope-labeled form of histamine, primarily functioning as an agonist for histamine receptors. This organic nitrogen compound plays a critical role in local immune responses, modulates intestinal physiological functions, and acts as a neurotransmitter. Histamine influences the p38 MAPK/Akt signaling pathway and demonstrates antitumor, antioxidant, and anti-inflammatory properties. Research applications of Histamine-13C5 include the investigation of conditions such as acute myeloid leukemia, malignant melanoma, and renal cell carcinoma, facilitating deeper insights into these diseases. -
Histamine H2-Receptor Antagonist
Ranitidine hydrochloride is a selective histamine H2-receptor antagonist that effectively inhibits gastric secretion. It demonstrates significant antagonism of histamine-induced cardiac and uterine responses in isolated animal models, with pA2 values of 7.2 and 6.95, respectively. Additionally, ranitidine hydrochloride has been shown to inhibit the development and metastasis of breast tumors in murine models, indicating its potential utility in cancer research. -
Histamine N-Methyltransferase Inhibitor
SKF 91488 dihydrochloride is a potent, noncompetitive inhibitor of histamine N-methyltransferase, exhibiting a Ki value of 0.9 μM. This compound effectively blocks the metabolism of histamine, leading to elevated concentrations of histamine in biological systems. SKF 91488 dihydrochloride plays a significant role in research focusing on infection, inflammation, and cardiovascular diseases, including studies on Mycoplasma pneumonia and hemorrhagic hypotension. Its influence on blood pressure and bronchoconstriction further underscores its utility in exploring related pathophysiological mechanisms. -
H1 Receptor Antagonist
Pheniramine maleate is a first-generation histamine H1 receptor antagonist that primarily targets the central nervous system to produce sedative and hypnotic effects. In addition to its antihistaminic activity, Pheniramine maleate exhibits antitumor properties by inducing apoptosis in leukemia cells. It also demonstrates effectiveness as a local agent to alleviate pain and provide antipruritic effects in various applications. -
Histamine receptors inhibitor
Histamine Receptors Inhibitor 1 (compound 303) functions as an inhibitor of H1 and H4 histamine receptors. This compound demonstrates key biological activity in modulating inflammatory processes and is particularly relevant for research applications focusing on autoimmune, allergic, and ocular conditions. Its ability to selectively inhibit these receptors makes it a valuable tool for investigating histamine-mediated pathways in various biological contexts. -
PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. - 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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PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
nonimidazole inverse agonist
Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM). -
Brompheniramine maleate 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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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.
- 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. -
H4 receptor antagonist
JNJ-39758979 is histamine H4 receptor antagonists with a Ki of 12.5 nM.
