Catalog No.
Product Name
Application
Product Information
Citations
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Histamine Receptor Inhibitor
Quinotolast sodium is a histamine receptor inhibitor that effectively blocks the release of histamine, LTC4, and PGD2 in a concentration-dependent manner within the range of 1-100 μg/mL. This compound is valuable for research applications focused on allergic responses and inflammatory processes, as it helps elucidate the mechanisms of histamine signaling and associated pathophysiologies. -
H1 Receptor Antagonist
Antazoline is a histamine H1 receptor antagonist that exhibits anticholinergic and antiviral activities. It functions by competitively inhibiting histamine binding to H1 receptors, thereby mitigating physiological allergic responses. This compound demonstrates a dose-dependent reduction of HBV DNA levels in HepAD38 and Huh7 cell lines, with EC50 values of 2.910 μmol/L and 2.349 μmol/L, respectively. Additionally, Antazoline may possess anti-arrhythmic properties relevant to acute myocardial infarction. Its diverse biological activities make it a valuable reagent for research in cardiovascular diseases and hepatitis B virus infections. -
Histamine H2 Antagonist
Zolantidine dimaleate is a potent and selective histamine H2 antagonist that effectively crosses the blood-brain barrier. This compound demonstrates significant antinociceptive activity, making it valuable for research focused on pain modulation and related neurological studies. Zolantidine dimaleate can be utilized in various experimental settings to investigate the mechanisms of pain relief and the role of histamine signaling in the central nervous system. -
H1 Histamine Receptor Antagonist
Thonzylamine is an orally active H1 histamine receptor antagonist that exhibits notable antihistaminic and antianaphylactic properties. This compound is valuable for research involving hypersensitivity diseases, as well as conditions such as nasal congestion and allergic conjunctivitis. Its targeted action on the H1 receptor makes it a useful tool in the study of various allergic disorders. -
Histamine H4 Receptor Agonist
VUF 8430 dihydrobromide is a potent and selective agonist of the histamine H4 receptor, exhibiting a Ki of 31.6 nM and an EC50 of 50 nM. This compound is valuable for investigating the role of the H4 receptor in immune response modulation and inflammation. Its specificity makes it a useful tool for research into histamine-related disorders and potential therapeutic applications in allergic and inflammatory conditions. -
histamine H4 receptor antagonist.
Seliforant is a selective histamine H4 receptor antagonist that is primarily utilized in the study of immune response modulation and allergic conditions. By inhibiting the H4 receptor, Seliforant demonstrates potential anti-inflammatory and anti-allergic activities, making it a valuable tool for researching pathways related to allergic diseases and immune regulation. Its oral bioavailability allows for convenient administration in various in vivo experimental settings. -
Histamine Antagonist
Dimethindene maleate is a selective histamine H1 antagonist known for its antihistaminic properties. It effectively mitigates hypersensitivity reactions, making it valuable in the study of allergic responses and other histamine-related conditions. Researchers utilize Dimethindene maleate to explore its effects on inflammation and allergic pathways. -
H1 Receptor Antagonist
Olopatadine is an orally active and selective antihistamine that functions as an H1 receptor antagonist and mast cell stabilizer. It effectively inhibits the release of pro-inflammatory mediators from human conjunctival mast cells, making it instrumental in the study of allergic conjunctivitis. Olopatadine is valuable in researching the mechanisms of allergic responses and the management of allergic symptoms. -
Histamine H1-Receptor Antagonist
Niaprazine is a selective histamine H1-receptor antagonist. It exhibits both antihistamine and antiserotonin properties, making it a valuable compound for investigating sleep disorders and related biological effects. Its ability to modulate neurotransmitter signaling is relevant for research into conditions such as insomnia and anxiety. -
H3R Inverse Agonist
H3R Antagonist 1 Hydrochloride is an inverse agonist of the histamine receptor 3 (H3R). This compound has been shown to elevate the expression levels of myelin-associated glycoprotein (MAG) and myelin basic protein (MBP) in differentiating oligodendrocytes. It serves as a valuable reagent for research investigating myelination processes and potential therapeutic strategies for multiple sclerosis. -
H3 Agonist
(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective agonist of the H3 histamine receptor, exhibiting a Kd of 50.3 nM. This compound has been shown to enhance memory retention and alleviate memory impairment in rat models, making it a valuable tool for research on cognitive function and neuropharmacology. Its ability to penetrate the blood-brain barrier further establishes its utility in neurological studies. -
H1/ H2 Agonist
HTMT dimaleate is a potent agonist of histamine H1 and H2 receptors. It exhibits significantly enhanced activity, being 40,000 times more effective than histamine in mediating H2 receptor effects in natural suppressor cells. This compound is valuable for research focused on immunological responses and histamine receptor signaling pathways. -
Histamine H2 Receptor Antagonist
BMY-25368 hydrochloride is a potent antagonist of the histamine H2 receptor, functioning primarily as a gastric acid secretion inhibitor. By competitively inhibiting gastric secretion stimulated by histamine, it also effectively antagonizes secretion induced by Pentagastrin, Bethanechol, and food intake. This reagent is applicable in research focused on understanding gastric physiology and the modulation of acid secretion. -
Histamine Dehydrogenase
Histamine dehydrogenase, Microorganism (EC 1.4.99) is a homodimeric enzyme that facilitates the oxidative deamination of histamine in conjunction with an electron carrier. This enzyme plays a crucial role in histamine metabolism and its regulation within biological systems. It is applicable in studies related to neurotransmission, immune response, and the mechanisms underlying allergic reactions. Researchers may utilize this enzyme to explore its potential roles in various physiological and pathological processes involving histamine. -
H1 Receptor Antagonist
Dimethindene is a selective histamine H1 receptor antagonist known for its ability to inhibit histamine-mediated processes. This compound has been shown to impair cutaneous wound healing through its antagonistic action. Additionally, Dimethindene is capable of blocking potassium (K+) currents, making it valuable for research applications focused on skin physiology and ion channel modulation. -
Histamine 1 Antagonist
Azelastine is a potent and selective antagonist of the histamine H1 receptor. It demonstrates significant antihistaminic activity, making it valuable for research into allergic rhinitis and asthma. Additionally, Azelastine has potential applications in studying diabetic hyperlipidemia and SARS-CoV-2-related pathophysiology. -
Histamine H2 Receptor Antagonist
Aminopotentidine is a potent antagonist of the histamine H2 receptor, exhibiting KB values of 220 nM for human H2 receptors and 280 nM for guinea pig H2 receptors. This compound is utilized in studying gastric acid secretion and has applications in gastrointestinal research. Additionally, it serves as a valuable precursor for the synthesis of [125I] iodo derivatives, facilitating radiolabeling studies. -
Stable Isotope
(Rac)-Levomepromazine-d3 hydrochloride is a labeled form of the racemic compound Methotrimeprazine, belonging to the phenothiazine class. This reagent exhibits antagonist activity at various neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin, and histamine receptors. It is primarily used as a stable isotope for research applications, enabling in-depth studies of pharmacological interactions and the metabolic pathways of related compounds. -
Histamine Receptor Agonist
LML134 is a highly selective inverse agonist of the Histamine 3 receptor (H3R), demonstrating an impressive affinity with Ki values of 0.3 nM for hH3R cAMP and 12 nM for hH3R binding. This compound exhibits rapid brain penetration, resulting in significant H3R occupancy and a swift disengagement from its target. LML134 holds promise for investigating therapeutic strategies for sleep disorders by modulating histaminergic signaling pathways. -
Antihistamine Agent
Brompheniramine is a selective histamine H1 receptor antagonist primarily utilized as an antihistamine agent. With a Kd of 6.06 nM, it effectively alleviates symptoms of allergic rhinitis. In addition to its antihistaminic properties, brompheniramine exhibits anticholinergic, antidepressant, and anesthetic effects, making it suitable for various research applications related to allergy and inflammation. The compound also interacts with hERG, calcium, and sodium channels, with IC50 values of 0.90 μM, 16.12 μM, and 21.26 μM, respectively. -
Histamine H1 Antagonist
Triprolidine hydrochloride is a potent histamine H1 antagonist that effectively alleviates symptoms associated with allergic conditions. It exhibits properties that provide spinal cord motor and sensory blockade, making it valuable for research applications in allergic rhinitis and other histamine-mediated disorders. This compound facilitates the study of antihistamine effects and their underlying mechanisms in various biological contexts. -
Histamine H4 Receptor Agonist
ST-1006 is a potent agonist of the histamine H4 receptor, characterized by a pKi value of 7.94. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into inflammatory processes and related diseases. Its potential applications include studies in immunology and the modulation of allergic responses, providing insights into therapeutic strategies targeting the H4 receptor pathway. -
Histamine H1-Receptor Blocker
Oxomemazine is a phenothiazine-derived antagonist targeting the histamine H1 receptor. It exhibits notable antihistamine and anticholinergic properties, making it useful in research related to cough treatments. Additionally, Oxomemazine demonstrates a selective blockade of the muscarinic M1 receptor with a significant affinity difference compared to the M2 receptor. Studies have shown its protective effects against anaphylactic microshock in guinea pigs, highlighting its potential for further pharmacological investigation. -
H1 Receptor Antagonist
Cetirizine Impurity C dihydrochloride is an impurity of cetirizine, which acts as a selective H1 receptor antagonist. This compound demonstrates significant inhibition of histamine activity, contributing to its use in studies of allergic responses and histamine-mediated disorders. Its characterization is essential for ensuring the purity and efficacy of cetirizine in pharmaceutical formulations and research applications. -
Histamine H1 Receptor Antagonist
Meclizine-d8 is a deuterated derivative of Meclizine, functioning primarily as a histamine H1 receptor antagonist. This compound exhibits significant efficacy in alleviating nausea and preventing motion sickness. Additionally, Meclizine serves as an agonist for the mouse constitutive androstane receptor (CAR) while acting as an inverse agonist for the human CAR, making it relevant for studies on receptor modulation and signaling pathways in pharmacology. -
H1 Receptor Antagonist
Chloropyramine is a competitive reversible antagonist of the H1 receptor. It exhibits anti-tumor activity, particularly in breast cancer models. This compound is valuable for research into allergic conditions, including conjunctivitis and bronchial asthma, providing insights into histamine-mediated physiological responses and potential therapeutic interventions. -
H1 Receptor Blocker
(R)-(+)-Dimethindene maleate is a selective H1 receptor antagonist, displaying significant antihistaminic activity. It is utilized in research to study allergic responses and histamine-mediated mechanisms in various biological models, including porcine studies. This compound serves as a valuable tool for exploring the effects of histamine signaling and the therapeutic potential of H1 receptor blockade. -
βH Inhibitor AND H1 Receptor Antagonist
Desmethylastemizole is a β-hematin (βH) inhibitor and a Histamine H1 receptor antagonist. It exhibits potent antiplasmodium activity against Plasmodium falciparum, with IC50 values of 0.12, 0.11, and 0.06 μM for the Pf3D7, PfDd2, and PfItG strains, respectively. Additionally, Desmethylastemizole effectively blocks hERG K+ channels and inhibits histone-lysine N-methyltransferase EZH2 activity. This compound is relevant for research in long QT syndrome and malaria. -
H4/H1 Receptor Antagonist
H4R Antagonist 3 is a selective histamine H4 and H1 receptor antagonist with an EC50 of ≤10 mM. This compound is valuable for investigating the mechanisms underlying inflammatory, autoimmune, allergic, and ocular diseases. Its ability to modulate histamine receptor activity makes it a useful tool for research applications focused on these conditions. -
Histamine H3 Receptor Antagonist
Proxyfan is a potent antagonist of the histamine H3 receptor, exhibiting Ki values of 2.9 nM and 2.7 nM for rat and human H3 receptors, respectively. This compound demonstrates over 1000-fold selectivity for the H3 receptor compared to other histamine receptors. Proxyfan is useful in research applications focused on neurological disorders, cognitive enhancement, and sleep regulation, making it a valuable tool for studying histaminergic signaling pathways. -
Histamine H3 Receptor Antagonist
PF-03654764 is a potent and selective antagonist of the histamine H3 receptor, demonstrating Ki values of 1.2 nM for human H3 and 7.9 nM for rat H3 in whole cell assays. This compound exhibits significant potential in research applications related to allergies, particularly in the treatment of allergic rhinitis when combined with other antihistamines. Its oral bioactivity provides a valuable tool for investigating the role of histamine signaling in various physiological and pathological processes. -
Histamine H1 Receptor Antagonist
Diphenylpyraline is a potent histamine H1 receptor antagonist. This compound exhibits anticholinergic and antiallergic properties, making it effective as an orally active antihistamine. Diphenylpyraline is applicable in research focused on allergic conditions, including rhinitis and hay fever, as well as pruritic skin disorders. -
Histamine H1 Receptor Antagonist/5-Lipoxygenase Inhibitor
UCB-35440 is an orally active antagonist of the histamine H1 receptor and a selective inhibitor of 5-lipoxygenase. It demonstrates significant inhibition of leukotriene B4 (LTB4) formation in human whole blood, as well as a reduction in polymorphonuclear cell infiltration in mouse models. UCB-35440 also effectively inhibits histamine-induced bronchoconstriction and alleviates skin inflammation in guinea pig studies. This compound is suitable for research applications related to asthma and inflammatory skin conditions. -
Histamine Receptor Inverse Agonist
Mianserin-d3 is a deuterium-labeled form of Mianserin, primarily acting as an H1 receptor inverse agonist. It has demonstrated biological activity by activating κ-opioid and octopamine receptors, while also promoting ERK1/2 and CREB phosphorylation. Mianserin-d3 is valuable for investigating neurological disorders, including depression and epilepsy, and may influence social and exploratory behavior as well as electroconvulsive thresholds. -
Histamine H2 Receptor Antagonist
Cimetidine sulfoxide is a sulfoxide metabolite of the histamine H2 receptor antagonist Cimetidine. This compound demonstrates inhibitory activity at the H2 receptors, making it relevant for research applications involving gastric acid secretion and gastrointestinal disorders. Cimetidine sulfoxide may hold potential for exploring treatment options in peptic ulcer disease and upper gastrointestinal hemorrhage. -
anti-Allergic Agent
Setastine is an orally effective, non-sedative antihistamine that primarily targets H1 histamine receptors. It exhibits significant blocking properties, making it suitable for research applications related to allergies and rhinitis. Its long-acting effects further enhance its potential in exploring various allergic responses in scientific studies. -
Histamine H1 Antagonist
Noberastine is a potent antagonist of the Histamine H1 receptor, exhibiting significant peripheral antihistamine activity. This compound is primarily utilized in research focused on allergic responses and histamine-related disorders. Its ability to effectively inhibit H1 receptor activity makes it a valuable tool for studies investigating antihistaminic properties and related therapeutic applications. -
H4 Receptor Agonist
4-Methylhistamine hydrochloride is a highly selective agonist for the histamine H4 receptor (H4R), exhibiting a Ki value of 50 nM and over 100-fold selectivity compared to other histamine receptor subtypes. With a pEC50 of 7.4, it effectively activates H4R, making it a valuable tool for research in cancer, inflammation, and immunology. Applications include studies related to lung cancer and skin inflammatory conditions, providing insights into H4R-mediated pathways in these areas. -
Histamine Receptor Antagonist
Pimethixene is a potent antagonist of multiple receptor types, primarily functioning as a histamine receptor antagonist. It demonstrates significant activity against serotonin receptors (5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C), dopamine receptors (D2, D4), and muscarinic receptors (M1, M2), with reported pKis of 7.63 to 10.44. This pharmacological profile positions pimethixene as an effective agent for migraine management and offers valuable insights for research into antihistaminic and antiserotonergic therapies. -
Histamine Receptor Antagonist
SUN 1334H is a potent, orally active, and highly selective H1 receptor antagonist, exhibiting a Ki value of 9.7 nM. This compound effectively inhibits histamine-induced signaling, making it valuable for research on allergic responses and related conditions. Its specificity and potency make it suitable for studies investigating the role of H1 receptors in various biological systems. -
Histamine 3 Receptor Inverse Agonist
Samelisant free base is a selective inverse agonist of the histamine H3 receptor (H3R) that exhibits high binding affinity (Ki values of 8.7 nM for human H3R and 9.8 nM for rat H3R). It demonstrates effective brain penetration and oral bioavailability, making it a valuable tool in the study of sleep-related disorders. Research applications include exploring the mechanisms underlying sleep regulation and potential therapeutic interventions for insomnia and other sleep disturbances. -
Histamine H2 Receptor Antagonist
Cimetidine hydrochloride is a potent histamine H2 receptor antagonist with an inhibition constant (Ki) of 0.6 μM. It serves as an effective gastric acid reducer and is widely utilized in research pertaining to duodenal and gastric ulcers. Additionally, Cimetidine hydrochloride exhibits notable anti-cancer and anti-inflammatory properties, making it relevant for various therapeutic investigations. -
Histamine Receptor Antagonist
Adriforant is a selective antagonist of the histamine H4 receptor, exhibiting a binding affinity (Ki) of 2.4 nM and functional antagonism with a Ki of 1.56 nM. It effectively inhibits the actions of histamine, making it a valuable tool for studying the role of H4 receptors in various biological processes. This compound is particularly relevant for research in immunology, allergy, and inflammation, providing insights into potential therapeutic applications targeting histamine-mediated pathways. -
Histamine Receptor
Alcaftadine carboxylic acid selectively targets histamine H1 and H2 receptors, exhibiting broad-spectrum antihistaminic properties. This compound demonstrates significant efficacy in modulating immune cell recruitment and stabilizing mast cells, contributing to its therapeutic effects. Alcaftadine carboxylic acid effectively alleviates ocular itching associated with allergic conjunctivitis, showing superior performance compared to placebo and comparable efficacy to olopatadine 0.01%. This makes it a valuable candidate for research on allergy-related conditions and immune response modulation. -
Histamine 1 Receptor Antagonist
Acrivastine-d7 is a deuterated derivative of Acrivastine, targeting the histamine H1 receptor as an antagonist. It exhibits potent antihistaminic activity, making it valuable in studying allergic reactions and histamine-related pathways. This reagent can be utilized in pharmacokinetic studies and metabolic research involving H1 receptor interactions. -
H1 Histamine Receptor Antagonist
Thonzylamine hydrochloride is an orally active H1 histamine receptor antagonist. It exhibits significant antihistaminic and antianaphylactic properties, making it valuable for investigating hypersensitivity diseases, nasal congestion, allergic conjunctivitis, and other allergic conditions. This compound is a useful tool for researchers studying the mechanisms underlying allergic responses and evaluating potential therapeutic interventions. -
Histamine Receptor Antagonist
A-331440 is a selective antagonist of the histamine H3 receptor, which plays a critical role in the regulation of neurotransmitter release through inhibition at presynaptic sites. In preclinical studies with mice subjected to a high-fat diet, A-331440 demonstrated significant dose-dependent effects on body weight and fat loss. At a dosage of 5 mg/kg, it effectively reduced body weight akin to dexfenfluramine, while a 15 mg/kg dose led to substantial reductions in body fat and enhanced insulin tolerance, resembling the metabolic profile of mice on a low-fat diet. These results indicate A-331440's potential as an antiobesity agent by influencing histaminergic pathways related to appetite control and metabolic processes. -
H1-Antihistamine
Sequifenadine is an H1-antihistamine that effectively inhibits histamine action at the H1 receptor. This compound exhibits anti-inflammatory properties and is instrumental in the research of inflammatory eye diseases associated with allergic symptoms. Its ability to mitigate allergic responses makes it a valuable tool for studying the underlying mechanisms of allergies and related ocular conditions. -
H3R Inverse Agonist
H3R antagonist 1 is an inverse agonist of the histamine receptor 3 (H3R). This compound promotes the upregulation of myelin-associated glycoprotein (MAG) and myelin basic protein (MBP) in differentiating oligodendrocytes, which is crucial for myelination processes. H3R antagonist 1 is applicable in research focused on multiple sclerosis and related demyelinating disorders, providing insight into oligodendrocyte differentiation and myelin repair mechanisms. -
Antihistamine/anticholinergic Agent
Chlorphenoxamine hydrochloride is an antihistamine and anticholinergic agent that functions as a GPCR antagonist. It exhibits potent antiviral activity against lethal viral pathogens, including SARS-CoV, MERS-CoV, and Ebola virus, with reported IC50 values of 1.1 μM against Ebola virus and 6.2 μM against Marburg virus. This compound is utilized in research related to allergic conditions, urticaria, viral infections, and the treatment of Parkinson’s disease.
