Catalog No.
Product Name
Application
Product Information
Citations
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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 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 Receptor Modulator
Betahistine dihydrochloride is a potent histamine H1 receptor agonist and H3 receptor antagonist. This compound demonstrates significant biological activity in modulating histaminergic systems and is employed in research focused on conditions such as rheumatoid arthritis (RA). Its dual action makes it a valuable tool for investigating the pathways involved in inflammation and immune response. -
Antidepressant
Doxepin Hydrochloride is a tricyclic antidepressant that primarily functions as a selective antagonist of the histamine receptor H1. It effectively inhibits the reuptake of serotonin and norepinephrine, contributing to its antidepressant properties. Additionally, Doxepin exhibits significant activity as a CYP450 inhibitor, particularly affecting CYP450 2C19 and 1A2. This compound has demonstrated therapeutic potential in conditions such as atopic dermatitis and chronic urticaria, and it may enhance cognitive processes while providing neuroprotective effects against oxidative stress. -
Histamine 1 Receptor Blocker
Ketotifen fumarate is a noncompetitive antagonist of the histamine H1 receptor, functioning as a mast cell stabilizer. It exhibits significant biological activity by inhibiting 6-phosphogluconate dehydrogenase in vitro and demonstrates antiviral properties against SARS-CoV-2 and Influenza viruses. This compound is particularly useful in researching autoimmune encephalomyelitis (EAE) and in developing strategies for asthma attack prevention. -
Histamine Receptor Antagonist
Doxylamine succinate is a first-generation antihistamine that acts as an H1 receptor antagonist. This compound exhibits key biological activity as an effective sedative and hypnotic agent, making it valuable in sleep disorder research. Additionally, it possesses local analgesic properties, providing potential applications in studies related to pain management and sleep regulation. -
Histamine H1 Receptor Antagonist
Epinastine hydrochloride is a selective histamine H1 receptor antagonist and mast cell stabilizer. It exhibits high affinity for neuronal octopamine receptors, with inhibitory constants of Ki = 2 nM in locusts and Ki = 1.1 nM in honeybees. This compound effectively inhibits inflammatory mediators such as TARC, IL-8, and IL-4, and enhances anti-colon cancer immunity while reducing scratching behavior and vascular permeability induced by Substance P. Epinastine hydrochloride is valuable for research in allergic diseases and related inflammatory conditions. -
Antihistamine Agent
Hydroxyzine dihydrochloride is an antihistamine agent that primarily functions as a histamine H1-receptor antagonist and serotonin antagonist. It exhibits anxiolytic properties, making it a valuable tool for research into generalized anxiety disorder and related conditions. This compound can also be utilized in studies involving sedation and allergic reactions due to its diverse pharmacological effects. -
Histamine Receptor Inhibitor
Levodropropizine is a selective histamine receptor inhibitor primarily used as a peripheral antitussive agent. Its mechanism of action involves the suppression of cough reflexes through its interaction with histamine receptors, making it effective in treating cough associated with colds and allergies. Levodropropizine is noted for its good tolerance profile, facilitating its use in various research applications focused on respiratory physiology and pharmacology. -
Histamine H1 Antagonist
Pemirolast potassium is a histamine H1 antagonist with antiallergic properties. It effectively mitigates hypersensitivity reactions associated with Paclitaxel and demonstrates potential applications in studies related to bronchial asthma and conjunctivitis. This compound is valuable for researchers focusing on allergic responses and treatment mechanisms in respiratory and ocular conditions. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride hydrochloride is a non-steroidal anti-inflammatory agent and an antagonist of the H1-histamine receptor. It selectively inhibits phosphodiesterase activities, including PDE3, PDE4, and PDE5, with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. This compound is valuable for research applications focused on respiratory diseases, highlighting its potential in therapeutic investigations and the modulation of inflammatory responses. -
Histamine Receptor Antagonist
Mepyramine maleate is a potent antagonist of the histamine H1 receptor, exhibiting a Kd of 0.8 nM for H1, alongside Kd values of 5200 nM and >3000 nM for H2 and H3 receptors, respectively. With a pKd value of 9.4 for the H1 receptor, this first-generation antihistamine is valuable for studies focused on allergic responses and the role of histamine in various physiological processes. It is widely used in pharmacological research to explore histamine-mediated signaling and potential therapeutic applications in allergy and inflammation. -
Bacterial Inhibitor
Chlorprothixene hydrochloride functions as an antagonist of dopamine and histamine receptors, exhibiting Kis of 18 nM for hD1, 2.96 nM for hD2, 4.56 nM for hD3, 9 nM for hD5, and 3.75 nM for hH1 receptors. This compound demonstrates significant antipsychotic activity, making it a valuable tool for research into neuropharmacology and the mechanisms underlying psychotic disorders. Its receptor modulation also indicates potential applications in the study of bacterial inhibition mechanisms, providing insights into the interplay between neurotransmitter systems and microbial pathogenesis. -
Histamine H1 Antagonist
Triprolidine hydrochloride monohydrate is a first-generation antihistamine that functions as a histamine H1 antagonist. It is primarily utilized in research on allergic rhinitis and has demonstrated effects on spinal motor and sensory block in rodent models. This compound is valuable for understanding histamine-related physiological responses and the mechanisms underlying allergic reactions. -
histamine H1 Receptor Agonist
Betahistine mesylate is an orally active agonist of the histamine H1 receptor, with antagonist properties at the H3 receptor. This compound is primarily utilized in research to investigate the role of histamine receptors in rheumatoid arthritis (RA) and other related inflammatory conditions. Its unique mechanism of action makes it a valuable tool for studying histaminergic signaling pathways and their implications in joint pathology. -
Histamine Receptor Modulator
Betahistine is a histamine receptor modulator, acting as an agonist at the H1 receptor and an antagonist at the H3 receptor. It has demonstrated potential in modifying histamine pathways and is utilized in research related to rheumatoid arthritis (RA). This compound serves as a valuable tool for investigating the role of histaminergic signaling in inflammatory conditions. -
VEGFR Inhibitor
Chloropyramine hydrochloride is an H1 histamine receptor antagonist that also serves as an inhibitor of vascular endothelial growth factor receptor 3 (VEGFR-3) and focal adhesion kinase (FAK). This compound exhibits key biological activities, contributing to research in angiogenesis and related pathways. It is valuable for studies aimed at understanding the role of VEGFR signaling in various physiological and pathological processes. -
Histamine 1 Receptor Antagonist
Decloxizine dihydrochloride is a potent antagonist of the histamine H1 receptor. It exhibits significant anti-allergic activity, making it valuable in research pertaining to allergy and asthma models. Additionally, this compound can be utilized to investigate the role of histamine signaling in various physiological and pathological processes. -
Histamine Receptor Inhibitor
Dexchlorpheniramine maleate is a potent histamine receptor inhibitor primarily utilized in the treatment of allergic conditions. This compound exhibits anti-inflammatory, anti-irritant, and anti-allergic properties, making it effective for managing symptoms of allergic rhinitis. Additionally, dexchlorpheniramine maleate has been shown to inhibit myocardial contraction in rat models, providing further insight into its biological effects. It serves as a valuable reagent for research applications exploring the mechanisms of allergic responses and their physiological effects. -
Antihistamine/anticholinergic Agent
Chlorphenoxamine is an antihistamine and anticholinergic agent that functions as a GPCR antagonist. This compound exhibits antiviral properties against several lethal viral diseases, including SARS-CoV, MERS-CoV, and Ebola virus (EBOV), with IC50 values of 1.1 μM for EBOV and 6.2 μM for Marburg virus (MARV). Chlorphenoxamine is utilized in research focused on allergic conditions, urticaria, viral infections, and Parkinson’s disease. -
Asenapine Metabolite
N-Desmethyl asenapine is a primary metabolite of Asenapine, an atypical antipsychotic agent. This compound functions as an antagonist at multiple receptor sites, including serotonin, adrenoceptors, dopamine receptors, and histamine receptors. N-Desmethyl asenapine is valuable for research into psychopharmacology and the pharmacokinetics of antipsychotic drugs. Its role in studying the therapeutic and side effects associated with Asenapine makes it a significant reagent in the field. -
Stable Isotope
Sarpogrelate-d3 hydrochloride is a deuterium-labeled form of Sarpogrelate hydrochloride, serving as a selective antagonist for the 5-HT2 receptor family. With pKis of 8.52, 6.57, and 7.43 for the 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively, it demonstrates notable selectivity over 5-HT1, 5-HT3, 5-HT4, and various adrenergic and histamine receptors. This reagent is valuable for studying vascular diseases related to thrombosis, enabling researchers to investigate the pharmacodynamics and metabolism of Sarpogrelate in biological systems. -
Antihistamine Agent
Meclizine is an antihistamine that reversibly inhibits the binding of histamine to H1 receptors, making it effective as an anti-motion sickness agent. As a piperazine derivative, it can cross the blood-brain barrier, enabling its use in neurological research. Additionally, Meclizine acts as an agonist for the mouse constitutive androstane receptor (CAR) and serves as an inverse agonist for the human equivalent. This compound is also relevant for studying polyglutamine (polyQ) toxicity disorders, including Huntington's disease. -
Antihistamine Agent
Meclizine dihydrochloride monohydrate is an antihistamine that reversibly inhibits histamine interactions at the H1 receptor. As a member of the piperazine class of H1 antagonists, it is primarily utilized as an effective anti-motion sickness agent. This compound also demonstrates the ability to cross the blood-brain barrier and functions as an agonist for the mouse constitutive androstane receptor (CAR), while acting as an inverse agonist for the human CAR. It has applications in research focusing on polyQ toxicity disorders, including Huntington's disease. -
Stable Isotope
Cyproheptadine-d3 is a deuterium-labeled derivative of the antihistamine Cyproheptadine, serving as a stable isotope for research applications. It primarily acts as a serotonin and histamine receptor antagonist, making it useful in studies investigating receptor interactions and pharmacokinetics. This reagent is valuable for tracing and quantifying Cyproheptadine in various biological samples, facilitating research in pharmacology and toxicology. -
Histamine Release Inhibitor
Alginic acid is a natural polysaccharide recognized for its ability to inhibit histamine release, making it a valuable compound for research into allergic reactions and inflammation. Its remarkable water solubility, film-forming properties, and biodegradability enhance its applicability in various biological studies. Alginic acid has been demonstrated to induce oxidative stress-mediated effects, resulting in hormone secretion disorders, apoptosis, and autophagy in mouse granulosa cells and ovaries. This compound is of particular interest in anti-anaphylactic and anti-inflammatory research applications. -
H1-histamine/P2X7 Receptor Antagonist
Oxatomide is a dual antagonist of the H1-histamine receptor and the P2X7 receptor, noted for its oral bioavailability. It exhibits significant antihistaminic, antiallergic, and anti-inflammatory properties, making it a valuable compound for the study of allergic diseases. Researchers can utilize Oxatomide to investigate mechanisms of allergy and inflammation, contributing to potential therapeutic advancements. -
H1 receptor Antagonist
R 58639 is a selective histamine H1 receptor antagonist. It demonstrates significant biological activity in the modulation of allergic responses and cognitive processes. This compound is primarily utilized in research focusing on the pathophysiology and treatment of gastric ulcers, providing insights into the role of H1 receptor signaling in gastrointestinal biology. -
Histamine H2 Receptor Agonist
Betazole hydrochloride is a pyrazole derivative that acts as a histamine H2 receptor agonist. This compound stimulates gastric acid secretion and significantly elevates common bile duct pressure. Betazole is primarily utilized as a diagnostic agent, known as histalog, to assess gastric acid secretory capacity. -
Antihistamine
Diphenhydramine is a first-generation antihistamine that functions primarily as a histamine H1-receptor antagonist. It exhibits anti-cholinergic properties, allowing it to effectively alleviate allergic symptoms. This compound is capable of crossing the blood-brain barrier, making it valuable in neurological studies and research focused on central nervous system effects. Its diverse applications also include exploration in pharmacology and behavioral research involving sedative effects. -
Histamine 1 Receptor Blocker
Ketotifen is an orally active second-generation noncompetitive antagonist of the histamine H1 receptor, known for its role as a mast cell stabilizer. It exhibits significant biological activity by inhibiting 6-phosphogluconate dehydrogenase in vitro and displays antiviral properties against SARS-CoV-2 and the Influenza virus. Ketotifen is applicable in research focused on autoimmune encephalomyelitis (EAE) and contributes to studies aimed at preventing asthma attacks. -
Histamine Receptor Antagonist
Levocetirizine is a third-generation peripheral histamine H1-receptor antagonist. As the R-enantiomer of Cetirizine, it demonstrates a higher binding affinity for the H1 receptor compared to its S counterpart. Levocetirizine is primarily utilized in the management of allergic rhinitis and chronic idiopathic urticaria, providing effective relief from allergy-related symptoms. Its efficacy makes it a valuable tool in related pharmacological research. -
H1R-H4R Agonist
Amthamine dihydrobromide is an agonist of the histamine receptors H1R to H4R. This compound has been shown to induce liver congestion and necrosis of hepatocytes, providing a valuable model for studying the hepatotoxic effects associated with H1R-H4R activation. It is suitable for research applications focused on the roles of these receptors in liver function and pathology. -
Anti-histamine
Chlorpheniramine is an H1 antihistamine that primarily targets histamine receptors to alleviate symptoms associated with allergic reactions. It exhibits significant efficacy in reducing peripheral and central histamine-induced effects, making it a valuable tool in the study of allergic diseases and related pathophysiological processes. This compound is widely utilized in research applications focusing on allergy management and pharmacological interventions. -
D2/H1 Antagonist
Thiethylperazine is a potent antagonist of dopamine D2 and histamine H1 receptors. This phenothiazine derivative exhibits notable anti-emetic, antipsychotic, and antimicrobial properties, making it valuable in various therapeutic contexts. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β (Aβ) load in murine models, thus highlighting its potential relevance in neurodegenerative research. -
Histamine-1 (H1R) Receptor Agonist
2-Pyridylethylamine hydrochloride functions as an agonist for the histamine-1 (H1R) receptor. This compound has demonstrated the ability to mitigate joint injury induced by formalin in rat models. Additionally, it serves as a valuable tool for investigating spinal cord neuropeptide Y (NPY) release, contributing to research in neurobiology and pain mechanisms. -
Histamine 4 Receptor Agonist
4-Methylhistamine dihydrochloride is a potent and selective agonist of the histamine H4 receptor (H4R), exhibiting a Ki value of 50 nM. It demonstrates greater than 100-fold selectivity for hH4R compared to other histamine receptor subtypes, with an effective activation pEC50 of 7.4. This compound is valuable for research in cancer, inflammation, and immunology, particularly in studies related to lung cancer and skin inflammation. -
Histamine Receptor Antagonist
Adriforant hydrochloride is a potent 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. This compound is valuable for research applications related to immune modulation and inflammation, providing insights into histamine signaling pathways. Its specificity for H4 receptors positions it as a useful tool for studying various biological processes influenced by histamine. -
Antihistamine Agent
Hydroxyzine is an antihistamine agent that primarily targets histamine H1 receptors and functions as a serotonin antagonist. This compound exhibits anxiolytic properties, making it valuable for research applications related to generalized anxiety disorder. Its dual action provides insights into the interplay between histamine and anxiety regulation in various biological contexts. -
H1 receptor Antagonist
Mianserin is an orally active antagonist of the H1 receptor, exhibiting unique pharmacological properties. In addition to its primary mechanism, Mianserin activates κ-opioid and octopamine receptors, leading to the phosphorylation of ERK1/2 and CREB. This compound has demonstrated effects on social and exploratory behavior, as well as raising electroconvulsive thresholds. Mianserin is valuable for research into neurological disorders including depression and epilepsy. -
H1-Receptor Antihistamine
Methapyrilene hydrochloride is an orally active H1-receptor antihistamine that also exhibits anticholinergic properties. This pyridine-derived compound is primarily utilized in research related to allergic responses and histamine-mediated processes. Additionally, due to its hepatotoxic effects, methapyrilene hydrochloride can serve as a tool for studying periportal hepatic necrosis in vivo, providing insights into liver pathology and toxicity mechanisms. -
H3 Agonist
(R)-(-)-α-Methylhistamine dihydrochloride is a potent and selective agonist for the H3 histamine receptor, demonstrating a Kd of 50.3 nM. This compound has been shown to enhance memory retention and reduce memory impairment in preclinical models, making it valuable for research focused on cognitive function and neurological disorders. Its ability to penetrate the blood-brain barrier further supports its potential in brain-related studies. -
Histamine H2-receptor Antagonist
Tiotidine is a selective antagonist of the histamine H2 receptor, exhibiting a pA2 value of 7.3-7.8 in the guinea pig right atrium. This compound demonstrates low affinity for H1 and H3 receptors, allowing for targeted modulation of H2 receptor activity. Tiotidine is primarily used in research applications related to gastric acid secretion and histamine-related signaling pathways. -
H1 Histamine Receptor Antagonist
Clemastine is a potent H1 histamine receptor antagonist with the ability to cross the blood-brain barrier, providing effective antiallergic properties. In addition to its antihistamine action, Clemastine also interacts with muscarinic acetylcholine receptors, specifically M1 and M4 subtypes. This compound demonstrates significant biological activities, including promoting central nervous system remyelination, activating autophagy, and exhibiting anti-apoptotic and neuroprotective effects. Its anti-inflammatory properties further highlight its potential in various research applications related to allergy, neurodegeneration, and inflammation. -
Histamine Receptor Agonist
N-Methylhistamine dihydrochloride is a selective agonist of the histamine H3 receptor, playing an important role in the study of mastocytosis. This compound is instrumental in the diagnosis and management of this condition. Additionally, it acts as a valuable biomarker for evaluating mast cell accumulation in clinical assessments. -
Histamine H3/H4 Receptor Agonist
Imetit dihydrobromide is a potent and selective agonist of the histamine H3 and H4 receptors, exhibiting binding affinities with Ki values of 0.3 nM and 2.7 nM, respectively. This compound effectively mimics histamine, inducing morphological changes in eosinophils, with an EC50 value of 25 nM. Imetit dihydrobromide is valuable for researching mechanisms related to allergic responses and inflammation modulation. -
Histamine Metabolite
1-Methyl-4-imidazoleacetic acid hydrochloride is a stable histamine metabolite formed through the oxidation of N-methylhistamine. This compound serves as a valuable tool in research investigating histamine metabolism and its physiological roles. It can be utilized in studies related to receptor interactions and the biochemical pathways involving histamine. -
H1 Receptor Antagonist
Tecastemizole, a major metabolite of Astemizole, functions as a potent and selective antagonist of the H1 receptor. It exhibits notable anti-inflammatory properties, making it valuable for research into allergic responses and inflammation-related conditions. This compound is useful for studies investigating the modulation of histamine signaling pathways and their implications in various biological processes. -
Histamine Inhibitor
Spinacetin is a natural compound derived from Inula japonica that acts as a histamine inhibitor. It effectively inhibits histamine release, demonstrating notable anti-inflammatory properties. This reagent is valuable for research applications focused on allergic responses, inflammation studies, and the elucidation of histamine-related pathways.
