Catalog No.
Product Name
Application
Product Information
Citations
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Histamine Receptor Antagonist
OUP-186 is a selective antagonist of the histamine H3 receptor, which plays a critical role in neurotransmission and the modulation of various physiological processes. It exhibits potent biological activity in blocking H3 receptor-mediated signaling pathways. This compound is useful in research applications focused on understanding central nervous system disorders, sleep regulation, and cognitive functions, making it a valuable tool for pharmacological studies targeting histamine receptors. -
H2 Receptor Agonist
Impromidine is a selective agonist of the histamine H2 receptor, effectively stimulating gastric mucosal blood flow and promoting acid secretion. Its potent activity makes it a valuable tool in studies investigating gastric physiology and the mechanisms underlying acid secretion. Impromidine can be utilized in research related to gastrointestinal disorders and the effects of histamine receptor modulation on gastric function. -
Histamine H1 Receptor Antagonist
(R)-(+)-Mequitazine is a histamine H1 receptor antagonist that inhibits histamine activity by competitively binding to H1 receptors in gastrointestinal, vascular, and respiratory tissues. This compound undergoes biotransformation in human liver microsomes, producing hydroxylated and S-oxidized metabolites. Additionally, (R)-(+)-Mequitazine has been shown to inhibit CYP3A-catalyzed midazolam 1'-hydroxylase activity. Its properties make it a valuable reagent for investigating various allergic diseases and related pharmacological studies. -
Histamine Receptor Inhibitor
D18024 is a potent histamine receptor inhibitor that demonstrates antiallergic and antihistaminic properties. This compound exhibits significant activity in modulating histamine-mediated processes, making it useful for research focused on allergy and inflammation pathways. D18024 can be employed in studies investigating the role of histamine receptors in various biological systems, contributing to the understanding of allergic responses and potential therapeutic interventions. -
Histamine Receptor Antagonist
Minocromil is a histamine receptor antagonist primarily employed in the treatment of asthma. It functions by inhibiting the histamine H1 receptor, leading to the reduction of bronchoconstriction and inflammation. This compound is valuable in research related to allergic responses and the development of therapeutic strategies for asthma management. -
Histamine Receptor Inhibitor
CI-949 is a potent histamine receptor inhibitor known for its ability to suppress the release of key allergic mediators. It demonstrates inhibition of histamine, leukotriene C4/D4, and thromboxane B2 with IC50 values of 11.4 μM, 0.5 μM, and 0.1 μM, respectively. This compound is useful for studies focused on allergic reactions and inflammation, providing insights into therapeutic strategies for allergic conditions. -
Histamine Receptor Inhibitor
KP136 is a potent histamine receptor inhibitor that exhibits antiallergic properties. It effectively blocks histamine release with an IC50 of 76.1 μg/mL and degranulation at 63 μg/mL. This compound is valuable for research applications focusing on allergic responses and related inflammation processes. -
Histamine Receptor Antagonist
FRG8701 is a selective antagonist of the Histamine H2 receptor, demonstrating an IC50 range of 0.25 to 0.43 μM. This compound exhibits significant inhibitory activity, making it a valuable tool for investigating histamine signaling pathways and their implications in various physiological processes. Research applications include studies on gastric acid secretion, allergic reactions, and potential therapeutic interventions for related pathologies. -
Histamine Receptor Modulator
H3 receptor-MO-1 is a selective modulator of the histamine H3 receptor, functioning as an antagonist to enhance release of neurotransmitters. This compound is pivotal for research into neurological disorders and sleep regulation, making it a valuable tool in studying the role of histamine in the central nervous system. Its unique pharmacological profile enables investigation into potential therapeutic applications for conditions such as cognitive deficits and mood disorders. - 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. -
LTC4 inhibitor
Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2). -
histamine H2-receptor antagonist
Niperotidine is a histamine H2-receptor antagonist. -
histamine H3 receptor antagonist
GSK189254A (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. -
histamine H1 receptor antagonist
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. -
histamine H3R antagonist/inverse agonist
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. -
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. -
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. -
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 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.
