Histamine Receptors

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  1. 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.
  2. 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.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
  7. 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.
  8. 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.
  9. 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.
  10. 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.
  11. Histamine Methylated Product

    3-Methylhistamine dihydrochloride is a methylated derivative of histamine that serves as a significant biomarker in the study of immune responses. This compound has been shown to be upregulated in vaccinated murine models, making it useful for research applications focused on immunological studies and histamine-related pathways. Its role in the modulation of immune activity positions it as a valuable reagent in exploring allergic reactions and other histamine-mediated processes.
  12. Histamine N-methyltransferase

    Histamine N-methyltransferase, rat is a biocatalyst that functions primarily by catalyzing the N-methylation of histamine. This enzyme plays a critical role in the metabolism of histamine, contributing to the regulation of physiological processes such as inflammatory responses and neurochemical signaling. Research applications include enzyme engineering aimed at optimizing reaction kinetics, enhancing substrate specificity, and improving enzyme stability under varying pH conditions, potentially facilitating dynamic control of enzymatic activity for various experimental needs.
  13. Endogenous Metabolite

    1-Methylhistamine dihydrochloride is a metabolite of histamine that primarily targets histamine receptors. This compound exhibits significant biological activity in the modulation of allergic responses and neurotransmission processes. It is widely utilized in research applications focusing on histamine signaling pathways and its role in various physiological and pathological conditions.
  14. H1-Receptor Antagonist

    Cetirizine Impurity B dihydrochloride is an impurity of the H1-receptor antagonist, cetirizine dihydrochloride. While cetirizine demonstrates significant antiallergic properties and effectively inhibits eosinophil chemotaxis during allergic responses, this specific impurity is valuable for analytical purposes and quality control in research applications. It aids researchers in understanding the pharmacological profile and potential effects associated with cetirizine and its metabolites.
  15. H1R Antagonist

    Fexofenadine Impurity F is a derivative of Fexofenadine, primarily acting as a histamine H1 receptor (H1R) antagonist. This compound exhibits biological activity associated with anti-allergic properties, making it relevant in the study of allergic reactions and potential therapeutic interventions for conditions such as seasonal allergic rhinitis and chronic idiopathic urticaria. It serves as a useful reagent for research in drug development and impurity profiling.
  16. Histamine H1 Receptor Antagonist

    Terfenadine N-oxide is a histamine H1 receptor antagonist with an IC50 value of 2.73 μM, also exhibiting inhibition of the hERG potassium channel with an IC50 of 0.698 μM. This compound is valuable for investigating histamine-related allergic diseases and the role of hERG channels in arrhythmias. Its dual activity makes it a useful tool for research in pharmacology and toxicology related to allergic responses and cardiac rhythm disturbances.
  17. Biochemical Assay Reagent Control

    N-Formyl desloratadine is an inhibitor targeting the H1 histamine receptor, primarily utilized as a biochemical assay reagent control. This compound demonstrates significant antihistamine activity, making it an essential tool for research related to allergic responses and histamine receptor activity. Its use in pharmacological studies allows for the assessment of H1 receptor modulation and the investigation of allergic conditions.
  18. H3 Agonist

    Immepip dihydrobromide acts as a selective agonist for the H3 histamine receptor. It is known to attenuate cortical histamine release, thereby influencing neurotransmitter dynamics. This compound is applicable in the study of neurological disorders, providing insights into histaminergic system modulation and its potential therapeutic effects.
  19. Impurity of Asenapine

    Asenapine impurity 1 is a recognized impurity of Asenapine, an atypical antipsychotic known for its antagonistic activity on serotonin, adrenoceptors, dopamine, and histamine receptors. With reported pKi values ranging from 8.2 to 10.5 across these targets, it is relevant for studies investigating the pharmacological profile of Asenapine. This impurity is important for quality control and characterization in research contexts focused on schizophrenia and bipolar disorder treatments.
  20. Stable Isotope

    Desloratadine-d5 hydrochloride is a stable isotope-labeled derivative of Desloratadine hydrochloride, designed for use in quantitative mass spectrometry applications. This compound retains the pharmacological properties of the parent drug while providing a valuable tool for understanding drug metabolism and pharmacokinetics. It is particularly suitable for research in allergology and histamine receptor studies, facilitating the assessment of drug interactions and efficacy in various biological systems.
  21. Histamine H2 receptor Antagonist

    Nizatidine is a potent and orally active histamine H2 receptor antagonist. It plays a crucial role in the inhibition of gastric acid secretion, making it valuable for research on gastric ulcers and gastrointestinal disorders. Nizatidine has been utilized in various animal models to study its effects on ulcer healing and prevention of recurrence.
  22. Histamine Receptor Antagonist

    Famotidine is a competitive antagonist of the histamine H2-receptor, primarily involved in the inhibition of gastric acid secretion. This compound demonstrates significant biological activity in reducing gastric acidity, making it valuable in research related to acid-related gastrointestinal disorders. Famotidine can be utilized in studies investigating the pathophysiology of conditions such as peptic ulcers and gastroesophageal reflux disease (GERD).
  23. Histamine Antagonist

    Methapyrilene is a histamine antagonist with anticholinergic properties, classified as a pyridine compound. It is known to induce specific epigenetic alterations in target organs, including a reduction in DNA methylation levels. Additionally, methapyrilene has been shown to induce hepatocellular carcinoma in rodent models, making it relevant for research in cancer biology and epigenetics.
  24. H1 Receptor Antagonist

    Pheniramine is a first-generation histamine H1 receptor antagonist that primarily targets the central nervous system (CNS) to produce sedative and hypnotic effects. It exhibits antitumor activity by inducing apoptosis in leukemia cells. Additionally, pheniramine serves as a local analgesic and is effective in suppressing pain while providing antipruritic properties, making it valuable for various research applications in pharmacology and oncology.
  25. Histamine Receptor Antagonist

    Chlorcyclizine is a histamine H1 receptor antagonist that modulates allergic responses and reduces symptoms of histamine-mediated conditions. This compound exhibits effective anti-allergic properties, making it useful in studying the mechanisms of allergic reactions and potential therapeutic interventions. Research applications include the investigation of histamine-related pathways and the evaluation of antihistaminic effects in various biological systems.
  26. H1 Receptor Antagonist

    Promethazine is an H1 receptor antagonist that belongs to the phenothiazine family. This first-generation antihistamine exhibits potent sedative properties and demonstrates weak antipsychotic effects. It is primarily utilized in research to explore its antiallergic and sedative capabilities, making it valuable for studies focused on allergic responses and sleep-related research.
  27. H1-receptor Antagonist

    Thenalidine is an H1-receptor antagonist primarily used for its antihistaminic properties. It exhibits anticholinergic activity, making it valuable in the study of allergic reactions and histamine-related processes. This compound is useful for research applications related to allergy treatment, pharmacological profiling, and the exploration of histaminergic signaling pathways.
  28. H1 Receptor Antagonist

    (R)-Promethazine is an H1 receptor antagonist, serving as the R-enantiomer of Promethazine. This compound exhibits potent antihistamine activity, primarily used for its sedative effects. Additionally, it demonstrates weak antipsychotic properties, making it useful in various research applications related to sleep disorders and psychotropic effects.
  29. Antihistamine Agent

    Buclizine is an orally active antihistamine that targets histamine receptors, reducing allergic responses. In addition to its antiallergic properties, Buclizine has demonstrated teratogenic effects in rodent models and exhibits anti-tumor activity, making it of interest in cancer research. Its diverse mechanisms of action make it valuable for studies on histamine-related pathways and potential therapeutic applications in oncology.

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