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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
COX inhibitor/histamine H1 receptor agonist
Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist -
PAFR inhibitor/H1 receptor inhibitor
Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively. -
Histamine H1 receptor inhibitor
Antazoline HCl is a first generation antihistamine, binding to the histamine H1 receptor and blocking the action of endogenous histamine. -
Histamine/cholinergic inhibitor
Azatadine is an histamine and cholinergic inhibitor with IC50 of 6.5 nM and 10 nM, respectively. -
LTC4 inhibitor
Nedocromil sodium suppresses the action or formation of multiple mediators, including histamine, leukotriene C4 (LTC4), and prostaglandin D2 (PGD2). -
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. -
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. -
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. -
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. -
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 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. -
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. -
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. -
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. -
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. -
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-release Inhibitor
Panaxydiol is a histamine-release inhibitor that effectively suppresses histamine secretion in biological systems. This compound features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating the formation of diverse chemical linkages. Its unique properties make Panaxydiol a valuable reagent for researchers involved in chemical biology, drug discovery, and the development of innovative therapeutic strategies. -
Histamine Receptor Inhibitor
AM-0466 is a selective histamine receptor inhibitor primarily targeting voltage-gated sodium channel NaV1.7. This compound demonstrates potent anti-pruritic activity in histamine-induced itch models and exerts significant analgesic effects in capsaicin-induced pain assays. Its optimized pharmacokinetic profile supports its use in advanced in vivo research for evaluating efficacy in pain modulation and itch relief. -
Histamine Receptor Inhibitor
Fenethazine is a histamine receptor inhibitor known for its antihistamine activity. It effectively alleviates allergic reactions and related symptoms. Additionally, its structural congeners exhibit anticholinergic effects, making fenethazine a candidate for research into therapeutic interventions for Parkinson's disease. This compound is valuable for studies focused on histaminergic pathways and associated disorders. -
Histamine H3 Receptor Antagonist/Serotonin Transporter Inhibitor
JNJ-28583867 is a selective histamine H3 receptor antagonist with a Ki of 10.6 nM and an inhibitor of the serotonin transporter (SERT) with a Ki of 3.7 nM. This compound shows promise in modulating neurotransmitter systems and can be utilized in research focusing on depression and related neuropsychiatric disorders. Its unique mechanism makes it a valuable tool for studying the interplay between histaminergic and serotonergic pathways. -
Histamine Receptor Inhibitor
(R)-Azelastine hydrochloride is a histamine receptor inhibitor that effectively down-regulates the expression of H1, M1, and M3 receptors. This compound exhibits notable biological activity by inhibiting the proliferation of human nasal epithelial cells (HNEpC). Its applications in research include studying allergic reactions and evaluating the roles of histamine receptors in various cellular processes. -
Histamine Receptor Inhibitor
Linadryl is a histamine receptor inhibitor that exhibits antihistaminic properties. It demonstrates a moderate impact on gastric acid secretion following oral administration, approximately half that of Diphenhydramine. Linadryl is primarily utilized in research focusing on allergic responses, gastrointestinal function, and exploring the broader effects of histamine modulation in various biological systems. -
Histamine H1 Receptor Inhibitor
SUN-1334H free base is a potent orally active inhibitor of the histamine H1 receptor, demonstrating an IC50 of 20.3 nM and a Ki value of 9.7 nM. This compound effectively inhibits histamine-induced contractions in isolated guinea-pig ileum with an IC50 of 0.198 μM. SUN-1334H free base has significant applications in research related to bronchoconstriction, allergic responses, and rhinitis, as evident in its ability to mitigate histamine-induced bronchoconstriction in guinea pigs, skin wheals in beagle dogs, and ovalbumin-induced rhinitis in guinea pigs. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride is a potent inhibitor of phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4), and phosphodiesterase 5 (PDE5), with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. Additionally, it acts as an antagonist of the H1-histamine receptor, contributing to its anti-inflammatory properties. Fenspiride is primarily utilized in research related to respiratory diseases, offering insights into mechanisms of action and potential therapeutic applications. -
Histamine Receptor Inhibitor
VUF14738 is a bidirectional photoswitch antagonist targeting the histamine H3 receptor. This compound exhibits rapid and reversible photoisomerization, allowing for modulation of binding affinity in response to illumination. Its unique properties make VUF14738 ideal for real-time electrophysiological studies, facilitating research into the dynamic light modulation of receptor activation and the underlying mechanisms of histamine signaling. -
EBOV/MARV Inhibitor
CP19 is a histamine receptor antagonist that functions as an entry inhibitor for both Ebolavirus (EBOV) and Marburgvirus (MARV), demonstrating IC50 values of 3.4 μM and 29.5 μM, respectively. With selectivity index (SI) values of 29.4 for EBOV and 3.4 for MARV, CP19 exhibits notable antiviral activity. This compound is valuable for research into viral entry mechanisms and the development of antiviral strategies targeting EBOV and MARV. -
Histamine Receptor Inhibitor
Mequitamium iodide is a potent histamine receptor inhibitor, demonstrating significant antiallergic and bronchodilatory properties. It effectively antagonizes airway contraction and inflammatory responses triggered by histamine and various antigens, exhibiting nanomolar affinity for H1 and smooth muscle receptors. When delivered via aerosol, Mequitamium iodide markedly reduces histamine- and antigen-induced airway pressure increases in allergic mouse models. Additionally, it decreases eosinophil accumulation in the airways and inhibits platelet aggregation and bronchoconstriction induced by PAF. This compound is valuable for investigating allergic diseases, including rhinitis and asthma. -
Histamine Receptor Inhibitor
Impentamine dihydrobromide is a histamine H3 receptor antagonist known for its potent antihistamine activity. This compound demonstrates selective H3 antagonism, with a pA2 value of 8.4, indicating significant efficacy in guinea pig jejunum studies. Impentamine dihydrobromide binds specifically to the H3 receptor, making it valuable for research in neuropharmacology and related fields investigating histamine's role in neurotransmission and various physiological processes. -
Gastric Secretory Inhibitor
UK-9040 is an orally active inhibitor of gastric secretion that targets histamine receptors. This compound effectively reduces gastric acid, pepsin, and volume output in response to food, insulin, histamine, N-methyl histamine, and pentagastrin. UK-9040 is valuable for research applications focused on gastric physiology and the modulation of acid secretion. -
Histamine Receptor Inhibitor
Hetramine is a histamine receptor inhibitor known for its antihistamine and antiallergic properties. It effectively prevents histamine-induced intestinal contractions and mitigates allergic responses, including anaphylactic shock, in animal models such as guinea pigs. This compound is useful in research related to allergy mechanisms and gastrointestinal function. -
Histamine H3 Antagonist/Serotonin Reuptake Inhibitor
Histamine H3 antagonist-1 is a potent histamine H3 receptor antagonist and serotonin reuptake inhibitor, playing a critical role in neuromodulation. Its primary biological activity makes it valuable for research in the field of depression and related neuropsychiatric disorders. This compound offers insights into the interactions between histamine and serotonin signaling pathways, facilitating the development of novel therapeutic strategies. -
Histamine Receptor Inhibitor
Perphenazine-d8 dihydrochloride is a deuterium-labeled derivative of Perphenazine, primarily functioning as a histamine receptor inhibitor. This compound exhibits potent antipsychotic properties by interacting with serotonin and dopamine receptors. It is valuable for research focused on neuropharmacology, chemical biology, and the study of receptor-ligand interactions in psychiatric disorders. -
Histamine Receptor Inhibitor
(R)-Azelastine is a histamine receptor inhibitor with notable antiallergic properties. This compound effectively downregulates the levels of H1R, M1R, and M3R, making it significant for research related to allergy and inflammation. Additionally, (R)-Azelastine has been demonstrated to inhibit the proliferation of human nasal epithelial cells (HNEpC), indicating its potential applications in studies of respiratory conditions and allergic responses. -
Histamine Release Inhibitor
Acreozast (TYB-2285) is a potent histamine release inhibitor that acts by blocking the release of histamine primed with interleukin-3 (IL-3). This compound has demonstrated the potential to modulate allergic inflammation in vivo through the suppression of inflammatory mediators. Acreozast is of particular interest for research applications involving allergy and immune response studies. -
Histamine Receptor Inhibitor
Azatadine is a histamine receptor inhibitor that functions by antagonizing H1 and H2 subtypes. This compound exhibits significant biological activity in blocking histamine-mediated processes, making it valuable in research related to allergic responses and motion sickness. Azatadine's mechanism of action also extends to cholinergic pathways, providing further insights into neuropharmacological studies. -
Histamine Receptor Inhibitor
(S)-Azelastine is a selective antihistamine that primarily targets the histamine H1 receptor. This compound exhibits antiallergic and antiasthmatic properties, demonstrating the ability to downregulate levels of histamine receptors H1R, M1R, and M3R. Additionally, (S)-Azelastine has been found to inhibit the proliferation of human nasal epithelial cells, making it a valuable reagent for research in allergy and asthma mechanisms. -
Histamine Inhibitor
Elbanizine is a potent histamine inhibitor that effectively suppresses histamine and bradykinin release from rat mast cells, demonstrating an IC50 of 0.26 μM. This compound has been shown to inhibit IgE-mediated passive cutaneous anaphylaxis (PCA) reactions. Additionally, Elbanizine exhibits significant antiallergic and antiasthmatic properties in guinea pig models, making it a valuable tool for research in allergy and asthma mechanisms. -
Dopamine Receptor Inhibitor
BL-1020 mesylate is a dopamine receptor inhibitor with high affinity for D2L, D2S, and 5-HT2A receptors, exhibiting Ki values of 0.066, 0.062, and 0.21 nM, respectively. This compound functions as an antipsychotic agent and also acts as an agonist at the GABAA receptor, enhancing GABA release with a Ki of 3.74 μM. Furthermore, BL-1020 mesylate interacts effectively with histamine receptors (Ki of 0.47 nM) and demonstrates the ability to diminish amphetamine-induced hyperactivity while minimizing catalepsy and sedation. It penetrates the blood-brain barrier, making it suitable for neurological research applications. -
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 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 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.
