Catalog No.
Product Name
Application
Product Information
Citations
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Histamine Receptor Agonist
UR-AK49 is a potent agonist of the human histamine H1 and H2 receptors. It exhibits an EC50 value of 23 nM in a GTPase assay utilizing the hH2R-Gsalpha fusion protein expressed in Sf9 insect cells. This compound is relevant for applications in neurobiology and offers potential insights into histamine receptor functions in various physiological processes. -
Histamine H3 Receptor Antagonist
JNJ-10181457 is a selective non-imidazole antagonist of the histamine H3 receptor, known to normalize acetylcholine neurotransmission. This compound also serves as a click chemistry reagent, featuring an alkyne group that enables it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc) reactions. Its properties make it valuable for insights into neurological signaling and the development of innovative chemical biology applications. -
H1 Receptor Antagonist
Antazoline phosphate is a potent H1 receptor antagonist that primarily modulates the central nervous system and exhibits significant antiarrhythmic properties. This compound effectively prevents histamine from binding to its receptor sites, leading to antiallergic effects and inhibition of physiological responses triggered by histamine. In addition, Antazoline phosphate has demonstrated a dose-dependent reduction of HBV DNA in both HepAD38 and Huh7 cells, with EC50 values of 2.910 μmol/L and 2.349 μmol/L, respectively. Its multifaceted biological activity makes Antazoline phosphate valuable for research applications in cardiovascular diseases and hepatitis B virus studies. -
Histamine Receptor Antagonist
A-349821 is a histamine H3 receptor antagonist that functions as a radioligand ([3H]-A-349821) for assessing in vivo receptor occupancy. In rodent studies, [3H]-A-349821 demonstrates significant brain penetration, with a marked preference for cortical binding over the cerebellum, indicating selective interaction with H3 receptors. Its occupancy in the cortex is saturable and aligns with in vitro binding affinities. Competitive inhibition studies reveal dose-dependent reductions in receptor occupancy, correlating with blood concentrations associated with cognitive enhancement in preclinical models. This compound represents a valuable tracer for H3 receptor occupancy, facilitating the development and clinical analysis of H3 receptor antagonists. -
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 H3 Receptor Antagonist
A 331440 hydrochloride is a potent and selective antagonist of the histamine H3 receptor. It exhibits high binding affinity for both human and rat H3 receptors, with a Ki value of less than 25 nM. This compound is particularly relevant for research applications in the field of antiobesity, offering insights into metabolic regulation and potential therapeutic strategies. -
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 H2 Receptor Antagonist
Dalcotidine is a competitive antagonist of the histamine H2 receptor, exhibiting oral bioactivity. This compound is primarily utilized for its ability to promote the healing of chronic ulcers and to inhibit gastric acid secretion, making it valuable in gastrointestinal research applications. Its pharmacological profile supports the investigation of acid-related disorders and potential therapeutic interventions. -
Histamine H1-receptor Antagonist
Hydroxyzine-d8 is a deuterium-labeled derivative of Hydroxyzine, a well-known antagonist of the histamine H1 receptor. It demonstrates significant antihistaminic activity, making it valuable in the study of allergic responses and histamine-mediated conditions. This reagent is particularly useful in pharmacokinetic studies and metabolic profiling of Hydroxyzine. -
Histamine H2 Receptor Antagonist
Ramixotidine is a potent histamine H2 receptor antagonist that effectively inhibits gastric acid secretion induced by pentagastrin. It is utilized in research applications to explore mechanisms of acid secretion and the role of H2 receptors in gastrointestinal disorders. This compound serves as a valuable tool for studying gastric physiology and developing therapeutic strategies for acid-related diseases. -
Histamine H2 Receptor Antagonist
Roxatidine acetate is a selective competitive antagonist of the histamine H2 receptor. It exhibits significant potency in inhibiting gastric acid secretion and plays a role in the suppression of inflammatory responses. This compound is applicable in research concerning gastric and duodenal ulcers, and it has been identified to possess potential antitumor activity. -
Histamine H2-Receptor Antagonist
Lavoltidine is a potent, orally active irreversible antagonist of the histamine H2 receptor. It effectively inhibits gastric acid secretion, leading to significant reductions in acid-related disorders. Lavoltidine also induces hypergastrinemia, making it valuable for investigations into gastric physiology and the role of gastrin in digestive health. This compound is ideal for research applications focusing on gastrointestinal disorders and receptor pharmacology. -
Histamine Receptor Antagonist
GSK-1004723 is a novel antagonist targeting both H1 and H3 histamine receptors. It exhibits significant biological activity relevant to the modulation of allergic responses, particularly in the context of seasonal allergic rhinitis. This compound is suitable for research applications focused on understanding histamine-mediated mechanisms and evaluating potential therapeutic strategies for allergic conditions. -
H2 Histamine Receptors/ α2-AR/5-HT2(B,C) Serotonin Receptors Ligand
Platelet aggregation-IN-3 is a ligand for H2 histamine receptors, α2-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. This compound effectively inhibits platelet aggregation induced by ADP and collagen and modulates tumor cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 shows potential for applications in antiplatelet therapy for cardiovascular diseases and in the prevention of cancer-related thrombosis and tumor metastasis. -
Histamine Receptor
Dacemazine hydrochloride is a phenothiazine derivative that acts as an H1 histamine receptor antagonist. It has been investigated for its potential therapeutic applications in oncology, particularly as an anticancer agent. This compound may facilitate research into histamine signaling pathways and their impact on tumor progression and treatment responses. -
Histamine H2-Receptor Antagonist
AY 29315 is a selective, orally active histamine H2-receptor antagonist that effectively inhibits gastric acid secretion. It demonstrates significant antiulcer activity, making it a valuable tool for research into gastric ulcer pathophysiology and treatment. This compound is suitable for studies examining the role of histamine in gastrointestinal disorders. -
Histamine H2 Receptor Antagonist
Lamtidine is a potent histamine H2 receptor antagonist that primarily inhibits gastric acid secretion. This compound exhibits significant biological activity in modulating gastric function and is utilized in research related to gastrointestinal disorders, acid reflux, and peptic ulcer diseases. The analogues and derivatives of Lamtidine demonstrate enhanced activity profiles, making them valuable tools for further investigation in pharmacological studies. -
Stable Isotope
Famotidine-13C,d3 is a stable isotope-labeled derivative of Famotidine, a competitive antagonist of the histamine H2-receptor. This compound primarily functions to inhibit gastric acid secretion, making it valuable for gastrointestinal research. It is widely used in studies focused on histamine receptor activity, pharmacokinetics, and metabolic pathways. -
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. -
Antihistamine Agent
Phenyltoloxamine is an antihistamine agent that exerts sedative and analgesic effects. It demonstrates significant binding affinity for the Sigma-1 receptor, with a Ki value of 160 nM. This compound is utilized in research applications focused on allergy treatment, pain management, and the exploration of Sigma-1 receptor functions in various physiological processes. -
Histamine H2 Receptor Antagonist
TRM-115 is a potent histamine H2 receptor antagonist that inhibits the action of histamine at the H2 receptor site. This compound demonstrates significant biological activity relevant to the modulation of gastric acid secretion and is valuable in the study of digestive system disorders. Research applications include investigations into acid-related gastrointestinal pathologies and potential therapeutic strategies for conditions such as peptic ulcers and gastroesophageal reflux disease (GERD). -
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 1 Antagonist
(S)-Azelastine hydrochloride is a potent and selective histamine H1 antagonist. This compound exhibits significant antihistaminic properties, making it valuable for research related to allergic rhinitis, asthma, and hyperlipidemia associated with diabetes. Additionally, (S)-Azelastine hydrochloride may also be utilized in studies focused on SARS-CoV-2, contributing to the understanding of its effects on respiratory conditions and allergic responses. -
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. -
H1 receptor ligand
Pirdonium bromide is a hydrophilic ligand for the H1 receptor, characterized by its quaternary ammonium structure. This compound displays significant activity in modulating histamine receptor signaling pathways and is utilized in research applications related to allergic responses and neurotransmission. Its ability to interact selectively with H1 receptors makes it a valuable tool for elucidating the physiological roles of histamine in various biological systems. -
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 H2 Antagonist
Zolantidine is a potent and selective histamine H2 antagonist that effectively crosses the blood-brain barrier. Its primary biological activity includes the induction of antinociception, making it a valuable tool for pain research. Zolantidine is used in studies aimed at understanding histamine-mediated pathways and their implications in analgesic effectiveness. -
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. -
Partial Histamine H3 Receptor Agonist
GR-175737 is a partial agonist of the histamine H3 receptor, exhibiting an EC50 value of 7.8 nM. This compound is primarily utilized in research focused on inflammatory diseases, facilitating the investigation of H3 receptor modulation in various pathophysiological contexts. Its pharmacological profile makes it a valuable tool for studying the role of histamine receptors in inflammation and related disorders. -
Histamine H4 Receptor antagonist
A-940894 is a potent antagonist of the histamine H4 receptor, demonstrating Ki values of 7.6 nM for the rat H4 receptor and 71 nM for the human H4 receptor. This compound exhibits notable anti-inflammatory properties, making it valuable for research applications focused on immune response modulation and inflammatory disorders. A-940894 is an effective tool for elucidating the role of the histamine H4 receptor in various biological processes. -
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. -
Stable Isotope
Fenspiride-d5 hydrochloride is a deuterium-labeled derivative of Fenspiride hydrochloride, functioning as an α-adrenergic and H1 histamine receptor antagonist. This stable isotope is instrumental in pharmacokinetic studies and metabolic research, allowing for the tracking of drug metabolism and distribution in biological systems. Its unique labeling enhances the understanding of receptor interactions and pharmacological profiles in various experimental settings. -
Histamine H4R/H1R Ligand
VUF-6884 is a ligand for the histamine receptors H4R and H1R. It exhibits strong binding affinity with pEC50 values of 7.70 and 8.17 for H4R and H1R, respectively, and corresponding pKi values of 7.55 and 8.11. VUF-6884 competitively binds to the orthosteric site of the H4R, effectively displacing histamine, while demonstrating inverse agonist properties at the H1R. This compound is suitable for research applications related to histamine signaling and receptor pharmacology. -
H1R-H4R Agonist
Amthamine is an agonist of the histamine receptors H1R and H4R. This compound has been shown to induce liver congestion and necrosis of liver cells, making it a valuable tool for studying hepatotoxicity associated with H1R-H4R agonism. Its application in research can provide insights into the physiological and pathological roles of histamine signaling in liver-related conditions. -
Histamine H1 Receptor Antagonist
Mizolastine dihydrochloride is a potent histamine H1 receptor antagonist, primarily utilized in the treatment of allergic reactions. This second-generation antihistamine exhibits high affinity and specificity for peripheral H1 receptors, leading to effective inhibition of mRNA expression of pro-inflammatory factors such as VEGF165, VEGF120, TNF-α, and KC. Mizolastine dihydrochloride is valuable in research applications related to allergic rhinitis and chronic idiopathic urticaria. -
anti-allergic
FR-A-19 is a potent histamine H2-agonist, exhibiting IC50 values of 0.02 μM, 0.015 μM, and 0.008 μM against arpromidine, BUA-75, and FRA-19, respectively. This compound demonstrates significant anti-allergic properties and can be utilized in research aimed at understanding and mitigating allergic responses. Its mechanistic action on histamine receptors makes it a valuable tool for studies in allergy and inflammation. -
Histamine Receptor Control
Meclizine N-oxide is a metabolite of the histamine H1 receptor antagonist Meclizine. It primarily functions as a modulator of histamine signaling, displaying properties that may alter receptor activity. This reagent is useful in research applications focused on histamine-related pathways, such as those involved in allergy responses, vestibular function, and motion sickness. -
Histamine Receptor Antagonist
APD-916 is an H3 receptor antagonist that exhibits favorable pharmacokinetic properties. This compound has demonstrated the ability to enhance wakefulness in various animal models following oral administration. Research applications include studying sleep-wake regulation and exploring potential therapeutic effects in sleep disorders. -
H1 Receptor Antagonist
NBI-75043 is a selective H1 receptor antagonist that modulates histamine signaling pathways. It demonstrates efficacy in blocking histamine-induced effects, making it a valuable tool for investigating allergic responses and other histamine-related conditions. This compound is applicable in research focused on immunology, neurobiology, and pharmacology, particularly in the development of therapeutics for allergic diseases. -
Stable Isotope
Loratadine-d4-1 is a deuterium-labeled derivative of Loratadine, a selective inverse agonist of peripheral H1-histamine receptors. With an IC50 value exceeding 32 μM, Loratadine exhibits significant biological activity, including anti-dengue virus (DENV) effects and the inhibition of immunologic release of inflammatory mediators. This stable isotope reagent is valuable for mechanistic studies, pharmacokinetic evaluations, and research applications in allergy and inflammatory response investigations. -
H3R Antagonist
A-317920 is a selective and potent antagonist of the histamine H3 receptor (H3R), demonstrating a pKi value of 9.2 for the rat and 7.0 for the human H3R, reflecting over 130-fold selectivity for the rat receptor. This compound has been shown to enhance cognitive function through blockade of H3R activity. A-317920 is valuable for research focused on cognition, neuropharmacology, and the role of histamine receptors in the central nervous system. -
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 H1-receptor Blocker
Oxomemazine hydrochloride is a phenothiazine-derived histamine H1-receptor blocker with significant antimuscarinic properties. It acts as a selective antagonist at the muscarinic M1 receptor, exhibiting approximately 20-fold variance in affinity compared to the M2 receptor (Ki= 84 nM for M1 and Ki= 1.65 μM for M2). This compound serves as an antihistamine and anticholinergic agent, making it valuable for research focused on cough treatment and related respiratory conditions. -
Histamine H2 Receptor Antagonist
Osutidine is a selective antagonist of the histamine H2 receptor, effectively inhibiting histamine-induced gastric acid secretion. This compound exhibits insurmountable and non-competitive inhibition, while not influencing [14C]aminopyrine accumulation prompted by carbachol or dibutyryl-cAMP. Osutidine is particularly useful for investigating gastric mucosal injury and related gastrointestinal disorders. -
Histamine Receptor Antagonist
JNJ-39220675 is a selective antagonist of the histamine H3 receptor, specifically designed to penetrate the blood-brain barrier. This compound has demonstrated efficacy in modulating alcohol stimulation and reward, effectively reducing alcohol consumption and preference in alcohol-preferring rat models. Notably, JNJ-39220675 does not influence the ataxic effects of alcohol, the elimination rate of ethanol, or the dopamine release associated with alcohol exposure. -
H1-antihistamine
AHR-14310C is a potent, long-acting H1-antihistamine that functions by selectively blocking H1 receptors. It demonstrates efficacy in preventing antigen-induced mucus formation, making it a valuable tool for research on allergic reactions and respiratory conditions. This compound is useful in studies examining the mechanisms of histamine-related responses and provides insights for developing new antihistamine therapies. -
Histamine H2 Receptor Antagonist
BMY-25368 is a selective histamine H2 receptor antagonist primarily designed to inhibit gastric acid secretion. It functions by competitively blocking gastric secretion induced by histamine, as well as by other stimulants such as Pentagastrin and Bethanechol. This compound serves as a valuable tool for research applications in studying gastric physiology and the regulation of acid secretion. -
H3R Antagonist
VUF 5681 dihydrobromide is an antagonist of the histamine H3 receptor, exhibiting neutral antagonistic properties as well as partial agonist functionality. This compound effectively inhibits the effects of Thioperamide, making it a valuable tool in investigating histamine receptor signaling. VUF 5681 dihydrobromide is utilized in research focused on central nervous system diseases, contributing to studies of neuropharmacology and receptor interactions. -
H1 receptor antagonists
Phenindamine tartrate is a potent histamine H1-receptor antagonist. It exhibits significant antihistaminic activity, making it effective in alleviating allergic symptoms by blocking the effects of histamine. This compound is used in research to study allergic reactions, respiratory disorders, and other conditions associated with histamine release. -
Histamine Receptor Antagonist
GSK189254A hydrochloride is a potent and selective antagonist of the histamine H3 receptor, exhibiting pKi values of 9.59-9.90 for human H3 and 8.51-9.17 for rat H3. This compound is useful in research applications focused on modulating neurotransmission and exploring the role of histamine in various physiological processes. Its selective antagonistic properties make it a valuable tool for studying the therapeutic potential in conditions such as neurodegeneration and cognitive disorders.
