Catalog No.
Product Name
Application
Product Information
Citations
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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. -
H1 Receptor Antagonist
Cyclizine hydrochloride is a selective antagonist of the histamine H1 receptor. It is primarily utilized in research focusing on the mechanisms underlying nausea, vomiting, and dizziness. This compound's ability to inhibit H1 receptor activity makes it a valuable tool for studies in the fields of neuropharmacology and gastroenterology. -
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. -
Antihistamine
Bromodiphenhydramine is a potent antihistamine that also exhibits antimicrobial properties. It effectively inhibits a wide range of both Gram-negative and Gram-positive bacteria. This dual functionality makes bromodiphenhydramine a valuable reagent for research on cutaneous allergies and related inflammation studies. -
Antihistamine
Dexchlorpheniramine is a potent histamine H1 receptor antagonist with the ability to penetrate the blood-brain barrier. This compound exhibits anticholinergic properties and is primarily utilized in research related to allergic responses and antihistamine efficacy. Its mechanism makes it valuable for studying the effects of histamine in various biological contexts. -
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. -
Histamine H4 Receptor Agonist
ST-1006 Maleate is a potent agonist of the histamine H4 receptor, exhibiting a pKi value of 7.94. This compound demonstrates significant anti-inflammatory activity, making it valuable for research focused on immune response modulation and allergic conditions. Its ability to selectively activate the H4 receptor positions ST-1006 Maleate as a promising tool for investigating histamine-related biological processes. -
Histamine H2 Receptor Antagonist
IT 066 hydrochloride is a potent Histamine H2 receptor antagonist. This compound demonstrates antioxidant activity and has been shown to protect against acute gastric mucosal injury due to ischemia-reperfusion in rat models. Additionally, IT 066 hydrochloride effectively inhibits secretagogue-induced gastric acid secretion and exhibits a long-lasting anti-lesion effect on experimental gastric and duodenal lesions. It is a valuable tool for researching gastrointestinal diseases and understanding the mechanisms of gastric protection and acid regulation. -
Stable Isotope
Fenspiride-d5 is a deuterium-labeled derivative of Fenspiride, an orally active non-steroidal anti-inflammatory agent. It functions primarily as an H1-histamine receptor antagonist and exhibits inhibitory activity against phosphodiesterase 3 (PDE3), phosphodiesterase 4 (PDE4), and phosphodiesterase 5 (PDE5), with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. This reagent is valuable for investigating respiratory diseases and understanding the pharmacodynamics of its parent compound in biochemical research. -
Histamine H3 Receptor Agonist
VUF5207 is a partial agonist of the histamine H3 receptor, playing a key role in modulating neurotransmitter release in the central nervous system. This compound is utilized in research applications investigating the physiological and pathophysiological roles of histamine signaling, as well as potential therapeutic strategies for conditions such as cognitive disorders and sleep regulation. Its unique properties make it a valuable tool for studying histaminergic mechanisms and their implications in neurobiology. -
Antihistamine Agent
Propiomazine hydrochloride is an orally active antihistamine agent that primarily targets histamine H1 receptors. It is recognized for its potent stimulation of prolactin release, mediated through the antagonism of dopaminergic pathways, and has the capability to inhibit luteinizing hormone secretion. Its applications include anesthesia support, the management of mental disorders, anxiety-induced sedation, and research into insomnia. -
Histamine Receptor
Vapitadine is a non-sedative antihistamine that selectively targets histamine receptors, providing relief from itching associated with atopic dermatitis. This compound demonstrates efficacy in managing allergic reactions without the sedative effects commonly seen with traditional antihistamines. Its application in research focuses on understanding the pathways involved in allergic responses and evaluating potential treatments for skin conditions characterized by histamine release. -
H1 Receptor Antagonist
Cyclizine lactate is a piperazine derivative that selectively antagonizes the histamine H1 receptor. It exhibits potent antiemetic properties, making it useful for research related to nausea, vomiting, and motion sickness. This compound is often utilized in studies investigating the pharmacological mechanisms of vertigo and related disorders. -
Histamine H3 Receptor Antagonist
Proxyfan Oxalate is a potent antagonist of the histamine H3 receptor, demonstrating Ki values of 2.9 nM and 2.7 nM for rat and human receptors, respectively. It exhibits over 1000-fold selectivity for H3 receptors compared to other histamine receptor subtypes. This specificity makes Proxyfan Oxalate a valuable tool for research applications focused on neurological and psychiatric disorders related to histamine signaling. -
5-HT Receptor Antagonist
Asenapine citrate is a 5-HT receptor antagonist that exhibits potent activity against serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4), and histamine receptors (pKi: 8.2-9.0). This atypical antipsychotic compound is primarily utilized in research focusing on schizophrenia and bipolar disorder, helping to elucidate the mechanisms of these neuropsychiatric conditions. -
Stable Isotope
Ebastine-d5 is a deuterium-labeled derivative of Ebastine, a second-generation histamine H1 receptor antagonist. It is utilized in research to study the pharmacokinetics and metabolic pathways of Ebastine, particularly in the context of allergic rhinitis and chronic idiopathic urticaria. This stable isotope provides a valuable tool for investigating the dynamics of histamine receptor interactions and drug efficacy in various biological systems. -
Histamine H3 Receptor Inverse Agonist
FUB 465 is an orally active inverse agonist targeting the histamine H3 receptor, exhibiting a pKi of 6.2. This compound is instrumental in investigating central nervous system disorders, offering insights into the modulation of histamine signaling pathways. Its activity may facilitate the development of novel therapeutic strategies for conditions associated with H3 receptor dysfunction. -
Histamine H1 Antagonist
Methapyrilene fumarate is a histamine H1 receptor antagonist known for its sedative properties. This compound exhibits potential analgesic effects, making it of interest in various research applications centered on pain management and sleep disorders. Its ability to modulate histamine signaling positions it as a valuable tool in pharmacological studies. -
Antihistamine
Bromodiphenhydramine hydrochloride is a potent antihistamine that exhibits antimicrobial properties. It effectively inhibits a wide range of Gram-negative and Gram-positive bacteria, making it a valuable compound for research involving cutaneous allergies and related skin responses. Its dual action as an antihistamine and antimicrobial agent provides insights into allergic reactions and potential therapeutic approaches. -
H2-Histamine Antagonist
DA 4626 is a competitive antagonist of the H2-histamine receptor. It effectively inhibits adenylate cyclase activity, exhibiting a KB value of 40 nM. This compound is utilized in research related to gastrointestinal physiology and histamine receptor biology, providing insights into the mechanisms of action associated with H2 receptor signaling. -
Histamine H1 Receptor Antagonist
Dacemazine is a phenothiazine derivative that functions as a histamine H1 receptor antagonist. This compound demonstrates local anesthetic properties and is effective in reducing spasms triggered by acetylcholine and histamine. Its mechanisms highlight its potential applications in pharmacological research related to allergic reactions and neuromuscular disorders. -
Antihistamine Agent
Propiomazine maleate is an orally active antihistamine agent that primarily acts as a potent prolactin (PRL) release stimulant through dopaminergic system antagonism. This compound inhibits luteinizing hormone (LH) secretion, making it valuable in various research applications. Propiomazine maleate is commonly utilized for anesthesia assistance, management of mental disorders, and anxiety-induced sedation, as well as in studies related to insomnia. -
Histamine H1 Antagonist
Noberastine maleate is a potent Histamine H1 antagonist that exhibits specific peripheral antihistamine activity. This compound effectively blocks the action of histamine in peripheral tissues, making it useful in research focused on allergic responses and related conditions. Its application in scientific studies includes exploring mechanisms of allergic reactions and developing therapeutic strategies for allergic disorders. -
Histamine H3 Antagonist
Carcinine, a selective and orally active histamine H3 receptor antagonist, has a Ki of 0.2939 μM. It demonstrates key biological activities, including reducing histamine content, exhibiting antioxidant properties, and displaying neuroprotective effects. Additionally, Carcinine has shown to have a positive inotropic effect and can lower blood sugar and lipid levels. This compound is valuable for research in fields such as inflammation, neurology, cardiovascular health, and metabolic disorders, including conditions like retinal damage, seizures, and diabetes. -
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 H3-Receptor Antagonist
Clobenpropit is a potent antagonist of the histamine H3 receptor. By blocking this receptor, Clobenpropit decreases dopamine release while increasing histamine levels in the hypothalamus. It exhibits antipsychotic-like activities and has been shown to exert resuscitating effects in rat models of hemorrhagic shock, making it valuable for research in neuropharmacology and potential therapeutic applications in psychiatric disorders. -
Antihistamine
Loratadine n-oxide is a metabolite of the antihistamine Loratadine, acting as a competitive antagonist of peripheral histamine H1 receptors. This compound exhibits antihistaminic activity, making it useful in research focused on allergic responses and related pathways. Its role in understanding the pharmacokinetics and pharmacodynamics of antihistamines provides valuable insights for studies on allergy treatment and management. -
Antihistamine
Efletirizine is an orally active antihistamine that exhibits high selectivity and affinity for the H1 receptor. It is primarily utilized in research related to allergic diseases, making it a valuable tool for studying histamine-mediated responses and developing therapeutic strategies. Its potency in blocking H1 receptor activity provides insights into allergy pathology and treatment options. -
Histamine H(3) Receptor Agonist
VUF 8328 is a potent histamine H(3) receptor agonist that selectively activates this receptor, influencing various neurotransmitter systems. It effectively inhibits electrically-evoked [3H]-noradrenaline release from rat cortical slices, demonstrating its potential impact on neurotransmission. This compound holds promise for research applications in central nervous system disorders, offering insights into the modulation of histaminergic signaling. -
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. -
Histamine H1 Receptor Antagonist
Bepotastine tosylate is a selective, orally active antagonist of the histamine H1 receptor. This compound effectively inhibits the expression of nerve growth factor (NGF), making it relevant in the study of allergic conditions. Bepotastine tosylate is commonly utilized in research focused on allergic rhinitis, allergic conjunctivitis, and urticaria or pruritus. -
Histamine Receptor
Talastine hydrochloride is an antihistamine that primarily targets histamine receptors, exerting significant antiallergic activity. It is utilized for the relief of various allergic symptoms, offering a potential therapeutic option for managing allergic conditions. Research has noted possible adverse reactions, such as rash, which may highlight variability in individual sensitivity to the compound. -
Antihistamine Agent
Alinastine is an antihistamine agent that functions primarily as an H1 receptor antagonist. It demonstrates efficacy in alleviating allergic symptoms by inhibiting the action of histamine, a key mediator in allergic reactions. This compound is utilized in research to explore its roles in anti-allergic therapies and the underlying mechanisms of histamine-related conditions. -
Histamine Receptor Antagonist
Doxylamine is a first-generation antihistamine that acts as a histamine H1 receptor antagonist. It is utilized for its sedative properties, making it an effective hypnotic agent, and also exhibits local analgesic effects. This compound is commonly applied in research focusing on sleep disorders, allergy treatments, and the modulation of histaminergic pathways. -
Histamine H3-Receptor Antagonist
Ciproxifan hydrochloride is a selective antagonist of the histamine H3-receptor, exhibiting a potent competitive binding capability with an IC50 of 9.2 nM. Its low affinity for other receptor subtypes enhances its specificity. This compound is valuable for research in aging disorders and Alzheimer's disease, providing insight into the role of histamine signaling in neurodegenerative processes. -
Antihistamine
Dioxopromethazine is an orally active antihistamine that targets H1 receptors. It effectively manages allergic reactions and alleviates symptoms associated with asthma. This compound is valuable in research focusing on respiratory disorders and the antihistaminic effects in various preclinical models. -
H1 Histamine Receptor
Dexbrompheniramine maleate is an orally active antagonist of the H1 histamine receptor. It functions as an antihistamine, effectively diminishing the physiological effects of histamine, which is implicated in allergic responses. This reagent is valuable for research applications related to hay fever, urticaria, and other histamine-mediated conditions. -
Natural Products
Embramine hydrochloride is a monoethanolamine compound that functions primarily as an antihistamine and anticholinergic agent. It effectively inhibits histamine receptors and blocks acetylcholine action, making it valuable in studies related to allergic responses and neurotransmission. This reagent is commonly utilized in research focused on understanding various natural products and their pharmacological effects. -
Histamine H3 Receptor Antagonist
AChE/BChE-IN-21 is a histamine H3 receptor antagonist that also functions as a calcium channel blocker and acetylcholinesterase inhibitor. This compound demonstrates neuroprotective properties against oxidative stress induced by H2O2 and amyloid-beta peptide Aβ1-40. Additionally, AChE/BChE-IN-21 has been shown to improve cognitive function in mouse models of Alzheimer's disease, making it a valuable tool for research into neurodegenerative disorders. -
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.
