Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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 Antagonist
(±)-Tazifylline functions as a potent and selective histamine H1 receptor antagonist. This compound exhibits long-acting biological activity, making it valuable in studies related to allergic responses, inflammation, and histamine-mediated physiological processes. Its targeted mechanism allows for exploration in various research applications, including asthma and allergic condition therapeutics. -
5-HT Receptor Inhibitor
Proxibarbal is a barbiturate derivative that acts as a selective inhibitor of the 5-HT receptor. It demonstrates notable anti-anxiety properties and is utilized in research focused on migraine headache mechanisms. This compound serves as a valuable tool for understanding serotonergic pathways and their implications in anxiety and migraine disorders. -
Histamine H2 Receptor Antagonist
FR-145715 is a selective histamine H2 receptor antagonist that exhibits specific activity against Helicobacter pylori. Its inhibition of H2 receptors contributes to its role in research studies focused on gastric lesions and related gastrointestinal disorders. This compound is valuable for investigating therapeutic strategies targeting H. pylori infection and associated pathologies. -
Histamine Receptor Control
Promethazine sulfoxide is a metabolite of the histamine H1 receptor antagonist, promethazine, formed through the action of the cytochrome P450 isoform CYP2D6. This compound exhibits potential biological activity related to histamine receptor modulation, making it relevant for research focused on allergic responses and central nervous system effects. Its involvement in metabolic pathways provides valuable insights for studies examining drug interactions and individual variability in histamine response. -
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. -
PFA Antagonist
SCH-44643 is a potent antagonist of platelet activating factor (PAF) and histamine receptors. This compound exhibits significant inhibitory activity on PAF-mediated platelet aggregation and histamine-induced responses. It is utilized in research applications focusing on inflammatory processes, cardiovascular disorders, and allergic reactions, contributing to the understanding of PAF and histamine-related pathways in various biological contexts. -
Stable Isotope
Asenapine-d3,13C is a stable isotope-labeled form of Asenapine, an atypical antipsychotic that acts as an antagonist at various serotonin, adrenoceptor, dopamine, and histamine receptors. This compound is valuable for studies investigating the pharmacokinetics and metabolism of Asenapine, particularly in the context of schizophrenia and bipolar disorder research. Its unique isotopic labeling allows for precise tracking and analysis in biochemical assays and in vivo studies. -
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 H3 Receptor Antagonist
GSK334429 is a selective, orally active non-imidazole antagonist of the histamine H3 receptor, exhibiting a pKi of 9.49 against the human H3 receptor. This compound is important for studies related to neurological disorders and may help elucidate the role of histaminergic signaling in the central nervous system. Its targeted mechanism makes it a valuable reagent for research applications involving neuropharmacology and related fields. -
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. - 5-Hydroxytryptophan (5-HTP) is a naturally occurring amino acid and chemical precursor as well as a metabolic intermediate in the biosynthesis of the neurotransmitters serotonin and melatonin from tryptophan.
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5-HT Receptor antagonist
Agomelatine is a melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist. - Alfuzosin (provided as the hydrochloride salt) is an α1 receptor antagonist used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
- Amfebutamone (Bupropion) is an atypical antidepressant and smoking cessation aid.
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Adenosine receptor antagonist
Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole. -
Dopamine Receptor antagonist
Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. - Azelastine is a potent, second-generation, selective, histamine antagonist (histamine-H1-receptor antagonist).
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β1 adrenergic receptor blocker
Bisoprolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. More specifically, it is a selective type β1 adrenergic receptor blocker. - 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.
