Catalog No.
Product Name
Application
Product Information
Citations
-
D2/H1 Antagonist
Thiethylperazine is a potent antagonist of dopamine D2 and histamine H1 receptors. This phenothiazine derivative exhibits notable anti-emetic, antipsychotic, and antimicrobial properties, making it valuable in various therapeutic contexts. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β (Aβ) load in murine models, thus highlighting its potential relevance in neurodegenerative research. -
Histamine-1 (H1R) Receptor Agonist
2-Pyridylethylamine hydrochloride functions as an agonist for the histamine-1 (H1R) receptor. This compound has demonstrated the ability to mitigate joint injury induced by formalin in rat models. Additionally, it serves as a valuable tool for investigating spinal cord neuropeptide Y (NPY) release, contributing to research in neurobiology and pain mechanisms. -
Histamine 4 Receptor Agonist
4-Methylhistamine dihydrochloride is a potent and selective agonist of the histamine H4 receptor (H4R), exhibiting a Ki value of 50 nM. It demonstrates greater than 100-fold selectivity for hH4R compared to other histamine receptor subtypes, with an effective activation pEC50 of 7.4. This compound is valuable for research in cancer, inflammation, and immunology, particularly in studies related to lung cancer and skin inflammation. -
Histamine Receptor Antagonist
Adriforant hydrochloride is a potent antagonist of the histamine H4 receptor, exhibiting a binding affinity (Ki) of 2.4 nM and functional antagonism with a Ki of 1.56 nM. This compound is valuable for research applications related to immune modulation and inflammation, providing insights into histamine signaling pathways. Its specificity for H4 receptors positions it as a useful tool for studying various biological processes influenced by histamine. -
Antihistamine Agent
Hydroxyzine is an antihistamine agent that primarily targets histamine H1 receptors and functions as a serotonin antagonist. This compound exhibits anxiolytic properties, making it valuable for research applications related to generalized anxiety disorder. Its dual action provides insights into the interplay between histamine and anxiety regulation in various biological contexts. -
H1 receptor Antagonist
Mianserin is an orally active antagonist of the H1 receptor, exhibiting unique pharmacological properties. In addition to its primary mechanism, Mianserin activates κ-opioid and octopamine receptors, leading to the phosphorylation of ERK1/2 and CREB. This compound has demonstrated effects on social and exploratory behavior, as well as raising electroconvulsive thresholds. Mianserin is valuable for research into neurological disorders including depression and epilepsy. -
H1-Receptor Antihistamine
Methapyrilene hydrochloride is an orally active H1-receptor antihistamine that also exhibits anticholinergic properties. This pyridine-derived compound is primarily utilized in research related to allergic responses and histamine-mediated processes. Additionally, due to its hepatotoxic effects, methapyrilene hydrochloride can serve as a tool for studying periportal hepatic necrosis in vivo, providing insights into liver pathology and toxicity mechanisms. -
H3 Agonist
(R)-(-)-α-Methylhistamine dihydrochloride is a potent and selective agonist for the H3 histamine receptor, demonstrating a Kd of 50.3 nM. This compound has been shown to enhance memory retention and reduce memory impairment in preclinical models, making it valuable for research focused on cognitive function and neurological disorders. Its ability to penetrate the blood-brain barrier further supports its potential in brain-related studies. -
Histamine H2-receptor Antagonist
Tiotidine is a selective antagonist of the histamine H2 receptor, exhibiting a pA2 value of 7.3-7.8 in the guinea pig right atrium. This compound demonstrates low affinity for H1 and H3 receptors, allowing for targeted modulation of H2 receptor activity. Tiotidine is primarily used in research applications related to gastric acid secretion and histamine-related signaling pathways. -
H1 Histamine Receptor Antagonist
Clemastine is a potent H1 histamine receptor antagonist with the ability to cross the blood-brain barrier, providing effective antiallergic properties. In addition to its antihistamine action, Clemastine also interacts with muscarinic acetylcholine receptors, specifically M1 and M4 subtypes. This compound demonstrates significant biological activities, including promoting central nervous system remyelination, activating autophagy, and exhibiting anti-apoptotic and neuroprotective effects. Its anti-inflammatory properties further highlight its potential in various research applications related to allergy, neurodegeneration, and inflammation. -
Histamine Receptor Agonist
N-Methylhistamine dihydrochloride is a selective agonist of the histamine H3 receptor, playing an important role in the study of mastocytosis. This compound is instrumental in the diagnosis and management of this condition. Additionally, it acts as a valuable biomarker for evaluating mast cell accumulation in clinical assessments. -
Histamine H3/H4 Receptor Agonist
Imetit dihydrobromide is a potent and selective agonist of the histamine H3 and H4 receptors, exhibiting binding affinities with Ki values of 0.3 nM and 2.7 nM, respectively. This compound effectively mimics histamine, inducing morphological changes in eosinophils, with an EC50 value of 25 nM. Imetit dihydrobromide is valuable for researching mechanisms related to allergic responses and inflammation modulation. -
Histamine Metabolite
1-Methyl-4-imidazoleacetic acid hydrochloride is a stable histamine metabolite formed through the oxidation of N-methylhistamine. This compound serves as a valuable tool in research investigating histamine metabolism and its physiological roles. It can be utilized in studies related to receptor interactions and the biochemical pathways involving histamine. -
H1 Receptor Antagonist
Tecastemizole, a major metabolite of Astemizole, functions as a potent and selective antagonist of the H1 receptor. It exhibits notable anti-inflammatory properties, making it valuable for research into allergic responses and inflammation-related conditions. This compound is useful for studies investigating the modulation of histamine signaling pathways and their implications in various biological processes. -
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. -
H1 Receptor Antagonist
Antazoline is a histamine H1 receptor antagonist that exhibits anticholinergic and antiviral activities. It functions by competitively inhibiting histamine binding to H1 receptors, thereby mitigating physiological allergic responses. This compound demonstrates a dose-dependent reduction of HBV DNA levels in HepAD38 and Huh7 cell lines, with EC50 values of 2.910 μmol/L and 2.349 μmol/L, respectively. Additionally, Antazoline may possess anti-arrhythmic properties relevant to acute myocardial infarction. Its diverse biological activities make it a valuable reagent for research in cardiovascular diseases and hepatitis B virus infections. -
Anticholinergic Agent
Benztropine is an orally active anticholinergic agent that effectively crosses the blood-brain barrier. It serves as a dopamine re-uptake inhibitor and a human D2 dopamine receptor allosteric antagonist, making it relevant in Parkinson's disease research. Additionally, Benztropine demonstrates potential anti-cancer stem cell activity, enhancing its applicability in oncology studies. -
Antipsychotic Agent
Levomepromazine maleate is an N-substituted phenylthiazine compound that acts as an antipsychotic agent primarily targeting dopamine receptors. This compound exhibits significant sedative properties and is also a potent inhibitor of CYP2D6, making it a valuable tool for investigating the pharmacological mechanisms underlying schizophrenia. Its multifaceted receptor-blocking activity contributes to its role in research applications related to neuropsychiatric disorders. -
Histamine H2 Antagonist
Zolantidine dimaleate is a potent and selective histamine H2 antagonist that effectively crosses the blood-brain barrier. This compound demonstrates significant antinociceptive activity, making it valuable for research focused on pain modulation and related neurological studies. Zolantidine dimaleate can be utilized in various experimental settings to investigate the mechanisms of pain relief and the role of histamine signaling in the central nervous system. -
H1 Histamine Receptor Antagonist
Thonzylamine is an orally active H1 histamine receptor antagonist that exhibits notable antihistaminic and antianaphylactic properties. This compound is valuable for research involving hypersensitivity diseases, as well as conditions such as nasal congestion and allergic conjunctivitis. Its targeted action on the H1 receptor makes it a useful tool in the study of various allergic disorders. -
Histamine H4 Receptor Agonist
VUF 8430 dihydrobromide is a potent and selective agonist of the histamine H4 receptor, exhibiting a Ki of 31.6 nM and an EC50 of 50 nM. This compound is valuable for investigating the role of the H4 receptor in immune response modulation and inflammation. Its specificity makes it a useful tool for research into histamine-related disorders and potential therapeutic applications in allergic and inflammatory conditions. -
histamine H4 receptor antagonist.
Seliforant is a selective histamine H4 receptor antagonist that is primarily utilized in the study of immune response modulation and allergic conditions. By inhibiting the H4 receptor, Seliforant demonstrates potential anti-inflammatory and anti-allergic activities, making it a valuable tool for researching pathways related to allergic diseases and immune regulation. Its oral bioavailability allows for convenient administration in various in vivo experimental settings. -
Histamine Antagonist
Dimethindene maleate is a selective histamine H1 antagonist known for its antihistaminic properties. It effectively mitigates hypersensitivity reactions, making it valuable in the study of allergic responses and other histamine-related conditions. Researchers utilize Dimethindene maleate to explore its effects on inflammation and allergic pathways. -
H1 Receptor Antagonist
Olopatadine is an orally active and selective antihistamine that functions as an H1 receptor antagonist and mast cell stabilizer. It effectively inhibits the release of pro-inflammatory mediators from human conjunctival mast cells, making it instrumental in the study of allergic conjunctivitis. Olopatadine is valuable in researching the mechanisms of allergic responses and the management of allergic symptoms. -
Histamine H1-Receptor Antagonist
Niaprazine is a selective histamine H1-receptor antagonist. It exhibits both antihistamine and antiserotonin properties, making it a valuable compound for investigating sleep disorders and related biological effects. Its ability to modulate neurotransmitter signaling is relevant for research into conditions such as insomnia and anxiety. -
H3R Inverse Agonist
H3R Antagonist 1 Hydrochloride is an inverse agonist of the histamine receptor 3 (H3R). This compound has been shown to elevate the expression levels of myelin-associated glycoprotein (MAG) and myelin basic protein (MBP) in differentiating oligodendrocytes. It serves as a valuable reagent for research investigating myelination processes and potential therapeutic strategies for multiple sclerosis. -
H3 Agonist
(R)-(-)-α-Methylhistamine dihydrobromide is a potent and selective agonist of the H3 histamine receptor, exhibiting a Kd of 50.3 nM. This compound has been shown to enhance memory retention and alleviate memory impairment in rat models, making it a valuable tool for research on cognitive function and neuropharmacology. Its ability to penetrate the blood-brain barrier further establishes its utility in neurological studies. -
H1/ H2 Agonist
HTMT dimaleate is a potent agonist of histamine H1 and H2 receptors. It exhibits significantly enhanced activity, being 40,000 times more effective than histamine in mediating H2 receptor effects in natural suppressor cells. This compound is valuable for research focused on immunological responses and histamine receptor signaling pathways. -
Histamine H2 Receptor Antagonist
BMY-25368 hydrochloride is a potent antagonist of the histamine H2 receptor, functioning primarily as a gastric acid secretion inhibitor. By competitively inhibiting gastric secretion stimulated by histamine, it also effectively antagonizes secretion induced by Pentagastrin, Bethanechol, and food intake. This reagent is applicable in research focused on understanding gastric physiology and the modulation of acid secretion. -
Histamine Dehydrogenase
Histamine dehydrogenase, Microorganism (EC 1.4.99) is a homodimeric enzyme that facilitates the oxidative deamination of histamine in conjunction with an electron carrier. This enzyme plays a crucial role in histamine metabolism and its regulation within biological systems. It is applicable in studies related to neurotransmission, immune response, and the mechanisms underlying allergic reactions. Researchers may utilize this enzyme to explore its potential roles in various physiological and pathological processes involving histamine. -
H1 Receptor Antagonist
Dimethindene is a selective histamine H1 receptor antagonist known for its ability to inhibit histamine-mediated processes. This compound has been shown to impair cutaneous wound healing through its antagonistic action. Additionally, Dimethindene is capable of blocking potassium (K+) currents, making it valuable for research applications focused on skin physiology and ion channel modulation. -
Histamine 1 Antagonist
Azelastine is a potent and selective antagonist of the histamine H1 receptor. It demonstrates significant antihistaminic activity, making it valuable for research into allergic rhinitis and asthma. Additionally, Azelastine has potential applications in studying diabetic hyperlipidemia and SARS-CoV-2-related pathophysiology. -
Histamine H2 Receptor Antagonist
Aminopotentidine is a potent antagonist of the histamine H2 receptor, exhibiting KB values of 220 nM for human H2 receptors and 280 nM for guinea pig H2 receptors. This compound is utilized in studying gastric acid secretion and has applications in gastrointestinal research. Additionally, it serves as a valuable precursor for the synthesis of [125I] iodo derivatives, facilitating radiolabeling studies. -
Stable Isotope
(Rac)-Levomepromazine-d3 hydrochloride is a labeled form of the racemic compound Methotrimeprazine, belonging to the phenothiazine class. This reagent exhibits antagonist activity at various neurotransmitter receptor sites, including dopaminergic, cholinergic, serotonin, and histamine receptors. It is primarily used as a stable isotope for research applications, enabling in-depth studies of pharmacological interactions and the metabolic pathways of related compounds. -
Histamine Receptor Agonist
LML134 is a highly selective inverse agonist of the Histamine 3 receptor (H3R), demonstrating an impressive affinity with Ki values of 0.3 nM for hH3R cAMP and 12 nM for hH3R binding. This compound exhibits rapid brain penetration, resulting in significant H3R occupancy and a swift disengagement from its target. LML134 holds promise for investigating therapeutic strategies for sleep disorders by modulating histaminergic signaling pathways. -
Antihistamine Agent
Brompheniramine is a selective histamine H1 receptor antagonist primarily utilized as an antihistamine agent. With a Kd of 6.06 nM, it effectively alleviates symptoms of allergic rhinitis. In addition to its antihistaminic properties, brompheniramine exhibits anticholinergic, antidepressant, and anesthetic effects, making it suitable for various research applications related to allergy and inflammation. The compound also interacts with hERG, calcium, and sodium channels, with IC50 values of 0.90 μM, 16.12 μM, and 21.26 μM, respectively. -
Histamine H1 Antagonist
Triprolidine hydrochloride is a potent histamine H1 antagonist that effectively alleviates symptoms associated with allergic conditions. It exhibits properties that provide spinal cord motor and sensory blockade, making it valuable for research applications in allergic rhinitis and other histamine-mediated disorders. This compound facilitates the study of antihistamine effects and their underlying mechanisms in various biological contexts. -
Histamine H4 Receptor Agonist
ST-1006 is a potent agonist of the histamine H4 receptor, characterized by a pKi value of 7.94. This compound exhibits significant anti-inflammatory activity, making it a valuable tool for research into inflammatory processes and related diseases. Its potential applications include studies in immunology and the modulation of allergic responses, providing insights into therapeutic strategies targeting the H4 receptor pathway. -
Histamine H1-Receptor Blocker
Oxomemazine is a phenothiazine-derived antagonist targeting the histamine H1 receptor. It exhibits notable antihistamine and anticholinergic properties, making it useful in research related to cough treatments. Additionally, Oxomemazine demonstrates a selective blockade of the muscarinic M1 receptor with a significant affinity difference compared to the M2 receptor. Studies have shown its protective effects against anaphylactic microshock in guinea pigs, highlighting its potential for further pharmacological investigation. -
H1 Receptor Antagonist
Cetirizine Impurity C dihydrochloride is an impurity of cetirizine, which acts as a selective H1 receptor antagonist. This compound demonstrates significant inhibition of histamine activity, contributing to its use in studies of allergic responses and histamine-mediated disorders. Its characterization is essential for ensuring the purity and efficacy of cetirizine in pharmaceutical formulations and research applications. -
Sigma Receptor Agonist
CB-64D is a dual agonist of sigma receptor 1 and sigma receptor 2, exhibiting Ki values of 16.5 nM and 3063 nM, respectively. It has been shown to induce apoptosis in SK-N-SH cancer cells, highlighting its potential role in cancer research. This compound can serve as a valuable tool for investigating the biological functions of sigma receptors and their implications in various pathologies. -
Stable Isotope
Perphenazine-d6 fumarate is a deuterated derivative of Perphenazine, primarily acting as a dopamine D2 and D3 receptor antagonist with Ki values of 0.56 nM and 0.43 nM, respectively. Additionally, it demonstrates affinity for the 5-HT2A and Alpha-1A adrenergic receptors. This compound exhibits notable biological activities, including the inhibition of cancer cell proliferation and the induction of apoptosis. Perphenazine-d6 fumarate is useful in research addressing mental health disorders, cancer mechanisms, and inflammatory processes. -
Dopamine Receptor Antagonist
Perphenazine dihydrochloride is a potent antagonist of dopamine receptors, primarily targeting D2 and D3 subtypes, with Ki values of 0.56 nM and 0.43 nM, respectively. Additionally, it exhibits activity against 5-HT2A and α1A adrenergic receptors. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and inducing apoptosis. Perphenazine dihydrochloride is particularly useful in research focused on mental disorders, oncology, and inflammatory processes. -
CB2R Agonist
CB2R agonist 4 is a selective agonist for the cannabinoid receptor 2 (CB2R), exhibiting an EC50 value of 6.9 μM. This compound can induce cellular apoptosis, promote reactive oxygen species (ROS) production, and contribute to protein misfolding. Due to its cytotoxic effects observed in various tumor cell lines, CB2R agonist 4 is a valuable tool for cancer research applications. -
Stable Isotope
D-Mannitol-d is a deuterium-labeled form of D-Mannitol, a polyol with significant applications in both food and pharmaceutical research. It functions primarily as an osmotic diuretic, utilized to alleviate tissue edema, while also promoting the absorption of calcium and magnesium through cecal fermentation. Additionally, D-Mannitol-d is instrumental in studies related to metabolic processes, including the induction of brown fat formation via β3-adrenergic receptor activation, potentially contributing to improved insulin sensitivity and reduced blood glucose levels. Its unique properties make it valuable for maintaining osmotic pressure in plant cell cultures, particularly when cellular integrity is compromised. -
CXCR-4 Inhibitor
SSB-2548 is a selective inhibitor of the chemokine receptor CXCR-4. It has demonstrated significant efficacy in inhibiting the proliferation and migration of acute myeloid leukemia cells, while also promoting apoptosis. Its favorable gastrointestinal absorption profile makes SSB-2548 a valuable tool for investigating the underlying mechanisms of leukemia and exploring potential therapeutic interventions. -
α-1A Adrenergic Receptor Agonist
Dabuzalgron hydrochloride is a selective agonist of the α-1A adrenergic receptor, primarily indicated for the management of urinary incontinence. This compound has demonstrated protective effects against Doxorubicin-induced cardiotoxicity by maintaining mitochondrial integrity and function. Its pharmacological properties make it a valuable tool in research focused on adrenergic signaling and cardiac health. -
5-HT2/D1/D2 Antagonist
Olanzapine hydrochloride is a selective antagonist of serotonin receptors (5-HT2A/2C, 5-HT3) and dopamine receptors (D1, D2). It exhibits high affinity binding to various targets, including H1, muscarinic M1-5, and adrenergic α1 receptors, contributing to its pharmacological profile. This atypical antipsychotic is primarily used in research focusing on neuropharmacology, the treatment of schizophrenia, and mood disorders, providing valuable insights into the modulation of neurotransmitter systems. -
Platelet Aggregation Inhibitor
2'-Hydroxyflavanone is a flavanone that functions as a platelet aggregation inhibitor. It demonstrates significant bioactivity by inhibiting platelet aggregation induced by arachidonic acid and adenosine diphosphate, with IC50 values of 47.8 μM and 147.2 μM, respectively. Additionally, 2'-hydroxyflavanone has been implicated in inhibiting cancer cell proliferation and inducing apoptosis, making it valuable for research in cancer and inflammatory pathways.
