Catalog No.
Product Name
Application
Product Information
Citations
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histamine H2-receptor antagonist
Niperotidine is a histamine H2-receptor antagonist. -
histamine H3 receptor antagonist
GSK189254A (GSK189254) is a novel, potent and selective histamine H3 receptor antagonist with pKi values of 9.59-9.90 and 8.51-9.17 for human and rat H3, respectively. -
histamine H1 receptor antagonist
Emedastine is an orally active, selective and high affinity histamine H1 receptor antagonist with a Ki value of 1.3 nM. -
histamine H3R antagonist/inverse agonist
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. - Antihistamine-1 is a H1-antihistamine (Ki=6.9 nM) with acceptable blood-brain barrier penetration and also an inhibitor of CYP2D6 and hERG channel with IC50s of 5.4 and 0.8 μM, respectively.
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histamine 1 receptor antagonist
Decloxizine(UCB-1402; NSC289116) is a histamine 1 receptor antagonist. -
histamine H4 receptor antagonist
Toreforant is a potent and selective histamine H4 receptor (H4R) antagonist, with a Ki at the human receptor of 8.4 nM. -
histamine H3 receptor antagonist
PF-03654746 is a potent and selective histamine H3 receptor antagonist with high brain penetration. -
histamine H3 receptor antagonist
PF-03654746 Tosylate is a potent and selective histamine H3 receptor antagonist with high brain penetration. -
histamine H3 receptor antagonist
JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively. -
histamine H1 receptor antagonist
ReN 1869 hydrochloride is a novel, selective histamine H1 receptor antagonist, which demonstrates affinity to the histamine H1 receptor (guinea pig brain) with Ki of 0.19±0.04 μM and the non-selective ?? site (guinea pig brain) with Ki of 0.45 μM. -
H4R antagonist
H4R antagonist 1 is a potent and highly selective histamine H4 receptor (H4R) antagonist with an IC50 of 27 nM. -
histamine H3 receptor antagonist
Cipralisant is a potent and selective histamine H3 receptor antagonist in vivo, and an agonist in vitro, with a pKi of 9.9 for histamine H3 receptor and a Ki of 0.47 nM for rat histamine H3 receptor; Cipralisant has entered in clinical trials for the treatment of attention-deficit hyperactivity disorder. -
histamine H4 receptor inverse agonist
H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM. -
H3 receptor antagonist
Bavisant dihydrochloride is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. -
H3 receptor antagonist
Bavisant dihydrochloride hydrate is a highly selective, orally active antagonist of the human H3 receptor with a novel mechanism of action, involving wakefulness and cognition, with potential as a treatment for ADHD. -
H1-receptor antagonist
Cetirizine, a second-generation antihistamine, is a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria. -
H1 histamine receptor antagonist
Clemizole hydrochloride is an antagonist of H1 histamine receptor with an IC50 value of 8 mM for NS4B RNA binding. -
H2-receptor antagonist
Ebrotidine is a competitive H2-receptor antagonist (Ki= 127.5 nM) with a potent antisecretory activity and evidenced gastroprotection. -
Nonimidazole inverse agonist
Pitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). -
Nonimidazole inverse agonist
Pitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM). - Buclizine HCl is an antihistamine and anticholinergic of the piperazine derivative family.
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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. -
H1 receptor Antagonist
R 58639 is a selective histamine H1 receptor antagonist. It demonstrates significant biological activity in the modulation of allergic responses and cognitive processes. This compound is primarily utilized in research focusing on the pathophysiology and treatment of gastric ulcers, providing insights into the role of H1 receptor signaling in gastrointestinal biology. -
Histamine H2 Receptor Agonist
Betazole hydrochloride is a pyrazole derivative that acts as a histamine H2 receptor agonist. This compound stimulates gastric acid secretion and significantly elevates common bile duct pressure. Betazole is primarily utilized as a diagnostic agent, known as histalog, to assess gastric acid secretory capacity. -
Antihistamine
Diphenhydramine is a first-generation antihistamine that functions primarily as a histamine H1-receptor antagonist. It exhibits anti-cholinergic properties, allowing it to effectively alleviate allergic symptoms. This compound is capable of crossing the blood-brain barrier, making it valuable in neurological studies and research focused on central nervous system effects. Its diverse applications also include exploration in pharmacology and behavioral research involving sedative effects. -
Histamine 1 Receptor Blocker
Ketotifen is an orally active second-generation noncompetitive antagonist of the histamine H1 receptor, known for its role as a mast cell stabilizer. It exhibits significant biological activity by inhibiting 6-phosphogluconate dehydrogenase in vitro and displays antiviral properties against SARS-CoV-2 and the Influenza virus. Ketotifen is applicable in research focused on autoimmune encephalomyelitis (EAE) and contributes to studies aimed at preventing asthma attacks. -
Histamine Receptor Antagonist
Levocetirizine is a third-generation peripheral histamine H1-receptor antagonist. As the R-enantiomer of Cetirizine, it demonstrates a higher binding affinity for the H1 receptor compared to its S counterpart. Levocetirizine is primarily utilized in the management of allergic rhinitis and chronic idiopathic urticaria, providing effective relief from allergy-related symptoms. Its efficacy makes it a valuable tool in related pharmacological research. -
H1R-H4R Agonist
Amthamine dihydrobromide is an agonist of the histamine receptors H1R to H4R. This compound has been shown to induce liver congestion and necrosis of hepatocytes, providing a valuable model for studying the hepatotoxic effects associated with H1R-H4R activation. It is suitable for research applications focused on the roles of these receptors in liver function and pathology. -
Anti-histamine
Chlorpheniramine is an H1 antihistamine that primarily targets histamine receptors to alleviate symptoms associated with allergic reactions. It exhibits significant efficacy in reducing peripheral and central histamine-induced effects, making it a valuable tool in the study of allergic diseases and related pathophysiological processes. This compound is widely utilized in research applications focusing on allergy management and pharmacological interventions. -
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.
