Catalog No.
Product Name
Application
Product Information
Citations
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H1 Histamine Receptor Antagonist
Thonzylamine hydrochloride is an orally active H1 histamine receptor antagonist. It exhibits significant antihistaminic and antianaphylactic properties, making it valuable for investigating hypersensitivity diseases, nasal congestion, allergic conjunctivitis, and other allergic conditions. This compound is a useful tool for researchers studying the mechanisms underlying allergic responses and evaluating potential therapeutic interventions. -
Histamine Receptor Antagonist
A-331440 is a selective antagonist of the histamine H3 receptor, which plays a critical role in the regulation of neurotransmitter release through inhibition at presynaptic sites. In preclinical studies with mice subjected to a high-fat diet, A-331440 demonstrated significant dose-dependent effects on body weight and fat loss. At a dosage of 5 mg/kg, it effectively reduced body weight akin to dexfenfluramine, while a 15 mg/kg dose led to substantial reductions in body fat and enhanced insulin tolerance, resembling the metabolic profile of mice on a low-fat diet. These results indicate A-331440's potential as an antiobesity agent by influencing histaminergic pathways related to appetite control and metabolic processes. -
H1-Antihistamine
Sequifenadine is an H1-antihistamine that effectively inhibits histamine action at the H1 receptor. This compound exhibits anti-inflammatory properties and is instrumental in the research of inflammatory eye diseases associated with allergic symptoms. Its ability to mitigate allergic responses makes it a valuable tool for studying the underlying mechanisms of allergies and related ocular conditions. -
H3R Inverse Agonist
H3R antagonist 1 is an inverse agonist of the histamine receptor 3 (H3R). This compound promotes the upregulation of myelin-associated glycoprotein (MAG) and myelin basic protein (MBP) in differentiating oligodendrocytes, which is crucial for myelination processes. H3R antagonist 1 is applicable in research focused on multiple sclerosis and related demyelinating disorders, providing insight into oligodendrocyte differentiation and myelin repair mechanisms. -
Antihistamine/anticholinergic Agent
Chlorphenoxamine hydrochloride is an antihistamine and anticholinergic agent that functions as a GPCR antagonist. It exhibits potent antiviral activity against lethal viral pathogens, including SARS-CoV, MERS-CoV, and Ebola virus, with reported IC50 values of 1.1 μM against Ebola virus and 6.2 μM against Marburg virus. This compound is utilized in research related to allergic conditions, urticaria, viral infections, and the treatment of Parkinson’s disease. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine mesylate is an orally active tricyclic antihistamine and anti-5-HT agent that exhibits significant activity against decerebrate rigidity, demonstrating minimal sedative and soporific effects. This compound effectively reduces or eliminates the influence of both static and dynamic fusimotor activity on muscle spindles in decerebrate models. Dimethothiazine mesylate is relevant for research applications related to hemicrania and spasticity. -
Histamine Receptor
Aplysamine-1 is a potent antagonist of the histamine H3 receptor. This compound demonstrates significant modulation of neurotransmitter release and offers valuable insights into histamine signaling pathways. Aplysamine-1 is utilized in research exploring its potential therapeutic applications for neurological disorders and conditions related to histamine dysregulation. -
Stable Isotope
Asenapine-13C,d3 is a stable isotope-labeled form of Asenapine, a novel atypical antipsychotic. This compound acts primarily as an antagonist of serotonin, dopamine, adrenoceptors, and histamine receptors, demonstrating a range of pKi values indicative of strong binding affinity. Asenapine-13C,d3 is valuable for pharmacokinetic studies and metabolic research related to schizophrenia and bipolar disorder, providing insights into drug behavior in biological systems. -
Histamine H3 Receptor Antagonist
GT-2016 is a potent and selective antagonist of the histamine H3 receptor, exhibiting a Ki value of 43.8 nM. This compound demonstrates high selectivity for the H3 receptor over H1 and H2 receptors and is inactive against histamine methyltransferase. GT-2016 is valuable for research into neurological disorders and sleep regulation, providing insights into histaminergic signaling pathways. -
Antihistamine
Dioxopromethazine hydrochloride is a potent antihistamine that functions primarily by blocking H1 histamine receptors. It exhibits significant activity in mitigating asthmatic symptoms and is frequently utilized in research focused on allergic responses and respiratory disorders. This compound's ability to alleviate histamine-mediated effects makes it a valuable tool in the study of inflammatory pathways and therapeutic interventions. -
Antihistamine
Talastine is a potent H1-antihistamine that effectively blocks the action of histamine at H1 receptor sites. This compound is utilized in research to study allergic responses and related conditions, and may induce allergic exanthema in experimental models. Its mechanism highlights its potential role in exploring antihistamine therapies and allergy-related pharmacology. -
H1 Receptor Antagonist
Promethazine-d4 is a deuterated form of promethazine, functioning primarily as an H1 receptor antagonist. This compound exhibits antihistamine, sedative, antiemetic, anticholinergic, and anti-motion sickness activities. It is widely utilized in research applications focused on histamine-related disorders and the pharmacological study of sedation and motion sickness. -
Isomer of Dropropizine
(+)-Dropropizine is an isomer of Dropropizine that functions as an orally active histamine receptor inhibitor, exhibiting notable anti-allergic properties. This compound has been shown to alleviate cough by modulating neuropeptides associated with the cough reflex and by interfering with the activation of peripheral sensory nerve endings. (+)-Dropropizine holds potential for research focused on addressing dry coughs linked to various respiratory diseases. -
Dopamine Receptor Agonist
Proterguride is a potent agonist of dopamine receptors, demonstrating significant potential in modulating dopaminergic signaling. Additionally, it exhibits antagonistic activity at the histamine H(1) receptor and alpha(1)-adrenoceptor, while also partially activating serotonergic 5-HT2A/B receptors. This compound is valuable for research focused on neurological diseases, including Parkinson's disease, providing insights into dopaminergic mechanisms and receptor interactions. -
PAF/Histamine Antagonist
Sch-40338 is a dual antagonist targeting platelet-activating factor (PAF) and histamine, exhibiting an IC50 of 0.59 μM in PAF-induced platelet aggregation and a Ki of 5.4 μM for histamine H₁ receptor binding. This compound is valuable for investigating the mechanisms underlying allergic diseases, offering insights into the modulation of inflammatory responses and platelet activation pathways. Sch-40338 serves as a useful tool for researchers exploring therapeutic strategies in allergen-mediated conditions. -
Antihistamine
Phenindamine is a first-generation antihistamine that primarily targets the H1 receptor. It exhibits significant anticholinergic and sedative effects, making it useful in alleviating allergic symptoms such as rhinitis and urticaria. This compound is often utilized in pharmacological studies to explore its effects on the central nervous system and its potential role in addressing respiratory conditions associated with allergic responses. -
Antihistamine
Cinnarizine-d8 is a deuterium-labeled derivative of Cinnarizine, which operates primarily as an antihistamine and calcium channel blocker. This compound has been utilized in pharmacological research to elucidate the mechanisms of action and metabolic pathways of antihistamines. Its isotopic labeling enhances analytical sensitivity in studies involving pharmacokinetics and pharmacodynamics. -
Histamine H3 Antagonist
Carcinine dihydrochloride is a selective histamine H3 receptor antagonist with a Ki value of 0.2939 μM. It demonstrates notable biological activities, including reducing histamine content, exhibiting antioxidant properties, and providing neuroprotective effects. Additionally, Carcinine dihydrochloride shows a positive inotropic effect and has potential to lower blood sugar and lipid levels. This compound is applicable in research related to inflammation, neurological disorders, cardiovascular health, and metabolic diseases, including retinal damage, seizures, and diabetes. -
Histamine-release Inhibitor
Panaxydiol is a histamine-release inhibitor that effectively suppresses histamine secretion in biological systems. This compound features an alkyne group, enabling it to participate in copper-catalyzed azide-alkyne cycloaddition (CuAAc), facilitating the formation of diverse chemical linkages. Its unique properties make Panaxydiol a valuable reagent for researchers involved in chemical biology, drug discovery, and the development of innovative therapeutic strategies. -
5-HT Receptor Agonist
8 Hydroxy PIPAT oxalate is a selective agonist of the 5-HT1A receptor. This compound activates serotonergic signaling pathways, promoting the degranulation of enteric mast cells and enhancing spontaneous histamine release in both guinea pig and human intestinal preparations. Its ability to modulate histamine release suggests potential applications in understanding and addressing functional gastrointestinal disorders, including irritable bowel syndrome. -
Histamine Receptor Agonist
Methimepip dihydrobromide is a potent and selective agonist of the histamine H3 receptor, exhibiting an EC50 of 0.316 nM. This compound is useful for investigating the role of H3 receptors in various physiological processes and could be valuable in research related to neurological disorders, sleep regulation, and appetite control. Its specificity and strength make it an essential tool in pharmacological studies of histamine signaling pathways. -
D2/H1 Antagonist
Norzine dimalate, a potent antagonist of dopamine D2 and histamine H1 receptors, exhibits significant anti-emetic and antipsychotic properties. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β load in murine models. Its diverse biological activities make Norzine dimalate a valuable reagent for research in neuropharmacology and Alzheimer's disease studies. -
Histamine H3 Receptor Agonist
Immethridine dihydrobromide is a selective agonist of the histamine H3 receptor (H3R) and demonstrates 300-fold selectivity for H3R over the H4 receptor, with no binding affinity for H1 or H2 receptors. This compound is valuable for research applications related to experimental autoimmune encephalomyelitis (EAE), providing insights into the role of H3R in neuroinflammatory conditions. Its specific targeting of H3R makes it a significant tool for investigating therapeutic approaches in neurological disorders. -
H3R Antagonist
H3R Antagonist 6 is a potent antagonist of the Histamine receptor 3 (H3R), exhibiting an IC50 of 5.6 nM. This compound, when labeled with 18F, demonstrates high radiochemical yield and molar activity, alongside moderate brain uptake, albeit with some off-target binding to the Sigma-1 receptor. H3R Antagonist 6 serves as a valuable PET radioligand for positron emission tomography imaging, facilitating research into central nervous system (CNS) disorders. -
Stable Isotope
Benztropine-d3 mesylate is a deuterium-labeled form of the centrally acting anticholinergic agent, Benztropine mesylate. This compound is primarily utilized in Parkinson's disease research and exhibits anti-histaminic properties alongside its function as a dopamine reuptake inhibitor. Additionally, Benztropine mesylate acts as an allosteric antagonist at the human D2 dopamine receptor and demonstrates effects against cancer stem cells (CSCs), making it valuable for studies in both neuropharmacology and oncology. -
Histamine H3 Receptor Modulator
Cipralisant maleate is a selective histamine H3 receptor modulator, exhibiting both antagonistic activity in vivo and agonistic effects in vitro. With a high affinity demonstrated by a pKi of 9.9 and a Ki of 0.47 nM for the rat histamine H3 receptor, this compound shows potential applications in attention-deficit hyperactivity disorder research. Additionally, Cipralisant maleate serves as a click chemistry reagent due to its alkyne group, enabling copper-catalyzed azide-alkyne cycloaddition (CuAAc) with azide-containing molecules. -
H1 Receptor Antagonist
Isothipendyl is a potent H1 receptor antagonist, classified as an azaphenothiazine derivative. This compound demonstrates significant anti-allergic activity by inhibiting the effects of histamine at the H1 receptor, making it useful in research related to allergic responses and asthma. Its role as a primary metabolite further supports its relevance in pharmacological studies focused on histamine-related pathways. -
Histamine H3 Receptor Antagonist
NNC 38-1049 is a potent and competitive antagonist of the histamine H3 receptor, demonstrating oral bioactivity. It effectively increases extracellular histamine levels in the paraventricular nucleus, suggesting potential implications in modulating neurotransmitter release. Research applications include the investigation of its effects on food intake and body weight regulation, making it a valuable tool for obesity studies. -
Histamine H2 Receptor Antagonist
Ranitidine bismuth citrate is a selective, orally active antagonist of the histamine H2 receptor, primarily used to inhibit gastric acid secretion. This compound effectively blocks histamine-induced contractile responses in the guinea-pig isolated rat atrium and relaxations in the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Additionally, ranitidine bismuth citrate demonstrates antiviral activity against SARS-CoV-2-infected cells and exhibits efficacy against Helicobacter pylori infections. Furthermore, it has been shown to inhibit breast tumor development and dissemination in murine models. -
Histamine H2-Receptor Antagonist
Etintidine hydrochloride is a potent oral histamine H2-receptor antagonist that effectively inhibits gastric acid secretion. Its primary mechanism involves blocking H2 receptors in the gastric mucosa, making it useful for studying gastrointestinal ulcer diseases and related research applications. Etintidine hydrochloride provides valuable insights into the role of histamine in gastric physiology and therapeutics. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine is a tricyclic antihistamine and anti-5-HT agent primarily targeting histamine receptors and serotonin pathways. It exhibits significant activity against decerebrate rigidity with minimal sedative and soporific effects. This compound effectively modulates fusimotor activity on muscle spindles in decerebrate models, making it a valuable reagent for studying conditions such as hemicrania and spasticity. -
Histamine Receptor Inhibitor
AM-0466 is a selective histamine receptor inhibitor primarily targeting voltage-gated sodium channel NaV1.7. This compound demonstrates potent anti-pruritic activity in histamine-induced itch models and exerts significant analgesic effects in capsaicin-induced pain assays. Its optimized pharmacokinetic profile supports its use in advanced in vivo research for evaluating efficacy in pain modulation and itch relief. -
Antihistamine Drug
Toladryl is an antihistamine drug with the ability to penetrate the blood-brain barrier, demonstrating both oral bioavailability and antihistaminic as well as anticholinergic properties. Its anticholinergic activity is approximately one-tenth that of diphenhydramine, while its protective efficacy against lethal doses of histamine in guinea pigs is 2-4 times greater. Toladryl exhibits milder and fewer side effects compared to diphenhydramine; however, higher doses may lead to central nervous system symptoms, including insomnia and agitation. This compound is valuable for research in the field of allergic diseases. -
Histamine Receptor
Nebidrazine targets histamine receptors and acts as a centrally-acting hypotensive agent. It induces dose-dependent hypotension and bradycardia with minimal sedative effects compared to clonidine, making it a potential candidate for hypertension management. The cardiovascular responses are influenced by central alpha-autoreceptors, as evidenced by the attenuation seen with yohimbine and the reduced effects following chemical sympathectomy. Additionally, research indicates that central histamine receptors play a role in modulating Nebidrazine's activity, underscoring its unique pharmacological profile and potential therapeutic applications in cardiovascular research. -
Histamine H2 Receptor Antagonist
(Z)-Lafutidine is a potent antagonist of the histamine H2 receptor. It exhibits significant anti-secretory and gastroprotective activities, making it valuable for research in gastrointestinal disorders and related therapeutic applications. Its ability to modulate gastric acid secretion positions it as a useful tool in studies aimed at understanding and treating conditions associated with excessive gastric acidity. -
PAF/Histamine Antagonist
N-Acetyldesloratadine is a potent dual antagonist of platelet-activating factor (PAF) and histamine, exhibiting oral bioactivity. It effectively inhibits PAF-induced aggregation of human platelets with an IC50 value of 0.6 µM. This compound is valuable for research into allergic diseases, including asthma, due to its ability to modulate PAF and histamine pathways. -
Histamine H4 Receptor Agonist
VUF 8430 is a potent and selective agonist of the histamine H4 receptor, exhibiting a Ki value of 31.6 nM and an EC50 of 50 nM. This compound plays a critical role in modulating immune responses and inflammatory processes. It is valuable for research into allergic reactions, autoimmune diseases, and other conditions related to the histamine H4 receptor pathways. -
Histamine H1 Receptor Antagonist
(S)-Cetirizine dihydrochloride is a potent antagonist of the histamine H1 receptor, exhibiting a Ki value of 39.1 nM. This compound demonstrates significant anti-allergic activity by inhibiting the effects of histamine, making it valuable for studying allergic conditions. It has potential applications in research focused on allergic diseases, including allergic rhinitis, providing insights into therapeutic strategies. -
H4R Agonist
4-Methylhistamine is a potent and selective agonist of the histamine 4 receptor (H4R), exhibiting a Ki of 50 nM and greater than 100-fold selectivity for hH4R relative to other histamine receptor subtypes. It effectively activates hH4R with a pEC50 of 7.4. This compound is valuable in research related to cancer, inflammation, and immunology, particularly in models of lung cancer and skin inflammation. -
Histamine H4 Receptor Antagonist
JNJ 40279486 is a selective antagonist of the histamine H4 receptor, exhibiting a Ki value of 9 nM. This compound plays a significant role in modulating immune responses and is primarily applied in research focused on immune-driven inflammatory diseases. Its specificity for the H4 receptor makes it a valuable tool for studying histamine signaling pathways and their implications in various inflammatory conditions. -
Histamine Receptor
Bodilisant is a fluorescent ligand for the histamine H3 receptor (hH3R). It demonstrates high affinity, allowing detection of hH3R activity in cells overexpressing the receptor at low concentrations (1-10 nM) and in hH3R-rich tissues at approximately 1 μM. This compound serves as a valuable pharmacological tool for receptor imaging and offers insights into histamine receptor signaling pathways in research applications. -
Antihistamine Agent
Vapitadine hydrochloride is a selective antihistamine agent with a primary mechanism of blocking the human histamine H1 receptor, exhibiting a binding affinity characterized by a Ki of 19 nM. This compound demonstrates significant biological activity by reducing histamine-induced lethality, with an ED50 range of 0.056-1.2 mg/kg, and effectively antagonizes cutaneous reactions to histamine, with an ED50 of 0.51-1.4 mg/kg in rat models. Vapitadine hydrochloride is suitable for research applications focusing on allergic responses and histamine-related disorders. -
Histamine Receptor Antagonist
(±)-Carbinoxamine is a potent histamine H1 receptor antagonist, widely utilized in research for its ability to inhibit histamine-mediated allergic responses. It demonstrates efficacy in alleviating symptoms associated with allergic rhinitis and urticaria. This compound is useful for studying the physiological effects of histamine signaling and the pharmacological modulation of allergic reactions. -
Dopamine Receptor Antagonist
Thiothixene is a potent dopamine D2 receptor antagonist, exhibiting selectivity over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). This compound demonstrates significant biological activity by reducing spontaneous and amphetamine-induced locomotor activity in rodent models, thereby influencing behavioral paradigms. Additionally, thiothixene enhances latent inhibition and competitive behavior, suggesting potential applications in understanding psychotropic effects and selective attention. Its diverse receptor binding profile also includes interactions with serotonin, histamine, adrenergic, muscarinic acetylcholine, and sigma receptors, broadening its relevance in psychopharmacological research. -
Neuroleptic Agent
Levomepromazine hydrochloride is a neuroleptic agent primarily acting as an antagonist at various neurotransmitter receptors, including dopamine, serotonin, cholinergic, and histamine receptors. This compound is known to inhibit the SERCA pump, resulting in increased cytoplasmic Ca2+ levels, which can induce adaptive endoplasmic reticulum stress and autophagy. Additionally, Levomepromazine hydrochloride exhibits a range of biological activities, including antiviral, anti-inflammatory, neuroprotective, analgesic, sedative, and anti-injurious properties. It serves as a valuable tool for investigating psychiatric disorders and managing nausea and vomiting in clinical settings. -
sigma-1/H3 receptor Antagonist
KSK68 is a high-affinity dual antagonist of the sigma-1 and histamine H3 receptors, exhibiting binding affinities with Kis of 7.7 nM for H3, 3.6 nM for sigma-1, and 22.4 nM for sigma-2 receptors. Importantly, KSK68 shows negligible affinity for other histamine receptor subtypes. This compound is particularly valuable for research into nociceptive mechanisms and neuropathic pain, providing a tool for the investigation of pain modulation pathways. -
Histamine Receptor Antagonist
DA 4643 dihydrochloride is an H2 receptor antagonist known for its unique properties in lipid peroxidation inhibition. This compound, with the chemical structure 2-guanidino-4 (3-methylaminomethyleneiminophenyl) thiazole dihydrochloride, exhibits antioxidant activity that contributes to its ability to suppress both enzymatic and non-enzymatic lipid peroxidation reactions. Unlike other H2 receptor antagonists, DA 4643 shows a weaker interaction with cytochrome P-450, further highlighting its distinct pharmacological profile. This makes DA 4643 dihydrochloride a valuable tool for studying H2 receptor-mediated pathways and oxidative stress in various biological contexts. -
Histamine Receptor Antagonist
Histamine H4 receptor antagonist-2 functions as a selective antagonist of the histamine H4 receptor. This compound has shown notable capability in activating the tumor suppressor protein p53, contributing to its significant antitumor effects. It is particularly useful in research applications focused on the modulation of immune responses and the potential treatment of various cancers. -
5-HT Receptor Antagonist
AVN-101 is a potent 5-HT7 receptor antagonist with a Ki of 153 pM, demonstrating significant brain penetration and oral bioavailability. It also interacts with 5-HT6, 5-HT2A, and 5-HT2C receptors, exhibiting Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively. Additionally, AVN-101 has a high affinity for histamine H1 and adrenergic α2A, α2B, and α2C receptors, with Ki values ranging from 0.41 to 3.6 nM. This compound is suitable for research related to general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis. -
H1 Receptor Antagonist
Isothipendyl hydrochloride is a potent H1 receptor antagonist belonging to the azaphenothiazine class. It effectively inhibits the action of histamine at H1 receptors, making it useful in various research applications related to allergy and inflammation studies. This compound may also be utilized to explore mechanisms of histamine-related disorders and assess the efficacy of potential therapeutic agents.
