Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Anti-inflammatory Agent
Tiopropamine is an anti-inflammatory agent primarily targeting histamine receptors. It exhibits significant potential in modulating inflammatory responses, making it a valuable tool for studying various inflammatory conditions. Its ability to influence histamine activity facilitates research into novel therapeutic strategies for related diseases. -
5-HT2A/ Histamine H1 Receptor Antagonist
LY2624803 is a potent antagonist of the 5-HT2A and histamine H1 receptors. This compound exhibits significant biological activity in modulating serotonergic and histaminergic signaling pathways, making it valuable for research in neuropharmacology. LY2624803 is particularly relevant for studies investigating mood disorders, anxiety, and other conditions associated with dysregulated serotonin and histamine receptor activity. -
H1-histamine receptor blocker
Quifenadine hydrochloride is an H1-histamine receptor antagonist known for its potential anti-arrhythmic properties. By blocking H1 receptors, it modulates the histaminergic pathways involved in cardiovascular responses, making it valuable for research into cardiac arrhythmias and their mechanisms. This compound may also provide insights into the broader impacts of histamine signaling in various physiological processes. -
Antihistamine Agent
Difeterol is an antihistamine agent that functions primarily as a histamine-1 receptor antagonist. It also inhibits butyrylcholinesterase (BChE), making it a valuable tool for studying cholinergic pathways. This compound is particularly relevant for research related to Alzheimer's disease, where modulation of histamine and cholinergic systems may provide insights into therapeutic strategies. -
Antihistamine Agent
Propiomazine is an orally active antihistamine agent that primarily functions as a potent prolactin release stimulant. Its mechanism involves the antagonism of the dopaminergic system, leading to the inhibition of luteinizing hormone secretion. Propiomazine is employed in clinical applications for anesthesia assistance, the management of mental disorders, and anxiety-induced sedation. Additionally, it serves as a valuable tool in research related to insomnia. -
Anti-inflammatory Agent
Pibaxizine is an orally active anti-inflammatory agent that functions as a histamine receptor antagonist. It effectively mitigates bronchoconstriction induced by histamine, making it a valuable tool for studies related to inflammation and immunology. Pibaxizine is particularly relevant in research focused on respiratory conditions, including asthma, where it can aid in understanding inflammatory pathways and potential therapeutic interventions. -
Histamine Receptor Inhibitor
Fenethazine is a histamine receptor inhibitor known for its antihistamine activity. It effectively alleviates allergic reactions and related symptoms. Additionally, its structural congeners exhibit anticholinergic effects, making fenethazine a candidate for research into therapeutic interventions for Parkinson's disease. This compound is valuable for studies focused on histaminergic pathways and associated disorders. -
Histamine Receptor Antagonist
Donetidine is a selective antagonist of the histamine H2 receptor, effectively inhibiting histamine-mediated processes. Its primary biological activity includes modulation of gastric acid secretion and potential implications for gastrointestinal research. Donetidine can be utilized in studies examining the roles of histamine signaling in various physiological and pathological conditions. -
Histamine H3 Receptor Antagonist/Serotonin Transporter Inhibitor
JNJ-28583867 is a selective histamine H3 receptor antagonist with a Ki of 10.6 nM and an inhibitor of the serotonin transporter (SERT) with a Ki of 3.7 nM. This compound shows promise in modulating neurotransmitter systems and can be utilized in research focusing on depression and related neuropsychiatric disorders. Its unique mechanism makes it a valuable tool for studying the interplay between histaminergic and serotonergic pathways. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine hydrochloride is an orally active tricyclic antihistamine and anti-5-HT agent. It exhibits notable efficacy against decerebrate rigidity, demonstrating minimal sedative and soporific effects. This compound has been shown to diminish or eliminate the influence of fusimotor activity on the muscle spindle in decerebrate cats. Dimethothiazine hydrochloride is valuable for research on hemicrania and spasticity. -
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.
