Catalog No.
Product Name
Application
Product Information
Citations
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5-HT1 Agonist
Rizatriptan benzoate is a selective agonist of the 5-HT1B and 5-HT1D serotonin receptors. It exhibits vasoconstrictive properties that affect peripheral blood flow and effectively penetrates the blood-brain barrier, thereby inhibiting pain neurotransmission within the central nervous system. This compound is primarily utilized in research focused on migraine pathophysiology and the modulation of serotonergic signaling. -
5-HT1 Receptor Agonist
Sumatriptan succinate is a selective agonist for the 5-HT1 receptor subtype, notably demonstrating IC50 values of 7.3 nM, 9.3 nM, and 17.8 nM for the 5-HT1D, 5-HT1B, and 5-HT1F receptors, respectively. This compound is primarily utilized in the study of migraine pathophysiology and therapeutics, providing insights into serotonin modulation during migraine attacks. Its pharmacological profile makes it an essential reagent for research investigating the efficacy of triptans in headache relief. -
5-HT1B/1D Agonist
Zolmitriptan is a selective partial agonist of the 5-HT1B and 5-HT1D receptors, demonstrating high affinity with Ki values of 5.01 nM and 0.63 nM, respectively. It effectively crosses the blood-brain barrier, making it a valuable tool in migraine research. This compound is primarily utilized for studying the pathophysiology of migraines and developing targeted therapeutic interventions. -
5-HT3 Receptor Antagonist
Alosetron (Z)-2-butenedioate is a potent and selective antagonist of the serotonin 5-HT3 receptor. This compound is primarily utilized in research related to irritable bowel syndrome (IBS), demonstrating efficacy in blocking fast 5HT3-mediated depolarization in guinea pig myenteric and submucosal neurons, with an IC50 of approximately 55 nM. Additionally, Alosetron has been shown to reduce the visceral nociceptive response to rectal distension in both conscious and anesthetized canine models, indicating its potential for anti-inflammatory applications. -
Antiarrhythmic Agent
Dronedarone is a class III antiarrhythmic agent primarily targeting ion channels to manage atrial fibrillation (AF) and atrial flutter. It effectively inhibits multiple ion currents, including potassium, sodium, and L-type calcium currents, while also displaying antiadrenergic properties through noncompetitive binding to β-adrenergic receptors. Additionally, Dronedarone acts as a moderate inhibitor and substrate for CYP3A4, making it valuable for pharmacological studies in cardiac rhythm disorders. -
5-HT3 Antagonist
Palonosetron is a selective 5-HT3 antagonist that effectively prevents acute, delayed, and overall chemotherapy-induced nausea and vomiting. In addition to its primary application in oncology, Palonosetron demonstrates moderate activity against flaviviruses and exhibits potent antiviral effects against Zika virus in mammalian cells. Furthermore, this compound has been associated with antidepressant properties, making it a valuable tool for diverse research applications in both oncology and virology. -
5-HT3 Antagonist
Palonosetron hydrochloride is a selective 5-HT3 receptor antagonist that primarily functions to prevent acute and delayed nausea and vomiting associated with chemotherapy. Beyond its primary application, Palonosetron hydrochloride demonstrates moderate activity against flaviviruses, including potent efficacy against the Zika virus in mammalian cells. Additionally, this compound has been associated with antidepressant effects, expanding its potential therapeutic applications in neurological research. -
Anticholinergic Agent
Benztropine mesylate is a centrally acting anticholinergic agent that effectively crosses the blood-brain barrier. It primarily functions as a selective antagonist at human D2 dopamine receptors, exhibiting anti-histaminic properties and acting as a dopamine re-uptake inhibitor. This compound is particularly relevant for Parkinson's disease research, as well as in studies exploring its effects on cancer stem cells (CSCs). Researchers can utilize Benztropine mesylate to examine its potential therapeutic benefits in neurodegenerative and cancer treatment contexts. -
Histamine Receptor Modulator
Betahistine dihydrochloride is a potent histamine H1 receptor agonist and H3 receptor antagonist. This compound demonstrates significant biological activity in modulating histaminergic systems and is employed in research focused on conditions such as rheumatoid arthritis (RA). Its dual action makes it a valuable tool for investigating the pathways involved in inflammation and immune response. -
Antidepressant
Doxepin Hydrochloride is a tricyclic antidepressant that primarily functions as a selective antagonist of the histamine receptor H1. It effectively inhibits the reuptake of serotonin and norepinephrine, contributing to its antidepressant properties. Additionally, Doxepin exhibits significant activity as a CYP450 inhibitor, particularly affecting CYP450 2C19 and 1A2. This compound has demonstrated therapeutic potential in conditions such as atopic dermatitis and chronic urticaria, and it may enhance cognitive processes while providing neuroprotective effects against oxidative stress. -
Histamine 1 Receptor Blocker
Ketotifen fumarate is a noncompetitive antagonist of the histamine H1 receptor, functioning as a mast cell stabilizer. It exhibits significant biological activity by inhibiting 6-phosphogluconate dehydrogenase in vitro and demonstrates antiviral properties against SARS-CoV-2 and Influenza viruses. This compound is particularly useful in researching autoimmune encephalomyelitis (EAE) and in developing strategies for asthma attack prevention. -
Dopamine Receptor Antagonist
Levosulpiride is a selective antagonist of dopamine D2 receptors, classified as an atypical antipsychotic agent within the benzamide family. This compound is primarily used in the investigation of its effects on psychotic disorders and gastrointestinal conditions due to its ability to modulate dopaminergic activity. Researchers utilize Levosulpiride to study its therapeutic potential in conditions such as schizophrenia and to explore its impact on gastrointestinal motility. -
5-HT2C Receptor Agonist
CP-809101 hydrochloride is a highly selective agonist of the 5-HT2C receptor, exhibiting pEC50 values of 9.96 for the human 5-HT2C receptor, along with lower activity at 5-HT2B and 5-HT2A receptors. This compound has been shown to inhibit conditioned avoidance responses in rodent models and effectively antagonizes PCP- and d-amphetamine-induced hyperactivity. Additionally, CP-809101 hydrochloride demonstrates potential in reducing food and nicotine dependence, making it a valuable tool for research in psychopharmacology and addiction studies. -
Adrenergic Receptor Antagonist
Dibenamine is an alpha-adrenergic receptor antagonist that inhibits both basal and histamine-stimulated gastric acid secretion. Its primary pharmacological activity renders it useful in studying conditions characterized by excessive gastric acid production. Additionally, Dibenamine can be employed in research concerning adrenergic signaling pathways and their impact on gastric physiology. -
Histamine Receptor Antagonist
Doxylamine succinate is a first-generation antihistamine that acts as an H1 receptor antagonist. This compound exhibits key biological activity as an effective sedative and hypnotic agent, making it valuable in sleep disorder research. Additionally, it possesses local analgesic properties, providing potential applications in studies related to pain management and sleep regulation. -
Histamine H1 Receptor Antagonist
Epinastine hydrochloride is a selective histamine H1 receptor antagonist and mast cell stabilizer. It exhibits high affinity for neuronal octopamine receptors, with inhibitory constants of Ki = 2 nM in locusts and Ki = 1.1 nM in honeybees. This compound effectively inhibits inflammatory mediators such as TARC, IL-8, and IL-4, and enhances anti-colon cancer immunity while reducing scratching behavior and vascular permeability induced by Substance P. Epinastine hydrochloride is valuable for research in allergic diseases and related inflammatory conditions. -
Antihistamine Agent
Hydroxyzine dihydrochloride is an antihistamine agent that primarily functions as a histamine H1-receptor antagonist and serotonin antagonist. It exhibits anxiolytic properties, making it a valuable tool for research into generalized anxiety disorder and related conditions. This compound can also be utilized in studies involving sedation and allergic reactions due to its diverse pharmacological effects. -
Histamine Receptor Inhibitor
Levodropropizine is a selective histamine receptor inhibitor primarily used as a peripheral antitussive agent. Its mechanism of action involves the suppression of cough reflexes through its interaction with histamine receptors, making it effective in treating cough associated with colds and allergies. Levodropropizine is noted for its good tolerance profile, facilitating its use in various research applications focused on respiratory physiology and pharmacology. -
5-HT Receptor Modulator
Lurasidone Hydrochloride is a potent antagonist of both dopamine D2 and 5-HT7 receptors, exhibiting IC50 values of 1.68 nM and 0.495 nM, respectively. Additionally, it acts as a partial agonist at the 5-HT1A receptor with an IC50 of 6.75 nM. This compound is utilized in research focused on neuropharmacology and the treatment of psychiatric disorders, such as schizophrenia and bipolar disorder. Its selective modulation of serotonin and dopamine receptors makes it a valuable tool for investigating neurochemical pathways and therapeutic interventions. -
5-HT(1B/1D) Receptor Agonist
Naratriptan hydrochloride is a selective agonist for the 5-HT1B and 5-HT1D receptors. It effectively induces vasoconstriction of cranial arteries through these receptor pathways, demonstrating an EC50 value of 0.11 μM in dog basilar artery models. Additionally, Naratriptan hydrochloride exhibits the ability to inhibit trigeminal nerve-mediated dural neurogenic plasma extravasation and mitigate sterile inflammation. This compound is primarily utilized in research focused on acute migraine, particularly in the investigation of cranial vascular and neuroinflammatory mechanisms. -
Histamine H1 Antagonist
Pemirolast potassium is a histamine H1 antagonist with antiallergic properties. It effectively mitigates hypersensitivity reactions associated with Paclitaxel and demonstrates potential applications in studies related to bronchial asthma and conjunctivitis. This compound is valuable for researchers focusing on allergic responses and treatment mechanisms in respiratory and ocular conditions. -
Dopamine Receptors Blocker
Trifluoperazine dihydrochloride is a dopamine receptor antagonist, primarily used in the study of schizophrenia. This compound demonstrates significant activity as an α1-adrenergic receptor blocker and acts as a potent inhibitor of NUPR1, exhibiting anticancer properties. Additionally, it functions as a calmodulin inhibitor and has been shown to inhibit P-glycoprotein, impacting multidrug resistance. Trifluoperazine dihydrochloride is also recognized for its reversible inhibition of influenza virus morphogenesis, making it valuable for various research applications in neuropharmacology and virology. -
5-HT3 Receptor Antagonist
VUF10166 is a potent 5-HT3 receptor antagonist, exhibiting high affinity with Ki values of 0.04 nM for the 5-HT3A subtype and 22 nM for the 5-HT3AB subtype. This compound effectively inhibits 5-HT-induced responses at these receptors at nanomolar concentrations. Additionally, at elevated concentrations, VUF10166 demonstrates partial agonistic activity at the 5-HT3 receptor, with an EC50 of 5.2 μM. Its unique pharmacological profile makes it a valuable tool for research in neurobiology and gastrointestinal pharmacology. -
5-HT3 Receptor Antagonist
Ramosetron Hydrochloride is a potent 5-HT3 receptor antagonist. It exhibits key biological activity in alleviating symptoms of dysphoria, activity interference, and food avoidance. This compound shows promise for research applications targeting irritable bowel syndrome with diarrhea, making it a valuable tool for studies in gastrointestinal disorders. -
PDE3/PDE4/PDE5/HRH1 Inhibitor
Fenspiride hydrochloride is a non-steroidal anti-inflammatory agent and an antagonist of the H1-histamine receptor. It selectively inhibits phosphodiesterase activities, including PDE3, PDE4, and PDE5, with -log IC50 values of 3.44, 4.16, and approximately 3.8, respectively. This compound is valuable for research applications focused on respiratory diseases, highlighting its potential in therapeutic investigations and the modulation of inflammatory responses. -
Histamine Receptor Antagonist
Mepyramine maleate is a potent antagonist of the histamine H1 receptor, exhibiting a Kd of 0.8 nM for H1, alongside Kd values of 5200 nM and >3000 nM for H2 and H3 receptors, respectively. With a pKd value of 9.4 for the H1 receptor, this first-generation antihistamine is valuable for studies focused on allergic responses and the role of histamine in various physiological processes. It is widely used in pharmacological research to explore histamine-mediated signaling and potential therapeutic applications in allergy and inflammation. -
5-HT Receptor Antagonist
Trimipramine maleate is a selective 5-HT receptor antagonist that effectively crosses the blood-brain barrier. It demonstrates significant binding affinity with pKi values of 6.39, 8.10, and 4.66 for the 5-HT1C, 5-HT2, and 5-HT1A receptors, respectively. Additionally, Trimipramine maleate acts as an inhibitor of human noradrenaline transporter (hNAT), serotonin transporter (hSERT), and organic cation transporters (hOCT1, hOCT2), with IC50 values of 4.99 μM, 2.11 μM, and 3.72 μM, and 8.00 μM, respectively. Its unique pharmacological profile also indicates potential applications in vascular activity and anxiety treatment research. -
5-HT4 Agonist
Cisapride monohydrate is a potent 5-HT4 receptor agonist and hERG inhibitor. As a prokinetic agent, it enhances gastrointestinal motility while facilitating or restoring function throughout the digestive tract. Cisapride monohydrate stimulates motor activity in the gastrointestinal system via an indirect mechanism, promoting acetylcholine release from postganglionic nerve endings in the myenteric plexus. This compound is valuable in research applications focused on gastrointestinal motility disorders. -
Bacterial Inhibitor
Chlorprothixene hydrochloride functions as an antagonist of dopamine and histamine receptors, exhibiting Kis of 18 nM for hD1, 2.96 nM for hD2, 4.56 nM for hD3, 9 nM for hD5, and 3.75 nM for hH1 receptors. This compound demonstrates significant antipsychotic activity, making it a valuable tool for research into neuropharmacology and the mechanisms underlying psychotic disorders. Its receptor modulation also indicates potential applications in the study of bacterial inhibition mechanisms, providing insights into the interplay between neurotransmitter systems and microbial pathogenesis. -
Histamine H1 Antagonist
Triprolidine hydrochloride monohydrate is a first-generation antihistamine that functions as a histamine H1 antagonist. It is primarily utilized in research on allergic rhinitis and has demonstrated effects on spinal motor and sensory block in rodent models. This compound is valuable for understanding histamine-related physiological responses and the mechanisms underlying allergic reactions. -
Adrenergic Receptor Agonist
Salbutamol is a short-acting β2-adrenergic receptor agonist that primarily targets the β2-adrenergic receptor. It is well-known for its ability to promote relaxation of bronchial smooth muscle, making it a valuable tool in the study of bronchospasm related to asthma and chronic obstructive pulmonary disease. Additionally, Salbutamol has been implicated in promoting tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling pathway, highlighting its relevance in cancer research. -
histamine H1 Receptor Agonist
Betahistine mesylate is an orally active agonist of the histamine H1 receptor, with antagonist properties at the H3 receptor. This compound is primarily utilized in research to investigate the role of histamine receptors in rheumatoid arthritis (RA) and other related inflammatory conditions. Its unique mechanism of action makes it a valuable tool for studying histaminergic signaling pathways and their implications in joint pathology. -
Histamine Receptor Modulator
Betahistine is a histamine receptor modulator, acting as an agonist at the H1 receptor and an antagonist at the H3 receptor. It has demonstrated potential in modifying histamine pathways and is utilized in research related to rheumatoid arthritis (RA). This compound serves as a valuable tool for investigating the role of histaminergic signaling in inflammatory conditions. -
VEGFR Inhibitor
Chloropyramine hydrochloride is an H1 histamine receptor antagonist that also serves as an inhibitor of vascular endothelial growth factor receptor 3 (VEGFR-3) and focal adhesion kinase (FAK). This compound exhibits key biological activities, contributing to research in angiogenesis and related pathways. It is valuable for studies aimed at understanding the role of VEGFR signaling in various physiological and pathological processes. -
β/α-1 Blocker
Carvedilol phosphate hemihydrate is a non-selective β/α-1 adrenergic receptor blocker. It demonstrates significant biological activity by inhibiting lipid peroxidation with an IC50 of 5 μM and acts as a multiple-action antihypertensive agent, with potential applications in treating angina and congestive heart failure. Additionally, carvedilol phosphate hemihydrate has been identified as an autophagy inducer that suppresses the NLRP3 inflammasome, making it valuable for research in inflammation and cardiovascular diseases. -
5-HT4 Agonist
Cinitapride monotartrate is a selective 5-HT4 agonist and also exhibits antagonistic properties on 5-HT2A and D2 receptors. This compound primarily enhances gastrointestinal motility and is utilized in the study of functional dyspepsia and related digestive disorders. Its dual action on serotonin and dopaminergic pathways makes it a valuable tool in gastrointestinal pharmacology research. -
5-HT Receptor Agonist
5-Methoxytryptamine is a nonselective agonist of the 5-HT receptors, playing a significant role in modulating serotonergic signaling. As a metabolite of melatonin, it does not exhibit affinity for the 5-HT3 receptor. Additionally, 5-Methoxytryptamine demonstrates potent antioxidant properties and provides radioprotective effects, making it valuable for various biological research applications. -
Cannabinoid Receptor Inhibitor
Yangonin is a selective cannabinoid receptor inhibitor that demonstrates affinity for the human recombinant CB1 receptor, with an IC50 value of 1.79 μM and a Ki of 0.72 μM. This compound is of significant interest for research applications aimed at understanding cannabinoid signaling and its implications in various physiological processes. Its modulation of CB1 receptor activity may provide insights into therapeutic strategies targeting cannabinoid-related pathways. -
Adrenergic Receptor Inhibitor
Penbutolol sulfate is a potent adrenergic receptor inhibitor, primarily acting as a β-adrenoceptor and 5-HT receptor antagonist, with Ki values of 11.6 nM and 11.9 nM for 5-HT in rat cornu ammonis 1 (CA1) and human CA3 regions, respectively. This compound demonstrates significant biological activity through modulation of neurotransmitter signaling pathways, making it valuable for research applications involving cardiovascular studies and neuropharmacology. -
Serotonin Receptor Antagonist
Setiptiline maleate is a serotonin receptor antagonist targeting multiple pathways in neurotransmitter regulation. As a tetracyclic antidepressant (TeCA), it functions primarily as a noradrenergic and specific serotonergic antidepressant (NaSSA), inhibiting norepinephrine reuptake and antagonizing α2-adrenergic receptors. Setiptiline maleate further interacts with serotonin receptor subtypes, including 5-HT2A, 5-HT2C, and/or 5-HT3, while also acting as an H1 receptor inverse agonist, demonstrating potential utility in depression and anxiety research. -
Histamine 1 Receptor Antagonist
Decloxizine dihydrochloride is a potent antagonist of the histamine H1 receptor. It exhibits significant anti-allergic activity, making it valuable in research pertaining to allergy and asthma models. Additionally, this compound can be utilized to investigate the role of histamine signaling in various physiological and pathological processes. -
Histamine Receptor Inhibitor
Dexchlorpheniramine maleate is a potent histamine receptor inhibitor primarily utilized in the treatment of allergic conditions. This compound exhibits anti-inflammatory, anti-irritant, and anti-allergic properties, making it effective for managing symptoms of allergic rhinitis. Additionally, dexchlorpheniramine maleate has been shown to inhibit myocardial contraction in rat models, providing further insight into its biological effects. It serves as a valuable reagent for research applications exploring the mechanisms of allergic responses and their physiological effects. -
5-HT Receptor Antagonist
Naftidrofuryl oxalate is a 5-HT2 receptor antagonist known for its vasodilatory properties. It primarily promotes increased blood flow in peripheral and cerebral vascular disorders by enhancing cellular oxidative capacity. This compound is relevant for research into vascular function and the cellular mechanisms underlying vascular diseases. -
5-HT Receptor Antagonist
Alprenolol is a non-selective β-adrenoceptor antagonist that also acts as an antagonist at the 5-HT1A and 5-HT1B serotonin receptors. It demonstrates significant biological activity in lowering blood pressure, alleviating angina, and managing arrhythmias. Alprenolol is commonly utilized in cardiovascular research and pharmacological studies focused on hypertension and related cardiac conditions. -
Antihistamine/anticholinergic Agent
Chlorphenoxamine is an antihistamine and anticholinergic agent that functions as a GPCR antagonist. This compound exhibits antiviral properties against several lethal viral diseases, including SARS-CoV, MERS-CoV, and Ebola virus (EBOV), with IC50 values of 1.1 μM for EBOV and 6.2 μM for Marburg virus (MARV). Chlorphenoxamine is utilized in research focused on allergic conditions, urticaria, viral infections, and Parkinson’s disease. -
5-HT1A Receptor Agonist
Tandospirone citrate is a selective partial agonist of the 5-HT1A receptor, exhibiting a binding affinity with a Ki value of 27 nM. It demonstrates significant selectivity over other serotonin and adrenergic receptors, including SR-2, SR-1C, α1, α2, D1, and D2, with Ki values ranging from 1300 to 41000 nM. This compound is primarily used in research related to psychiatric disorders and anxiety management, making it a valuable tool for exploring serotonergic pathways and their implications in mental health. -
5-HT1 Receptor Agonist
Sumatriptan is a selective agonist of the 5-HT1 receptor subtypes, demonstrating IC50 values of 7.3 nM for 5-HT1D, 9.3 nM for 5-HT1B, and 17.8 nM for 5-HT1F. It is primarily utilized in migraine headache research, providing insights into mechanisms of action and potential therapeutic applications for migraine treatment. -
5-HT Receptor Antagonist
(±)-Fabesetron is a potent dual antagonist of the 5-HT3 and 5-HT4 receptors. This compound exhibits significant activity in blocking serotonin receptor signaling, making it valuable for the investigation of gastrointestinal motility disorders and the modulation of nausea and vomiting. Researchers can utilize (±)-Fabesetron to study the roles of these receptors in various biological processes and potential therapeutic applications. -
5-HT(3A)R Blocker
Hydrodolasetron is a potent 5-HT(3A) receptor antagonist, exhibiting an IC50 of 0.29 nM. It is recognized for its antiemetic properties and is a metabolite of Dolasetron, demonstrating enhanced efficacy in blocking nicotinic acetylcholine receptors compared to its parent compound. This compound is valuable in research focused on gastrointestinal disorders and the modulation of serotonin-mediated pathways. -
5-HT Receptor Antagonist
5-HT3 antagonist 3 is a high-affinity antagonist of the 5-HT3 receptor. It demonstrates potent binding to the 5-HT3 receptors in rat brain cortical membranes, exhibiting a Ki value of 0.25 nM. This compound is valuable for research applications involving neuropharmacology and gastrointestinal function, contributing to the study of disorders related to serotonin signaling.
