Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
5-HT1AR Agonist/α1-Adrenergic Receptor Antagonist
Enciprazine is an orally active non-benzodiazepine anxiolytic that primarily functions as a 5-HT1A receptor agonist and an α1-adrenergic receptor antagonist. This compound has demonstrated the ability to modulate electroencephalogram activity by decreasing δ and θ wave power while increasing α and fast β wave power. With its anti-aggressive properties, Enciprazine exhibits minimal sedative and ataxic side effects. Additionally, it influences plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis, making it a valuable tool for research into anxiety disorders, generalized anxiety syndrome, and psychosis. -
5-HT Receptor
5HT6-ligand-1 is a potent ligand for the 5-HT6 receptor, exhibiting a competitive inhibition constant (Ki) of 1.43 nM. This compound is utilized in neuropharmacological research to investigate the role of the 5-HT6 receptor in various neurological conditions and psychiatric disorders. Its high affinity contributes to studies focused on neurotransmitter modulation and potential therapeutic applications. -
5-HT Receptor Antagonist
5-HT2 antagonist 1 is a selective antagonist of the 5-HT2 receptor, primarily inhibiting serotonin signaling. This compound exhibits the ability to modulate various serotonergic pathways, contributing to its potential utility in investigating mood disorders and other neuropsychiatric conditions. Its minimal activity at α1 adrenoceptors makes it suitable for studies focused on serotonin receptor dynamics without significant adrenergic interference. -
5-HT Receptor Antagonist
5-HT3 antagonist 1 is a selective antagonist of the serotonin 3 (5-HT3) receptor, effectively blocking serotonin-mediated signaling pathways. This compound exhibits significant potential in the study of gastrointestinal disorders, nausea, and anxiety-related conditions. Its ability to modulate 5-HT3 receptor activity makes it a valuable reagent for pharmacological research and drug development focused on serotonin receptor interactions. -
5-HT Receptor Agonist
Minesapride is a selective partial agonist of the serotonin 4 (5-HT4) receptor. It promotes gastrointestinal peristalsis and enhances colonic transport by activating these receptors. Additionally, Minesapride effectively increases bowel movements and may alleviate visceral allergic reactions. This compound is utilized in research related to constipation-type irritable bowel syndrome (IBS-C). -
5-HT(1B/1D) Receptor Agonist
Naratriptan-d3 is a deuterium-labeled variant of Naratriptan, functioning primarily as an agonist of the 5-HT1B/1D receptors. This compound is known for its peripheral activity and favorable oral bioavailability, effectively inducing vasoconstriction of cranial arteries by activating the specified receptors with an EC50 of 0.11 μM in canine basilar artery models. Naratriptan-d3 also plays a role in inhibiting migraine-associated trigeminal nerve activity and reducing sterile inflammation, making it a valuable tool for investigating acute migraine mechanisms and associated cranial vascular and neuroinflammatory pathways. -
5-HT Receptor Agonist
Des-4-fluorobenzyl mosapride is a primary metabolite of Mosapride, functioning primarily as a 5-HT receptor agonist. This compound exhibits gastroenterokinetic properties, enhancing gastrointestinal motility through its action on 5-HT4 receptors. Its biological activity makes it useful in research exploring gastrointestinal disorders and the modulation of enteric nervous system functions. -
5-HT Receptor Inhibitor
BF-1 is a potent antagonist of the 5-HT2B receptor, exhibiting a pKi value of 10.05 and an IC50 of 2.6 nM. This compound demonstrates significant inhibitory activity, making it valuable for research applications in neurobiology and pharmacology. Its specificity for the 5-HT2B receptor allows for detailed investigation into serotonin signaling pathways and related physiological processes. -
5-HT3 receptor antagonist
Indisetron is a potent 5-HT3 receptor antagonist known for its anti-emetic properties. It effectively blocks serotonin receptors in the central nervous system, making it valuable for preventing nausea and vomiting associated with chemotherapy and surgery. This compound is widely utilized in pharmacological research related to gastrointestinal motility and neuropharmacology. -
5-HT Antagonist
L 646462 is a selective antagonist of serotonin (5-HT) receptors, primarily targeting the peripheral nervous system. With a central/peripheral activity ratio of 143, it is particularly suitable for research into nausea and vomiting, as well as associated neurological disorders. This compound enables the investigation of mechanisms underlying serotonin-related pathologies and the development of therapeutics aimed at these conditions. -
5-HT3 Receptor Antagonist
Cilansetron hydrochloride hydrate is a selective antagonist of the 5-HT3 receptor, primarily involved in the modulation of gastrointestinal function. This compound exhibits biological activity relevant to the treatment of conditions such as irritable bowel syndrome (IBS). It serves as a valuable tool for research focused on gastrointestinal disorders and the underlying mechanisms of 5-HT3 receptor activity. -
5-HT Receptor Antagonist
Flufylline functions primarily as a 5-HT receptor antagonist, exhibiting antihypertensive properties in spontaneously hypertensive rat models. This compound demonstrates the ability to modulate serotonin signaling, making it a valuable tool for investigating cardiovascular disease mechanisms and therapeutic approaches. Its efficacy in various animal models positions Flufylline as a relevant reagent for cardiovascular research. -
5-HT Receptor Antagonist
Piboserod hydrochloride is a selective antagonist for the 5-HT4 receptor. This compound demonstrates significant inhibition of serotonin-mediated pathways, making it a valuable tool for research into gastrointestinal motility and cognitive function. Its role in the modulation of 5-HT receptor activity makes it relevant for studying neurological disorders and gastrointestinal diseases. -
5-HT Receptor Antagonist
T 82 is a potent 5-HT3 receptor antagonist that also functions as an acetylcholinesterase (AChE) inhibitor. This compound exhibits significant biological activity relevant for modulating neurotransmitter signaling in the central nervous system. T 82 is primarily utilized in research related to neurodegenerative diseases, including Alzheimer's Disease, making it a valuable tool in understanding the pathophysiology and treatment approaches for related conditions. -
5-HT Receptor 4 Agonist
DA-6886 monohydrochloride is a selective agonist of the 5-Hydroxytryptamine receptor 4 (5-HT4), demonstrated to induce relaxation in rat esophageal tissue via a 5-HT4 receptor antagonist-sensitive mechanism. This compound shows significant selectivity, with an inhibitory pIC50 value of 4.3 for hERG channels, indicating it is 1000-fold more preferential for 5-HT4 receptors. DA-6886 is suitable for research into constipated irritable bowel syndrome and related gastrointestinal disorders. -
5-HT2 Receptor Agonist
2,4-DMA hydrochloride is a serotonin 5-HT2 receptor agonist, exhibiting an apparent PA2 value of 5.6. This compound is classified as an amphetamine and demonstrates significant biological activity relevant to studies involving serotonin receptor modulation. It serves as a valuable reagent for research into neurological pathways and psychiatric conditions associated with serotonin signaling. -
5-HT4 Receptor Antagonist
Sulamserod hydrochloride is a selective antagonist of the 5-HT4 receptor. This compound exhibits significant biological activity in inhibiting gastrointestinal motility and is utilized in research related to gastrointestinal diseases. Its role in modulating serotonergic signaling makes it valuable for studies investigating disorders such as irritable bowel syndrome and other functional gastrointestinal disorders. -
5-HT Antagonist
p-MPPF is a selective antagonist of the 5-HT receptor, primarily targeting serotonergic signaling pathways. It effectively dose-dependently inhibits the reduction of phosphorylated Erk1/2 levels in the hippocampus induced by 8-OH-DPAT in rat models. This compound is valuable for research into neurological diseases, providing insights into serotonergic modulation and its effects on neuronal signaling. -
5-HT7/5-HT1A Receptor Antagonist
5-HT7R antagonist 4 is a selective antagonist of the 5-HT7 receptor, exhibiting a binding affinity of Ki = 2.6 nM, while demonstrating lower affinity for the 5-HT1A receptor (Ki = 476 nM). This compound serves as a valuable tool for investigating the role of 5-HT7 receptors in neurological disorders and may contribute to the development of therapeutic strategies targeting these pathways. Its pharmacological profile makes it suitable for research applications focused on serotonin-related signaling and neurodegenerative diseases. -
5-HT2A Ligand
6-Fluoro-N,N-diethyltryptamine (6-F-DET) is a selective ligand for the 5-HT2A receptor. This compound exhibits high affinity and binding characteristics, making it valuable for investigating serotonergic signaling pathways. Its biological activity is essential for studies related to neuropharmacology, psychopharmacology, and the exploration of potential therapeutic agents targeting serotonin-related disorders. -
α7 nAChR Agonist/5-HT3 antagonist
(S)-PNU-282987 hydrochloride is a potent agonist of the α7 nicotinic acetylcholine receptor (nAChR), exhibiting an EC50 of 154 nM. In addition, it acts as a functional antagonist of the 5-HT3 receptor with an IC50 of 4541 nM. This compound is valuable for research applications exploring the central and peripheral nervous systems, facilitating the study of neurotransmission and signaling pathways involving cholinergic and serotonergic systems. -
5-HT Receptor Inhibitor
5-APDI hydrochloride is a selective inhibitor of the 5-HT receptor, exhibiting significant biological activity in modulating neurotransmitter uptake. It effectively inhibits the reuptake of serotonin, dopamine, and norepinephrine in crude synaptosomes, with IC50 values of 82 nM, 1,847 nM, and 849 nM, respectively. This compound is valuable in research applications related to neuropharmacology and the study of mood disorders. -
5-HT3 Receptor Antagonist
WAY-100289 is a selective antagonist of the 5-HT3 receptor, demonstrating high affinity with a pA2 value of 8.9 in isolated rat vagus nerve studies. This compound effectively inhibits the Bezold-Jarisch reflex in both anesthetized and awake rat models, highlighting its potential applications in neuropharmacological research and studies of gastrointestinal function. Its oral bioavailability makes it a valuable tool for investigating the therapeutic roles of 5-HT3 receptor modulation in various physiological and pathological states. -
5-HT Receptor Agonist
5-HTQ chloride is a potent 5-HT receptor agonist derived from the skin secretions of the Australian golden bell frog (Litoria aurea). This indole alkaloid exhibits strong biological activity by fully activating the 5-HT receptor, making it a valuable tool in the study of serotonin signaling pathways. Its applications include research into neuropharmacology and the modulation of mood-related disorders. -
5-HT receptor antagonist
Cyanopindolol fumarate acts as a selective antagonist of the 5-HT receptor, playing a significant role in modulating serotonergic activity. Its ability to inhibit serotonin receptors makes it a valuable tool for research in neuropharmacology and the study of mood disorders. This compound is commonly used to investigate the effects of serotonin modulation in various biological systems. -
5-HT Receptor Control
Triazolomethylindole-3-acetic acid acts as an agonist for the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D. This compound exhibits significant biological activity in modulating serotonergic signaling, making it a valuable tool for research in neuropharmacology and developmental biology. It is particularly relevant for studies investigating the therapeutic potential of serotonin-related pathways in various neurological disorders. -
5-HT Receptor
Ebalzotan is a selective agonist of the 5-HT1A receptor, primarily studied for its role in modulating serotonergic signaling related to depression. This compound has potential applications as a precursor in the synthesis of important active pharmaceutical ingredients. The synthesis of Ebalzotan employs a multi-enzyme catalyzed reduction reaction, yielding saturated primary or secondary alcohols with high enantioselectivity and efficiency. -
5-HT3 Receptor Antagonist
KF 18259 is a potent antagonist of the 5-HT3 receptor. It effectively inhibits propulsive motility in both the proximal and distal colon induced by wrap-restraint stress. This compound is valuable for research into gastrointestinal motility disorders and the role of serotonin receptors in stress-related gastrointestinal functions. -
5-HT Ligand
D-5-Hydroxytryptophan (D-5-HTP) is a D-isomer of 5-Hydroxytryptophan that primarily serves as a ligand for serotonin (5-HT) receptors. As a significant research tool, D-5-HTP binds to the 5-HT site with micromolar affinity, providing a valuable negative control in behavioral studies. Unlike its L-counterpart, D-5-HTP does not elicit any observable effects on mouse behavior, making it crucial for comparative studies in neuropharmacological research. -
5-HT3 Receptor Antagonist
GYKI-46903 is a non-competitive antagonist of the 5-HT3 receptor, exhibiting a pIC50 of 6.91. This compound is primarily used in research focused on the modulation of serotonin signaling pathways and the study of related gastrointestinal and neurological disorders. Its ability to inhibit 5-HT3 receptor activity makes it a valuable tool for investigating therapeutic approaches in conditions such as anxiety and nausea. -
5-HT Receptor Antagonist
Cinanserin is a potent and selective antagonist of the 5-HT2 receptor, exhibiting Ki values of 41 nM for 5-HT2 and 3500 nM for the 5-HT1 receptor. Additionally, it acts as an inhibitor of the SARS-CoV 3CLpro, demonstrating KD values of 49.4 µM and 18.2 µM against SARS-CoV 3CLpro and HCoV-229E 3CLpro, respectively. Cinanserin has been shown to effectively reduce systemic burn edema levels, making it valuable for research in neuropharmacology and viral pathogenesis.
