Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
Adrenergic Receptor Antagonist
Tertatolol is a potent antagonist of beta-adrenoceptors and 5-HT receptors. It exhibits unique renal vasodilatory effects, making it a valuable tool for investigating cardiovascular and renal physiology. Tertatolol is utilized in research applications focusing on the modulation of adrenergic signaling and its implications in various pathological conditions. -
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. -
Stable Isotope
Pindolol-d7 is a deuterated form of Pindolol, primarily targeting the 5-HT 1A (Ki=33 nM) and 5-HT 1B receptors, as well as β1/β2-adrenergic receptors. This stable isotope is utilized in research to investigate the pharmacokinetics and metabolic pathways of Pindolol. The compound demonstrates significant anti-anxiety and antidepressant activities, making it valuable for studies related to psychiatric disorders and neuropharmacology. -
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.
