Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
5-HT Receptor Ligand
2-Methyl-N,N-dimethyltryptamine acts as a ligand for the serotonin (5-HT) receptors, exhibiting a pA2 value of 6.04. Its affinity for these receptors positions it as a valuable tool in the study of neuropharmacology and neurological diseases. Researchers can utilize this compound to investigate serotonin signaling pathways and their implications in various neurological conditions. -
5-HT1A/1B Autoreceptor Antagonist
SB-649915 is a potent antagonist of the 5-HT1A and 5-HT1B autoreceptors, demonstrating pKi values of 8.6 and 8.0, respectively. This compound also acts as a serotonin reuptake inhibitor in native tissue systems, making it valuable for investigating the mechanisms underlying antidepressant therapies. Its ability to modulate serotonergic signaling supports its role in research related to mood disorders and other neuropsychiatric conditions. -
5-HT1 Agonist
IS-159 is a potent agonist of the serotonin 5-HT1 receptor. This compound demonstrates significant biological activity in modulating serotonergic signaling, making it a valuable tool for researching migraine pathophysiology and potential therapeutic interventions. Its selective action on the 5-HT1 receptor provides insights into serotonin-related mechanisms in migraine and other related disorders. -
5-HT3 Receptor Antagonist
Cilansetron is a selective 5-HT3 receptor antagonist that inhibits serotonin-mediated signaling at this receptor subtype. It is primarily utilized in research focused on gastrointestinal disorders, particularly in studies of irritable bowel syndrome. Cilansetron's ability to modulate gut motility and visceral hypersensitivity makes it a valuable tool for investigating therapeutic strategies for related conditions. -
5-HT2 Ligand
4-Bromo-2,5-DMMA is a selective ligand for the 5-HT2 receptor. It demonstrates a significant affinity for 5-HT2 binding sites, with an effective dose (ED50) of 0.82 mg/kg observed in rat discrimination tests. This compound is utilized in pharmacological research focusing on serotonergic signaling and its implications in neuropsychopharmacology. -
5-HT1BR Inverse Agonist
SB-236057 is an inverse agonist of the 5-HT1B receptor, known for its significant impact on skeletal development in animal models. This compound influences gene expression during embryonic development by disrupting the Notch signaling pathway and interacting with r-esp1. In preclinical studies, SB-236057 has been shown to cause somatic patterning and tail extension defects in rat embryos, making it a valuable tool for investigating developmental biology and teratogenicity. -
5-HT3 Antagonist
MCI-225 is a selective antagonist of the 5-HT3 receptor, with notable activity as a noradrenaline reuptake inhibitor. This compound exhibits antidepressant effects in vivo, making it valuable for research focused on mood disorders and neuropharmacology. Its unique mechanism can aid in the investigation of therapeutic strategies addressing serotonergic and noradrenergic system interactions. -
5-HT Uptake Inhibitor
Litoxetine is a selective 5-HT uptake inhibitor that functions primarily through its action on serotonin transporters. It also acts as a 5-HT3 receptor antagonist, exhibiting a Ki value of 85 nM for cerebral 5-HT3 receptors. This compound is utilized in research related to depression and nausea, showcasing its potential as an antidepressant and antiemetic agent. -
5-HT1A Partial Agonist
Zalospirone is a cyclic imide and a partial agonist of the 5-HT1A receptor. It exhibits antidepressant-like activity, making it a valuable candidate for research into mood disorders. Its mechanism of action may provide insights into neuropharmacology and potential therapeutic applications in the treatment of depression. -
5-HT3/5-HT4 Receptor Antagonist
Fabesetron hydrochloride is an orally active antagonist of the 5-HT3 and 5-HT4 receptors. This compound demonstrates significant efficacy in mitigating both acute and delayed emesis associated with cancer chemotherapy. Fabesetron hydrochloride serves as a valuable tool in research on anti-emetic therapies and the management of nausea and vomiting in oncological treatments. -
5-HT Receptor
WAY 163909 hydrochloride is a selective agonist of the 5-hydroxytryptamine receptor 2C (5-HT2C) with an EC50 of 8 nM and maximum efficacy reaching 90%. Exhibiting minimal interaction with 5-HT2A receptors, it demonstrates a Ki value of 10.5 nM for 5-HT2C, while showing much higher Ki values of 212 nM for 5-HT2A, 343 nM for 5-HT7, and 485 nM for 5-HT2B. This specificity makes it a valuable tool for studying the physiological and pharmacological roles of the 5-HT2C receptor in various biological systems. -
5-HT6 Receptor Modulator/Lp-PLA2 Inhibitor
Goxalapladib is a selective modulator of the 5-HT6 receptor that also serves as an inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Its mechanism of action suggests potential applications in the investigation of atherosclerosis-related cardiovascular diseases. This compound facilitates research into the modulation of lipid metabolism and inflammation, making it a valuable tool for studies focused on cardiovascular health. -
5-HT Antagonist
p-MPPF dihydrochloride is a selective 5-HT antagonist that effectively inhibits the reduction of phosphorylated Erk1/2 levels in the hippocampus caused by 8-OH-DPAT in rat models. This compound is valuable for studying the neurochemical pathways involved in neurological diseases, making it a key reagent in neuroscience research. -
5-HT1/D2 Agonist
Sarizotan dihydrochloride is a potent agonist of the serotonin 5-HT1A receptor and dopamine receptors. It demonstrates strong activity with IC50 values of 6.5 nM for rat 5-HT1A, 0.1 nM for human 5-HT1A, 15.1 nM for rat D2, 17 nM for human D2, 6.8 nM for human D3, and 2.4 nM for human D4.2. Sarizotan dihydrochloride is utilized in research to explore neuropharmacology, behavior, and potential therapeutic effects on psychiatric disorders. -
5-HT3 Receptor Antagonist
Itasetron is a selective 5-HT3 receptor antagonist known for its potent antiemetic properties. This compound has been shown to enhance spatial learning and memory in aged rat models, making it relevant for studies on age-related cognitive decline. Research applications include investigations into memory degeneration and the therapeutic potential of 5-HT3 receptor modulation in cognitive disorders. -
5-HT Receptor Agonist
25I-NBMD hydrochloride is a potent agonist of the 5-HT2A receptor, a key target in serotonin signaling pathways. This compound enhances the affinity and activity at this receptor, making it valuable for research investigating serotonin-related effects and behaviors. Its unique structure positions it as a useful tool for exploring the pharmacological properties of hallucinogenic compounds and their influence on neuropsychiatric conditions. -
5-HT Receptor Control
8-Hydroxy mirtazapine primarily targets 5-HT receptors, functioning as a significant metabolite of the antidepressant Mirtazapine. It is produced through the enzymatic action of cytochrome P450 isoform CYP2D6. This compound is utilized in research focused on serotonin receptor modulation and its implications in mood disorders.
