Catalog No.
Product Name
Application
Product Information
Citations
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5-HT6 Receptor Ligand
E-6837 is an orally active selective ligand for the 5-HT6 receptor, exhibiting partial agonism at the rat 5-HT6 receptor and full agonism at the constitutively active human variant, as evidenced by modulation of the cAMP signaling pathway. This compound has been shown to induce hypophagia, decrease fat mass and body weight, and enhance glycemic control. E-6837 is a valuable tool for research applications related to obesity and metabolic disorders. -
5-HT Receptor
m-Chlorophenylbiguanide (mCPBG) is a high-affinity agonist of the 5-HT3 receptor, known to inhibit long-term potentiation (LTP) in the mossy fiber-CA3 circuit. It effectively reduces the magnitude of LTP at concentrations ranging from 0.3 to 1 µM, highlighting its significant role in the modulation of synaptic plasticity. Furthermore, the reversible nature of mCPBG's effect on LTP in the presence of the GABAA receptor antagonist bicuculline suggests its involvement in GABAergic neurotransmission pathways. -
5-HT2A Agonist
5-HT2A agonist 5 is a potent 5-HT2A receptor agonist with an EC50 of 0.01 nM for human 5-HT2A. This compound is valuable in the research of neuropsychiatric conditions such as depression, drug addiction, and alcoholism, as well as post-traumatic stress disorder (PTSD) and neuropathic pain. Its high potency makes it a useful tool for investigating the therapeutic potential of 5-HT2A modulation in various biological studies. -
5-HT4 Agonist
TKS 159 is a selective agonist of the 5-HT4 receptor, facilitating enhanced gastrointestinal motility. This compound is particularly relevant for studies investigating gastrointestinal disorders and their potential therapies. TKS 159’s role in promoting motility makes it a valuable tool for researchers exploring the pharmacological modulation of gut function. -
5-HT1 Receptor Agonist
3,4-Dihydro Naratriptan is a selective agonist of the serotonin 5-HT1 receptor. It demonstrates potent vasoconstrictor activity, making it relevant in studies related to migraine pathology. This compound is useful for research aimed at understanding migraine mechanisms and developing potential therapeutic strategies. -
5-HT2C Antagonist
5-HT2C antagonist 1 is a selective and orally bioavailable antagonist of the 5-HT2C receptor, exhibiting a pKi of 8.0. This compound effectively inhibits mCPP-induced penile erection in rat models, highlighting its potential in neurological and endocrinological research. It serves as a valuable tool in studies related to anxiety and other related disorders. -
5-HT7R Antagonist
5-HT7R Antagonist 3 is a selective antagonist of the 5-HT7 receptor, exhibiting a Ki value of 8 nM, which illustrates its high affinity for the target. It shows lower affinity for other receptors, such as D2 (Ki: 511 nM), 5-HT1A (Ki: 8930 nM), and 5-HT2A (Ki: 5786 nM). This compound demonstrates significant antidepressant and anxiolytic effects in murine models, making it a valuable tool for research in mood disorders and anxiety-related conditions. -
5-HT Reuptake Inhibitor
Ifoxetine hemisulfate is a selective inhibitor of the serotonin (5-HT) reuptake process in the central nervous system. By specifically targeting 5-HT transporters, it effectively blocks serotonin reuptake in the brain while sparing peripheral uptake in blood platelets. This compound shows promise for its antidepressant properties and is utilized in research focused on mood regulation and neuropharmacology. Additionally, Ifoxetine hemisulfate has been demonstrated to inhibit the uptake of radiolabeled 5-HT in rat brain synaptosomes, providing valuable insights into serotonin dynamics and receptor interactions. -
5-HT1/5-HT2/adrenergic (α1) Receptors Antagonist
Centpropazine is a non-selective antagonist of serotonin (5-HT1/5-HT2) and adrenergic (α1) receptors. It modulates monoamine neurotransmission by reducing the reuptake of serotonin and norepinephrine, leading to antidepressant effects. This compound is valuable for research into depression and related mood disorders, facilitating insights into neurotransmitter dynamics and their role in mental health. -
5-HT2B Antagonist
VU0631019 is a selective antagonist of the serotonin receptor 5-HT2B, exhibiting an IC50 value of 29 nM. This compound is useful in studying the role of 5-HT2B in various physiological processes and disease states. Due to its predicted limited ability to penetrate the blood-brain barrier and potential for P-glycoprotein-mediated efflux, VU0631019 can be utilized in in vitro and ex vivo experimental settings to explore peripheral effects of 5-HT2B modulation. -
5-HT7 Receptor Antagonist
DR-4004 is a selective antagonist of the 5-HT7 receptor, known for its ability to mitigate performance impairments induced by mCPP and restore function following p-chloroamphetamine lesions affecting the serotonergic system. Additionally, DR-4004 effectively reverses amnesia induced by Scopolamine and Dizocilpine, highlighting its potential in cognitive enhancement research. This compound is particularly relevant for investigations into schizophrenia, cognitive deficits, and the development of atypical antipsychotic agents. -
D2R/D3R/5-HT1AR Agonist
D2R/D3R/5-HT1AR agonist 1 is an orally active compound that selectively targets dopamine receptors D2R and D3R, as well as the serotonin receptor 5-HT1AR, exhibiting EC50 values of 1.29 nM, 1.05 nM, and 153.5 nM, respectively. This compound has demonstrated efficacy in alleviating behavioral disorders induced by MPTP and possesses anti-depressant properties. D2R/D3R/5-HT1AR agonist 1 is valuable for research in the fields of Parkinson's disease and depression, aiding in the exploration of potential therapeutic interventions. -
5-HT2 Receptor Agonist
4-Hydroxy MPT is a potent agonist of the 5-HT2A and 5-HT2B serotonin receptors, exhibiting EC50 values of 3.82 nM and 3.4 nM, respectively. This compound serves as a crucial tool in research focused on serotonergic pathways and their role in neuropharmacology. Its applications extend to studying the mechanisms of action of hallucinogens and exploring potential therapeutic targets for psychiatric disorders. -
5-HT Receptor Antagonist
LY-272015 is a selective antagonist of the 5-HT2B receptor, demonstrating efficacy in modulating signaling pathways related to serotonin activity. It effectively inhibits the phosphorylation of ERK2 induced by serotonin or BW723C86, making it a valuable tool for studying serotonin receptor functions. Additionally, LY-272015 exhibits antihypertensive properties in animal models, specifically in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats, supporting its use in cardiovascular research. -
5-HT4 Receptor Agonist
PRX-03140 is a selective 5-HT4 receptor agonist that effectively crosses the blood-brain barrier, exhibiting a Ki value of 110 nM against the rat brain 5-HT4 receptor. This compound enhances cortical levels of acetylcholine and histamine, making it a valuable tool for investigating cognitive function. PRX-03140 is particularly relevant for research applications related to Alzheimer’s disease, where modulation of neurotransmitter systems is critical. -
5-HT1B/1D Receptor Agonist
Donitriptan hydrochloride is a potent agonist of the 5-HT1B and 5-HT1D receptors, exhibiting high efficacy with pKis of 9.4 and 9.3, respectively. This compound is primarily utilized in research focused on migraine treatments and the modulation of serotonin pathways. Its strong receptor activity makes it a valuable tool for studying the pharmacological effects of serotonin receptor signaling in various biological contexts. -
5-HT6 Antagonist
BVT-74316 is a selective antagonist of the 5-HT6 receptor, which plays a crucial role in appetite regulation. This compound has demonstrated the ability to significantly reduce food intake and body weight gain in rodent models, making it an important tool for research into metabolic disorders, particularly obesity. BVT-74316 is valuable for studies focused on the mechanisms of appetite control and energy balance. -
5-HT Agonist
Serotonin maleate acts as a selective agonist for 5-HT receptors in the central nervous system, influencing various physiological processes, including mood regulation and cognitive function. Additionally, it serves as a catechol O-methyltransferase (COMT) inhibitor with a Ki value of 44 μM, making it valuable for research involving neurotransmitter dynamics and the modulation of serotonergic pathways. Its multiple biological activities position it as a critical reagent for studies in neuroscience and pharmacology. -
5-HT5A Receptor Agonist
UCSF678 is a 5-HT5A receptor agonist exhibiting a partial agonist profile with an affinity of 42 nM. This compound demonstrates arrestin-biased signaling, providing a more focused exploration of the 5-HT5AR pathway with fewer off-target effects and reduced assay-related issues. UCSF678 serves as a valuable tool for investigating the physiological roles and functional dynamics of the 5-HT5A receptor in various research applications. -
5-HT Receptor Agonist
CGS 12066 dimaleate is a selective agonist of the 5-HT1B receptor, exhibiting an IC50 of 51 nM. This compound enhances serotonergic signaling and is utilized in research focused on neuropharmacology and psychiatric disorders. Its specific action on the 5-HT1B receptor makes it a valuable tool for investigating serotonin-related pathways and potential therapeutic targets. -
5-HT₂ Receptor Anagonist
Setoperone is a potent antagonist of the 5-HT₂ receptor with moderate activity at dopamine D₂ receptors. Its unique pharmacokinetics allow it to dissociate rapidly from receptors while maintaining prolonged inhibition of serotonin signaling. This compound is valuable in research focused on the negative symptoms of type II schizophrenia and related mood disorders, providing insights into serotonergic and dopaminergic system interactions. -
5-HT1B Receptor Antagonist
GR 55562 is a selective antagonist of the 5-HT1B receptor, which plays a crucial role in serotonin neurotransmission. This compound is primarily utilized in neuropharmacology research to investigate the implications of serotonin signaling in various neurological disorders. GR 55562 provides valuable insights into potential therapeutic approaches for conditions related to nerve function and dysfunction. -
5-HT2C Inhibitor
SB 242084 monohydrochloride is a selective and high-affinity antagonist of the 5-HT2C receptor with a pKi value of 9.0. This compound effectively enhances the basal activity of dopaminergic neurons in the ventral tegmental area, stimulating dopamine release in the vomeronasal nucleus. Additionally, SB 242084 promotes mitochondrial gene expression and oxidative metabolism through 5-HT2A receptor interactions. Its potential applications in research include the investigation of negative symptoms associated with anxiety, depression, and schizophrenia, as well as the study of acute organ damage. -
5-HT3 Receptor Antagonist
5-HT3 antagonist 5 is a quinoxalin-2-carboxamide that functions as a selective antagonist of the 5-HT3 receptor. It demonstrates effective inhibition of 5-HT3 agonists, including 2-methyl-5-HT, and exhibits antidepressant-like effects in murine models. This compound is suitable for research applications in neuropharmacology and behavioral studies related to serotonin signaling and mood disorders. -
5-HT1D Receptor Agonist
Rizatriptan is a potent and selective agonist of the 5-HT1D receptor. It is primarily utilized in research focused on migraine pathophysiology and treatment, contributing to the understanding of serotonin signaling in this condition. This compound's ability to effectively activate the 5-HT1D receptor makes it a valuable tool for exploring therapeutic strategies in migraine management. -
5-HT1 Receptor Agonist
Sumatriptan hydrochloride is a potent 5-HT1 receptor agonist, exhibiting 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 plays a significant role in the study of migraine pathophysiology and treatment. Its primary biological activity aids in the understanding and management of migraine headaches in research settings. -
5-HT6R Antagonist
SGS518 oxalate is a selective antagonist of the 5-HT6 receptor. It exhibits significant potential in research related to cognitive impairments, including amnesia, anxiety, and depression. Additionally, SGS518 oxalate has demonstrated efficacy in protecting the mouse retina at elevated doses, providing a valuable tool for studies in neuroprotection and cognitive function. -
5-HT1B Agonist
CP 93129 is a potent and selective agonist of the 5-HT1B receptor. This compound exhibits significant biological activity in modulating serotonergic signaling, making it a valuable tool in the study of various neurological conditions. CP 93129 is particularly relevant for research applications related to Parkinson's disease, where serotonergic pathways are implicated in disease progression and symptomatology. -
Quetiapine Metabolite
Quetiapine sulfone is a primary metabolite of Quetiapine, acting predominantly as a serotonin (5-HT) receptor agonist and a dopamine receptor antagonist. This compound is essential for studying the pharmacokinetics and efficacy of Quetiapine in various neurological disorders, including schizophrenia and bipolar disorder. Its role in modulating neurotransmitter systems makes it a valuable reagent for researchers exploring antipsychotic mechanisms and drug metabolism. -
5-HT4(e) Receptor Partial Agonist
Capeserod hydrochloride is a potent partial agonist of the 5-HT4(e) receptor, demonstrating a Ki value of 0.6 nM. This compound effectively stimulates cAMP production in cells expressing both 5-HT4(b) and 5-HT4(e) splice variants, with IC50 values of 244 nM and 29 nM, respectively. Capeserod hydrochloride is primarily utilized in research focused on cognitive enhancement, memory impairment, and dementia-related studies. -
D2/5-HT2A Receptors Antagonist
Clocapramine dihydrochloride hydrate is a potent antagonist of the D2 and 5-HT2A receptors. It demonstrates significant biological activity by inhibiting the signaling pathways associated with these receptors, making it valuable for pharmacological research. This compound is particularly useful in studies related to neuropharmacology, psychopharmacology, and the development of therapeutic agents targeting psychiatric disorders. -
5-HT2C Receptor Agonist
PF-04781340 is a potent and selective agonist of the 5-HT2C receptor. This compound exhibits oral bioavailability and demonstrates effective penetration of the central nervous system. PF-04781340 is relevant for research applications involving mood regulation, appetite control, and other neuropsychiatric disorders, making it a valuable tool for studies exploring serotonin receptor modulation. -
GlyT2/5HT2A Antagonist
Opiranserin is a dual antagonist of the glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), exhibiting IC50 values of 0.86 μM and 1.3 μM, respectively. Additionally, it demonstrates antagonistic activity on the recombinant P2X3 receptor with an IC50 of 0.87 μM. This compound is being developed as an injectable analgesic for the management of postoperative pain, highlighting its potential utility in pain research and pharmacological studies. -
5-HT Receptor Agonist
Deramciclane fumarate is a selective inverse agonist of the 5-HT2C receptor, exhibiting an IC50 of 168 nM. This compound modulates serotonin receptor activity, leading to decreased basal phosphoinositide hydrolysis. Deramciclane fumarate is utilized in research applications focused on neuropharmacology and the investigation of serotonin-related pathways. -
5-HT2A Receptor Agonist
5-HT2A Receptor Agonist-9 is a β-arrestin-biased agonist specifically targeting the 5-HT2A receptor. This compound exhibits significant biological activity associated with modulation of serotonin pathways, making it a valuable tool in the study of neurological disorders, including antidepressant effects and psychedelic research. Its unique mechanism offers potential insights into receptor signaling dynamics relevant to neuropharmacology. -
5-HT/Dopamine Antagonist
BGC20-761 is a selective antagonist of the 5-HT6 and dopamine receptors, exhibiting human receptor Ki values of 20 nM for 5-HT6, 69 nM for 5-HT2A, and 140 nM for D2. It has demonstrated the ability to enhance long-term memory, suggesting its potential utility in cognitive enhancement therapies. Additionally, BGC20-761 may serve as a promising candidate for the development of antipsychotic agents, supporting research in neuropharmacology and mental health disorders. -
5-HT1A Antagonist
5-HT1A Antagonist 2 is a selective antagonist of the 5-hydroxytryptamine 1A (5-HT1A) receptor. This compound is instrumental in investigating the physiological and pharmacological roles of the 5-HT1A receptor in disorders such as depression and attention deficit hyperactivity disorder (ADHD). Its ability to modulate serotonin signaling makes it a valuable tool in neuropharmacological research. -
5-HT Agonist
Tiflucarbine is a potent agonist of serotonin receptors (5-HT), specifically acting on both 5-HT1 and 5-HT2 subtypes. As a derivative of tetrahydrothieno-7-carboline, Tiflucarbine exhibits significant antidepressant properties through its interaction with central 5-HT binding sites. This compound is valuable for research applications focused on depression, anxiety disorders, and other conditions linked to serotonin dysregulation. -
5-HT Receptor
R 50595 hydrochloride is a selective noncompetitive antagonist of the 5-HT receptor. This compound effectively inhibits the actions of cisapride and BRL 24924, demonstrating a complete blockade of 5-HT effects at concentrations up to 3 X 10(-7) M without influencing responses to electrical stimulation. R 50595 hydrochloride is valuable for researchers investigating serotonin receptor signaling and related pathways in pharmacological studies. -
5-HT2A Agonist
5-HT2A Agonist 7 is a highly selective agonist for the serotonin receptor 2A (5-HT2A), exhibiting an EC50 value of 12 nM. This compound demonstrates significant biological activity and is particularly relevant for research into psychiatric disorders, including depression. Its oral bioavailability enhances its potential for in vivo studies, making it a valuable tool for investigating the role of 5-HT2A in neuropsychiatric conditions. -
5-HT Receptor Agonist
Rizatriptan hemisulfate hemihydrate is a potent agonist of the 5-HT1B and 5-HT1D serotonin receptors. It exhibits peripheral vasoconstrictive properties and effectively crosses the blood-brain barrier, making it valuable for modulating pain neurotransmission within the central nervous system. This compound is primarily used in research related to migraine pathophysiology and the study of serotonin receptor mechanisms. -
5-HT2A Agonist
5-HT2A receptor agonist-7 is a selective agonist for the 5-HT2A receptor. It demonstrates a compelling biological activity with an EC50 value of less than 100 nM, making it a potent tool for the modulation of serotonergic signaling. This compound is useful in research applications focused on understanding mood disorders, psychotropic drug actions, and neuropharmacology involving serotonergic pathways. -
5-HT Receptor Agonist
2C-TFM hydrochloride is a potent agonist of the 5-HT receptor subtypes 5-HT2A and 5-HT2C, known for its para-trifluoromethyl substitution on a 5-dimethoxyphenethylamine framework. This compound exhibits significant biological activity related to serotonin receptors, making it valuable for research in neuropharmacology and the study of serotonergic signaling pathways. It may be utilized in investigations of mood disorders, anxiety, and other conditions influenced by serotonin receptor modulation. -
5-HT4 Receptor Agonist
THRX-194556 is a 5-HT4 receptor agonist that enhances gastrointestinal motility and may play a role in cognitive function. Its primary biological activity makes it a valuable tool for studying gastrointestinal functional disorders and Alzheimer's disease. This compound can help elucidate the therapeutic potential of 5-HT4 receptor modulation in various pathological conditions. -
5-HT6R Antagonist
SGS-518 is a selective antagonist of the 5-HT6 receptor. It exhibits potential therapeutic effects in the study of cognitive impairments, including amnesia, anxiety, and depression. Additionally, SGS-518 has been shown to provide protective effects in mouse retina at elevated doses, offering valuable insights for neuroprotective research applications. -
5-HT2CR Agonist
5-HT2CR agonist 1 is a selective partial agonist of the 5-HT2C receptor, displaying an effective maximum response (Emax) of 71.09% and an EC50 of 121.5 nM. This compound has been shown to exhibit specificity, with no activity towards 5-HT2A or 5-HT2B receptors. Furthermore, it demonstrates no recruitment activity for β-arrestin and minimal inhibition of hERG channels at 10 μM. This profile makes 5-HT2CR agonist 1 a valuable tool for research in neuropharmacology and receptor signaling pathways. -
D2 Antagonist
Clozapine dihydrochloride is an antipsychotic compound that primarily functions as a dopamine D2 receptor antagonist, exhibiting a Ki of 75 nM. It demonstrates significant affinity for muscarinic M1 and serotonin 5HT2A receptors, with Kis of 9.5 nM and 4 nM, respectively. Additionally, Clozapine acts as a potent and selective agonist at the muscarinic M4 receptor, with an EC50 of 11 nM. This compound is crucial for research into schizophrenia and related neuropsychiatric disorders. -
5-HT7/5-HT1A Receptor Agonist
E-55888 is a selective and potent agonist of the 5-HT7 and 5-HT1A receptors, exhibiting Ki values of 2.5 nM and 700 nM, respectively. This compound demonstrates significant analgesic and antinociceptive properties, effectively reducing the nociceptive response in capsaicin-sensitized mice. E-55888 serves as a valuable tool for researchers investigating pain mechanisms and therapeutic approaches to pain management. -
Triple Reuptake Inhibitor
Tedatioxetine is a serotonin and norepinephrine-preferring triple reuptake inhibitor (TRI) that also functions as an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors. This compound exhibits significant biological activity in modulating neurotransmitter levels, making it relevant for research in neuropharmacology. Its mechanism of action positions it as a valuable tool in studies related to mood disorders and anxiety. -
5-HT2A Receptor Agonist
5-HT2A receptor agonist-2 is a potent agonist targeting the serotonin 5-HT2A receptor. It demonstrates high affinity with EC50 values of 1.7 nM for 5-HT2A, 0.58 nM for 5-HT2B, and 0.50 nM for 5-HT2C receptors. This compound is valuable for research into serotonin signaling pathways and their implications in neuropsychiatric disorders, as well as in studies evaluating receptor pharmacology and function.
