Catalog No.
Product Name
Application
Product Information
Citations
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5-HT1A antagonist
DU125530 is a potent and selective antagonist of the 5-HT1A receptor, demonstrating Ki values of 0.7 nM for 5-HT1A and significantly higher values for other serotonin receptors. This compound exhibits antidepressant properties, making it a valuable tool for research into mood disorders and serotonin signaling pathways. It is particularly relevant for studies aimed at understanding the role of 5-HT1A receptor modulation in behavioral and neurochemical responses. -
5-HT6 Antagonist
5-HT6 Inverse Agonist 1 is a selective antagonist of the 5-HT6 receptor, exhibiting a Ki of 23 nM and a Kb of 6.62 nM. This compound effectively inhibits the 5-HT6R-mediated signaling pathways, including Cdk5 and mTOR. Additionally, 5-HT6 Inverse Agonist 1 has demonstrated efficacy in reducing tactile hypersensitivity in a rat model of spinal nerve ligation, making it a valuable tool for research into pain management and neurobiology. -
5-HT Receptor Agonist
TMPPAA is an allosteric agonist and positive allosteric modulator of the 5-HT3 receptor. It enhances serotonin (5-HT)-mediated signaling through the 5-HT3A receptor, making it a valuable tool for studying 5-HT3 receptor pharmacology. TMPPAA is applicable in research related to neurotransmission, pain pathways, and gastrointestinal functioning. -
5-HT Inhibitor
Femoxetine hydrochloride is a selective serotonin (5-HT) inhibitor known for its antidepressant properties. By inhibiting the reuptake of serotonin, it elevates serotonin levels within the synaptic cleft, thereby enhancing serotonergic signaling. This compound is valuable in research focusing on the role of serotonin in mood regulation and its implications in depression and related emotional disorders. -
5-HT2A Receptor Antagonist
Temanogrel hydrochloride is a selective antagonist of the 5-HT2A receptor, exhibiting a Ki value of 4.9 nM. This compound is primarily utilized in research related to serotonergic pathways and their implications in various neuropsychiatric disorders. Its use in pharmacological studies can provide insights into the modulation of serotonin receptors and their role in cardiovascular and central nervous system functions. -
5-HT2C Agonist
5-HT2C agonist-5 is a potent 5-HT2C receptor agonist with an EC50 of less than 1 nM. This compound demonstrates significant biological activity through modulating serotonin signaling pathways, making it a valuable tool for investigating neuropsychiatric and neurodegenerative disorders. Its application in research may provide insights into the therapeutic potential of targeting 5-HT2C receptors in various brain-related conditions. -
5-HT2C Receptor Agonist
PF-4479745 is a potent and selective agonist of the 5-HT2C receptor, demonstrating an EC50 of 10 nM and a Ki of 15 nM. This compound has significant biological activity relevant to cardiovascular research, particularly in the study of conditions such as hypertension. Its selectivity for the 5-HT2C receptor makes it an invaluable tool for elucidating the role of serotonin signaling in cardiovascular disease mechanisms. -
5-HT Receptor Inhibitor
Org 6582 is a competitive and selective inhibitor of the 5-HT receptor, demonstrating a Ki value of 89 nM. This compound exhibits a long-lasting inhibitory effect on serotonin uptake, persisting for over 48 hours. Org 6582 is primarily utilized in research focusing on depressive disorders, providing valuable insights into serotonergic modulation in various neuropsychological studies. -
Antidepressant Agent
Captodiame, a 5-HT2c receptor antagonist, exhibits significant antidepressant activity by modulating serotonin signaling. In addition, it acts as an agonist at sigma-1 and D3 dopamine receptors, enhancing its therapeutic potential. This compound is of interest for researchers focused on neuropharmacology and the development of novel antidepressant therapies. -
5-HT Receptor Antagonist
Alverine is a selective 5-HT1A receptor antagonist, exhibiting an IC50 value of 101 nM. This compound is primarily utilized in research focused on gastrointestinal disorders and the modulation of serotonin signaling pathways. Its antagonistic activity at the 5-HT1A receptor may provide insights into the mechanisms underlying dysregulation of serotonin-related pathologies. -
5-HT2A/dopamine D2 Antagonist
Abaperidone hydrochloride is a potent antagonist of the 5-HT2A receptor and dopamine D2 receptor, exhibiting IC50 values of 6.2 nM and 17 nM, respectively. This compound demonstrates significant affinity in modulating serotonergic and dopaminergic signaling pathways, making it a valuable tool for studying neuropharmacology and the treatment of psychiatric disorders. Research applications include investigations into schizophrenia, anxiety, and mood disorders. -
5-HT2A Agonist
5-HT2A agonist 3 is a highly selective agonist for the 5-hydroxytryptamine 2A receptor (5-HT2A), exhibiting an EC50 value of 13.80 nM. This compound is valuable for investigating various mental health disorders, including depression, post-traumatic stress disorder, and obsessive-compulsive disorder. Its specific action on the 5-HT2A receptor provides a crucial tool for studying central nervous system functions and the underlying mechanisms of these conditions. -
5-HT Receptor Antagonist
5-HT3 antagonist 2 is a selective antagonist of the 5-HT3 receptor, a subtype of the serotonin receptor. This compound exhibits significant biological activity by inhibiting the effects of serotonin, making it useful in research focused on neurotransmission, gastrointestinal function, and the treatment of nausea and anxiety disorders. Its application in pharmacological studies supports the development of therapeutic strategies targeting the 5-HT3 receptor pathway. -
5-HT Receptor Antagonist
Zatosetron maleate is a potent and selective antagonist of the 5-HT3 receptor. This compound exhibits strong inhibitory effects on serotonin signaling, making it valuable in exploring gastrointestinal functions and managing nausea and vomiting. Its utility extends to various research applications, including studying neuropharmacology and the role of serotonin in mood regulation. -
5-HT Receptor Antagonist
Alosetron-d3 hydrochloride is a deuterium-labeled derivative of Alosetron, functioning as a selective antagonist of the serotonin 5-HT3 receptor. This compound exhibits significant potency in modulating gastrointestinal activity and is primarily utilized in research focused on understanding and treating disorders related to serotonin signaling, such as irritable bowel syndrome. Alosetron-d3 hydrochloride serves as a valuable tool for investigating the role of 5-HT receptors in various biological processes. -
Adrenergic Receptor Antagonist
(4E)-SUN9221 is a potent antagonist of the α1-adrenergic receptor and the 5-HT2 receptor, demonstrating significant biological activity in modulating cardiovascular responses. This compound exhibits antihypertensive effects and inhibits platelet aggregation, making it a valuable tool for research in hypertension and thrombosis. Its ability to selectively target these receptors provides insights into adrenergic signaling and related pathological conditions. -
5-HT Receptor Inhibitor
5-HT3-In-1 is a selective inhibitor of the 5-HT3 receptor, effectively blocking serotonin's action at this target. This compound demonstrates notable efficacy in inhibiting 5-HT3-mediated signaling pathways, making it valuable for research focused on neuropharmacology and gastrointestinal function. Its use extends to studying various conditions, including anxiety, depression, and nausea-related disorders. -
5-HTIDβ Receptor Agonist
5-(Nonyloxy)tryptamine oxalate is a selective agonist for the 5-HTIDβ receptor, demonstrating a high affinity with an ED50 value of 68 nM. This compound exhibits significant antitumor activity in vivo and has been shown to enhance the efficacy of T cell-mediated targeting of tumor cells. Its applications in cancer research and immunotherapy make it a valuable tool for studying receptor signaling and cellular responses in tumor microenvironments. -
D3 Receptor Antagonist
RGH-1756 is a selective antagonist of the human D3 dopamine receptor, exhibiting pronounced effects in modulating dopaminergic pathways. This compound demonstrates lesser antagonistic activity on the human D2L and 5HT1A receptors. RGH-1756 is primarily utilized in research focusing on neuropharmacology and the mechanism of antipsychotic treatments, particularly in understanding conditions related to dopamine dysregulation. -
5-HT Receptor Agonist
Donitriptan mesylate is a potent agonist of the 5-HT1B and 5-HT1D receptors, demonstrating high efficacy with pKis of 9.4 and 9.3, respectively. This compound is primarily utilized in research focused on migraine treatments and neurological disorders, enabling studies on serotonin receptor signaling pathways. Its strong affinity for 5-HT receptors makes it a valuable tool for exploring the role of serotonin in various biological processes. -
5-HT/DA Receptor Antagonist
Ziprasidone mesylate is a potent antagonist of the 5-HT and dopamine receptors, specifically targeting the Rat D2 receptor (Ki=4.8 nM), the 5-HT2A receptor (Ki=0.42 nM), and the 5-HT1A receptor (Ki=3.4 nM). This compound demonstrates significant activity in modulating serotonergic and dopaminergic pathways, making it valuable for research in psychiatric disorders, such as schizophrenia and mood disorders. Its unique pharmacological profile allows for a better understanding of the interplay between these neurotransmitter systems in various biological contexts. -
5-HT Receptor Agonist
RS 67333 is a selective agonist of the 5-HT4 receptor, known for its stress-preventive properties. This compound has been shown to mitigate stress-induced changes in body weight and to alleviate depression- and anxiety-like behaviors across various mouse models. Its potential applications include studies on stress response, mood disorders, and the neurobiological mechanisms underlying anxiety and depression. -
5-HT6 Receptor Antagonist
Ro 04-6790 di(hydrochloride) is a potent and selective antagonist of the 5-HT6 receptor, exhibiting pKi values of 7.26 and 7.35 for rat and human 5-HT6 receptors, respectively. This compound demonstrates a high degree of specificity, showing no significant affinity for other receptors. Ro 04-6790 di(hydrochloride) is primarily utilized in neurological research to elucidate the role of 5-HT6 receptor modulation in various physiological and pathological processes. -
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.
