Catalog No.
Product Name
Application
Product Information
Citations
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5-HT7 Receptor Agonist
LP 12 hydrochloride is a potent and selective agonist of the 5-HT7 receptor, exhibiting a Ki value of 0.13 nM. This compound demonstrates significant selectivity for the 5-HT7 receptor compared to D2, 5-HT1A, and 5-HT2A receptors, with Ki values of 224 nM, 60.9 nM, and >1000 nM, respectively. LP 12 hydrochloride is valuable for research applications focusing on serotonin receptor signaling and its implications in neuropharmacology. -
5-HT Receptor Agonist
25C-NBF hydrochloride is a selective agonist of the 5-HT receptors, specifically activating both the 5-HT2A and 5-HT2C subtypes with similar efficacy (EC50s approximately 0.3 μM for each). This compound is valuable for research applications focused on serotonergic signaling pathways, neuropharmacology, and the study of psychoactive effects associated with serotonin receptor modulation. Its activity may provide insights into various neuropsychiatric disorders and facilitate the development of novel therapeutic strategies. -
5-HT Agonist
F-14258 is a selective agonist for the 5-HT1B and 5-HT1D serotonin receptors. This compound demonstrates receptor-specific analgesic properties, making it particularly useful in the study of localized pain mechanisms. F-14258 is applicable in research focused on addressing ear pain and related sensory disorders. -
5-HT6 Agonist
WAY-181187 hydrochloride is a potent and selective full agonist of the 5-HT6 receptor, exhibiting a Ki of 2.2 nM and an EC50 of 6.6 nM. This compound activates 5-HT6 receptor-dependent signaling pathways, including cAMP, Fyn, and ERK1/2 kinase, making it a valuable tool for research into neuropharmacology and the modulation of serotonergic pathways. Its selective action supports investigations into potential therapeutic applications for cognitive disorders and other conditions influenced by serotonin signaling. -
5-HT receptor antagonist
MS 245 is a potent antagonist of the 5-HT6 receptor, exhibiting a Ki value of 1.5 nM. This compound is primarily utilized in research applications aimed at understanding serotonin signaling and its implications in neuropharmacology. MS 245's inhibition of the 5-HT6 receptor can aid in the investigation of potential therapeutic strategies for cognitive disorders and mood regulation. -
D2/5-HT1A Agonist
Bifeprunox is a potent partial agonist for the dopamine D2 receptor and the 5-HT1A receptor, exhibiting a pKi of 7.19 for cortex 5-HT1A and 8.83 for striatum D2. It demonstrates a pEC50 of 6.37 for hippocampus 5-HT1A. This compound is utilized in research related to antipsychotic mechanisms and is particularly relevant for studies focusing on schizophrenia. -
5-HT Receptor Agonist
F-15599 tosylate is a selective G-protein biased agonist of the 5-HT1A receptor, exhibiting a Ki of 3.4 nM. This compound demonstrates significant biological activity in modulating serotonergic neurotransmission and is valuable in researching anxiety, depression, and other neuropsychiatric disorders. Its specificity makes it a useful tool for elucidating the role of 5-HT1A receptors in various physiological and pathological processes. -
5-HT Receptor Modulator
Eltoprazine dihydrochloride is a dual-action modulator of the serotonin receptor system, functioning as an agonist for both 5-HT1A and 5-HT1B receptors while antagonizing the 5-HT2C receptor. This compound has demonstrated notable antiaggressive and anxiolytic properties in preclinical studies. Eltoprazine dihydrochloride is utilized in research investigating anxiety disorders, aggression modulation, and the broader implications of serotonin signaling in neuropsychiatric conditions. -
5-HT1A Receptor Agonist/5-HT2A Receptor Antagonist
Flibanserin hydrochloride is a selective agonist of the 5-HT1A receptor and antagonist of the 5-HT2A receptor, exhibiting binding affinities of Ki 1 nM and 49 nM, respectively. Additionally, it interacts with dopamine D4 receptors with a Ki range of 4-24 nM. This compound demonstrates notable antidepressant and anxiolytic effects, making it a valuable tool for researching hypoactive sexual desire disorder (HSDD) and related conditions. -
5-HT6 Receptor Antagonist
Ro 04-6790 is a selective antagonist of the 5-HT6 receptor, exhibiting competitive binding with pKi values of 7.26 and 7.35 for rat and human receptors, respectively. This compound demonstrates a unique specificity, showing no significant affinity for other receptor targets. Ro 04-6790 is valuable for research applications focused on neuropharmacology and the modulation of serotonergic signaling pathways. -
5-HT2A/5-HT2C Receptor Inverse Agonist
5-HT2A/5-HT2C inverse agonist 1 functions as a potent dual inverse agonist at the 5-HT2A and 5-HT2C receptors, demonstrating minimal hERG channel inhibition to mitigate cardiovascular risks. This compound exhibits significant antipsychotic effects in the MK-801-induced mouse model, making it a valuable tool for the investigation of psychotic disorders. It is particularly relevant for studies aiming to elucidate the molecular mechanisms underlying psychosis and for the development of new therapeutic strategies. -
5-HT6 Receptor Agonist
ST1936 oxalate is a selective agonist of the 5-HT6 receptor, demonstrating high nanomolar affinity with a Ki value of 13 nM for the human receptor. It exhibits additional binding affinity for 5-HT7 and 5-HT2B receptors with Ki values of 168 nM and 245 nM, respectively, as well as moderate binding to α2 adrenergic receptors in both human and rat models (Ki of 300 nM). This compound is valuable for research applications focused on serotonergic signaling and its implications in neuropharmacology. -
5-HT Antagonist
ICI 169369 is a competitive antagonist of serotonin receptors, specifically targeting the 5-HT2 and 5-HT1C subtypes. This compound demonstrates Ki values of 1.79 x 10−8 M for 5-HT2 and 1.58 x 10−6 M for 5-HT1C, indicating its specificity and potency. ICI 169369 is utilized in research to investigate the role of serotonin signaling in various physiological and pathological processes, making it a valuable tool in pharmacological studies related to mood disorders and neuropsychiatric research. -
5-HT2A Receptor Antagonist
LY320954 is a selective antagonist of the 5-HT2A receptor, exhibiting a Ki value of 96 nM. This compound effectively diminishes Ca2+ influx in cellular assays, demonstrating an EC50 of 35.5 nM. Additionally, LY320954 has shown significant efficacy in vivo by reducing 5-HT-induced paw swelling in rat models, with an ED50 of 4.8 mg/kg. This makes it a valuable tool for research into psychiatric disorders and the role of serotonergic signaling. -
5-HT Receptor
LY206130 free base is a selective antagonist of the 5-HT1A receptor, which plays a crucial role in serotonin signaling. This compound has demonstrated the ability to enhance the effects of exogenous serotonin levels and may amplify the appetite-suppressing properties of fluoxetine. Research indicates that LY206130 free base significantly reduces the consumption of sweetened milk concentrate in dietary models, suggesting its potential utility in addressing eating disorders and obesity in clinical settings. -
5-HT1A agonist
S-14506 is a potent agonist of the 5-HT1A receptor, demonstrating significant biological activity relevant to neuropharmacology. In addition to its action on 5-HT1A, S-14506 exhibits dopamine antagonist properties by blocking dopamine D2 receptors, which may facilitate its anxiolytic effects. This compound has been shown to inhibit the in vivo binding of [3H]raclopride in both the striatum and olfactory bulbs, supporting its utility in the study of anxiety disorders and related therapeutic applications. -
5-HT1D Receptor Agonist
L-772405 is a selective agonist for the 5-HT1D receptor, demonstrating Ki values of 318 nM and 29 nM against guinea pig 5-HT1B and 5-HT1D receptors, respectively, while exhibiting a Ki value greater than 1000 nM for the rat 5-HT transporter. This compound effectively reduces potassium-induced serotonin (5-HT) release, with an IC50 of 240 nM. L-772405 is valuable in exploring serotonergic signaling and could serve as a useful tool in studies of mood disorders and other neurological research applications. -
5-HT2A Receptor Agonist
5-HT2A receptor agonist-10 is a selective agonist targeting the 5-HT2A receptor, demonstrating an IC50 of 2192.39 nM against both human 5-HT2A and 5-HT1A receptors. This compound is valuable for studying its role in psychosis, mental health disorders, and central nervous system (CNS) research. It serves as a crucial tool for elucidating the pharmacological mechanisms underlying various neuropsychiatric conditions. -
5-HT1A Receptor Modulator
IHCH-7179 is a selective modulator of the 5-HT1A receptor with antagonistic activity at the 5-HT2A receptor. This compound demonstrates potential in influencing serotonergic signaling pathways, making it valuable for studies related to neurological disorders. Its unique mechanism of action positions IHCH-7179 as a significant tool for neuropharmacology research applications. -
5-HT1A Agonist
5-HT1AR agonist 3 is a potent agonist of the 5-HT1A receptor, with an EC50 value of 1.3 nM. This compound primarily activates the 5-HT1A receptors, making it a valuable tool for investigating neuropsychiatric disorders, including anxiety, depression, and sleep disturbances. Its selective receptor modulation supports research aimed at understanding the therapeutic potential of serotonergic pathways in mental health. -
5-HT1E/1F Agonist
BRL 54443 maleate is a potent agonist of the 5-HT1E and 5-HT1F receptors, exhibiting Ki values of 1.1 nM and 0.7 nM, respectively. This compound demonstrates over 30-fold selectivity against other serotonin and dopamine receptors, making it a valuable tool in the study of serotonergic signaling pathways. BRL 54443 maleate is primarily used in research applications focused on anxiety, depression, and other neuropsychiatric disorders where 5-HT receptor modulation is implicated. -
Stable Isotope
Quetiapine-d4-1 fumarate is a deuterated analogue of Quetiapine, specifically designed to enhance analytical precision in research applications. As a serotonin (5-HT) receptor agonist, it exhibits a pEC50 of 4.77 at the human 5-HT1A receptor and acts as a dopamine receptor antagonist with a pIC50 of 6.33 for the human D2 receptor. Quetiapine-d4-1 fumarate demonstrates moderate to high affinity for several key receptors, including D2, 5-HT1A, 5-HT2A, and 5-HT2C, making it suitable for studies in neuropharmacology, particularly in exploring antidepressant and anxiolytic effects. -
5-HT2A Receptor Modulator
CTW0404 is a selective positive allosteric modulator of the 5-HT2A receptor, enhancing its signaling. This compound exhibits significant potential in the research of neuropsychiatric disorders, making it a valuable tool for understanding the role of serotonin receptors in various mental health conditions. Its unique modulation may facilitate the development of novel therapeutic strategies targeting 5-HT2A receptor-related pathways. -
5-HT Receptor Agonist
25H-NBOMe hydrochloride is a potent agonist of the serotonin 5-HT2A receptor, exhibiting Ki values of 1.19 nM for rat receptors and 2.83 nM for human receptors. This compound is valuable for studying serotonergic signaling pathways and their role in neurobiology and psychiatric disorders. Its distinctive receptor interactions make it a useful tool in pharmacological research and the development of novel therapeutic agents. -
5-HT Receptor Antagonist
Elzasonan hydrochloride is a selective antagonist of the 5-hydroxytryptamine 1B and 5-hydroxytryptamine 1D receptors. This compound is primarily utilized in research related to depression, enabling investigations into serotonergic signaling pathways and their implications in mood disorders. Its role as a 5-HT receptor antagonist makes it a valuable tool in pharmacological studies aimed at understanding the therapeutic potential of targeting these receptors. -
5-HT3 Receptor Antagonist
3-AQC is a piperazinylquinoxaline derivative that acts as a competitive antagonist of the 5-HT3 receptor. This compound has demonstrated significant potency in inhibiting serotonin's action at this receptor, making it valuable for research focused on neuropharmacology and the modulation of gastrointestinal function. Its efficacy positions it as a useful tool in studies related to anxiety, depression, and emesis. -
5-HT1A Receptor Agonist
FG-5893 is a selective agonist of the 5-HT1A receptor, known for its anxiolytic properties. By activating the 5-HT1A receptor, FG-5893 facilitates a reduction in anxiety-related behaviors. This compound is particularly relevant for research involving anxiety disorders and the neuropharmacological mechanisms of serotonin modulation. Additionally, FG-5893 acts as an antagonist at the 5-HT2 receptor, potentially providing insights into its multi-faceted role in psychiatric applications. -
5-HT2CR Agonist
5-HT2CR Agonist 2 is a selective agonist targeting the 5-HT2C receptor, demonstrating an EC50 of 36 nM. This compound effectively penetrates the blood-brain barrier and exhibits Gq-biased signaling. It has been shown to attenuate MK801-induced hyperlocomotion and reverse hyperlocomotor activity induced by phencyclidine, making it a valuable tool for research into neuropsychiatric disorders and the modulation of dopaminergic activity. -
CB2R/5-HT1AR Agonist
CB2R/5-HT1AR agonist 1 is a dual agonist targeting the CB2 receptor and the 5-HT1A receptor, displaying partial agonism at the former (EC50=479.6 nM) and full agonism at the latter (EC50=2.7 μM). This compound demonstrates significant anti-anxiety and anti-depressive effects, making it relevant for research in neurological and psychiatric applications. Additionally, it exhibits favorable pharmacokinetic properties, enhancing its potential as a therapeutic candidate. -
5-HT1A/1B/1D Receptor Antagonist
GSK-163090 dihydrochloride is a potent and selective antagonist of the 5-HT1A, 5-HT1B, and 5-HT1D serotonin receptors, exhibiting pKi values of 9.4, 8.5, and 9.7, respectively. Additionally, it inhibits the serotonin reuptake transporter (SerT) with a pKi value of 6.1. This compound demonstrates significant antidepressant and anxiolytic effects, making it a valuable tool for research in neuropharmacology and the investigation of serotonin-related disorders. -
5-HT2 Receptor Antagonist
LY53857 free base is a selective antagonist of the 5-HT2 receptor, exhibiting an ED50 of 17.5 nM. This compound demonstrates notable antiviral activity against influenza A virus, making it a valuable tool for research into viral pathogenesis and therapeutics targeting serotonin receptors. Its ability to modulate serotonin signaling may also provide insights into various neuropsychiatric conditions associated with 5-HT2 receptor dysfunction. -
5-HT2 Antagonist
LY314228 is a selective 5-HT2 antagonist primarily targeting the 5-HT2A receptor, exhibiting an IC50 of 147.9 nM. With Ki values of 65 nM for 5-HT2A, 1214 nM for 5-HT2B, and 168 nM for 5-HT2C, it demonstrates relative selectivity within the serotonin receptor family. This compound effectively inhibits 5-HT-induced paw edema in ovariectomized female rats, with an ED50 of 6.4 mg/kg, and can serve as a valuable tool for research in neuropharmacology and related fields. -
Stable Isotope
Sarpogrelate-d3 hydrochloride is a deuterium-labeled form of Sarpogrelate hydrochloride, serving as a selective antagonist for the 5-HT2 receptor family. With pKis of 8.52, 6.57, and 7.43 for the 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively, it demonstrates notable selectivity over 5-HT1, 5-HT3, 5-HT4, and various adrenergic and histamine receptors. This reagent is valuable for studying vascular diseases related to thrombosis, enabling researchers to investigate the pharmacodynamics and metabolism of Sarpogrelate in biological systems. -
5HT2A Agonist
Luvesilocin, a tryptamine prodrug, is designed to convert into an active form that acts as a 5HT2A agonist in vivo. This compound is primarily used in research investigating mental disorders, providing insights into serotonin receptor modulation and its effects on neuropsychological conditions. Its mechanism of action positions Luvesilocin as a valuable tool for studying the role of the 5HT2A receptor in various biological pathways. -
5-HT2 Antagonist
Sarpogrelate is a specific, orally active antagonist of the 5-HT2 receptor. It has been shown to modulate platelet aggregation and exert hemostatic effects, making it a valuable tool for investigating conditions like Buerger’s disease. Research applications may include studies on platelet function and vascular disorders. -
5-HT1/D2 Agonist
Sarizotan hydrochloride is a potent agonist of the serotonin 5-HT1A receptor and dopamine receptors D2, D3, and D4. It demonstrates high affinity with IC50 values of 0.1 nM for human 5-HT1A, 15.1 nM for rat D2, and 2.4 nM for human D4.2, among others. This compound is primarily utilized in neurological research and pharmacological studies, particularly in the exploration of psychopharmacological interventions and the modulation of serotonergic and dopaminergic pathways. -
Antipsychotic Agent
Mazapertine is an orally active antipsychotic agent primarily targeting dopamine D2, D3, and D4 receptors with high affinity (Ki values < 3 nM). Additionally, it exhibits significant binding to serotonin 5-HT1A receptors (Ki = 1.7 nM) and α1-adrenergic receptors (Ki = 1.3 nM). This compound is valuable for research into neurological diseases, particularly in the context of antipsychotic drug development and neuropharmacology studies. -
5-HT1b Antagonist
SB-216641 is a selective antagonist of the 5-HT1b receptor, known for its ability to modulate serotonergic signaling. This compound exhibits potential to mitigate stress-induced behavioral performance dysregulations, making it of interest in the study of anxiety and depression-related disorders. Its application in research facilitates the understanding of serotonin receptor interactions and their implications in neuropsychiatric conditions. -
5-HT5A Receptor Modulator
UCSF686 is a selective modulator of the 5-HT5A receptor, primarily used to investigate its functional role in serotonergic signaling. This compound exhibits significant affinity for the 5-HT1A, 5-HT2B, and 5-HT7 receptors, ensuring that its effects can be accurately attributed to 5-HT5A modulation. Researchers utilize UCSF686 to control for off-target interactions, making it a valuable tool in studies related to neuropharmacology and receptor biology. -
5-HT7 Receptor Agonist
5-HT7 agonist 2 is a potent agonist of the 5-HT7 receptor, exhibiting an IC50 value of 28.7 nM. This compound is valuable for research into central nervous system (CNS) disorders, facilitating the exploration of serotonergic signaling pathways and their implications in various neuropsychiatric conditions. Its activity at the 5-HT7 receptor may provide insights into therapeutic strategies for targeting mood regulation and cognitive function. -
5-HT2C Receptor Agonist
PF-03246799 monohydrochloride is a potent and selective agonist of the 5-HT2C receptor, exhibiting an EC50 of 190 nM and a Ki of 160 nM. This compound demonstrates a high selectivity for the 5-HT2C receptor compared to the 5-HT2A and 5-HT2B receptors. PF-03246799 monohydrochloride is primarily utilized in research focused on stress urinary incontinence (SUI) and may contribute to further understanding of serotonergic modulation in related conditions. -
5-HT6 Receptor Antagonist
Ro 63-0563 is a potent and selective antagonist of the 5-HT6 receptor, exhibiting competitive inhibition with pKi values of 7.83 and 7.91 for rat and human 5-HT6 receptors, respectively. This compound demonstrates minimal off-target effects, displaying no affinity for other receptors. It is relevant in exploring the role of 5-HT6 in neurological disorders and may be useful in research focused on neuropharmacology and cognitive function. -
5-HT Type 3 Receptor Antagonist
GR65630 acts as a potent and selective antagonist of the 5-hydroxytryptamine (5-HT) type 3 receptor. This compound is valuable for investigating the expression patterns of 5-HT3 receptors across various brain regions and elucidating their roles within the central nervous system. Additionally, GR65630, along with its radiolabeled form [3H]GR65630, can be employed to analyze receptor distribution, density, and binding affinity, facilitating advancements in neuropharmacological research. -
5-HT7R Antagonist
5-HT7R Antagonist 2 specifically targets the 5-HT7 receptor, functioning as a potent antagonist that inhibits G protein and β-arrestin signaling pathways, with a Ki value of 67 nM. This compound exhibits biological activities relevant to neurogenesis and has shown potential in reducing repetitive behaviors associated with autism spectrum disorder (ASD). It is an important tool for research applications focused on neurodevelopmental disorders and signaling pathway modulation. -
5-HT Receptor
Brilaroxazine hydrochloride is a potent modulator of the 5-HT receptor, demonstrating promising therapeutic effects in the management of pulmonary arterial hypertension (PAH). This compound has been shown to mitigate both functional and structural alterations linked to PAH, resulting in marked improvements in pulmonary hemodynamics and right ventricular hypertrophy. Moreover, Brilaroxazine hydrochloride can enhance oxygen saturation levels and reduce elevated pulmonary arterial pressures when administered alongside conventional PAH treatment regimens. -
Antipsychotic Agent
PZ-1190 is a multitarget ligand that primarily interacts with serotonin and dopamine receptors, exhibiting potential antipsychotic activity. This compound has been studied in rodent models to explore its effects on psychotic behaviors. Its unique mechanism of action positions it as a valuable tool for research into psychiatric disorders and the underlying neurotransmitter systems. -
5-HT Receptor Agonist
25P-NBOMe hydrochloride is a potent 5-HT receptor agonist targeting the 5-HT2A and 5-HT2C subtypes. This compound exhibits high binding affinity for these receptors, making it a valuable tool for studying serotonergic systems and their role in various neuropharmacological processes. Research applications include investigations into psychotropic effects and potential therapeutic mechanisms for mood disorders. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole is a potent α2-adrenoceptor antagonist and 5-HT receptor reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is primarily utilized in research related to depression, facilitating studies on the modulation of serotonergic and adrenergic signaling pathways. Its unique pharmacological profile makes it a valuable tool for investigating potential therapeutic approaches in mood disorders. -
5-HT2C Receptor Positive Allosteric Modulator
CYD-1-79 is a selective positive allosteric modulator of the 5-HT2C receptor. This compound enhances 5-HT-induced intracellular calcium release through a distinct allosteric site, demonstrating significant inhibition at dopamine D3 receptors, DAT, and α2A/α2B adrenergic receptors. CYD-1-79 has been shown to modulate spontaneous ambulation in rodents and can synergize with low doses of 5-HT2C receptor agonists. Additionally, it reduces relapse vulnerability in models of psychoactive substance self-administration, highlighting its potential applications in neurological disease research. -
Positive Ago-allosteric Modulator Of 5HT2CR
5-HT2CR Allosteric Modulator 1 is a selective positive ago-allosteric modulator of the 5-HT2C receptor, exhibiting an EC50 of 8 nM. In addition to its modulating properties, it acts as a selective agonist at the 5-HT2C receptor with an EC50 of 25 nM. This compound has been shown to reduce food intake, making it a valuable tool for research into appetite regulation and related neurobiological pathways.
