Catalog No.
Product Name
Application
Product Information
Citations
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5-HT1A Receptor Antagonist
S14063 is a potent antagonist of the 5-HT1A receptor. It selectively inhibits this receptor without exhibiting β-adrenoceptor blocking properties. S14063 is utilized in research applications focusing on serotonergic signaling and its implications in neuropharmacology. -
5-HT6R Agonist
EMD 386088 free base is a potent agonist of the serotonin 6 receptor (5-HT6R). It has been shown to induce cell death and modulate ERK1/2 activity, making it a valuable tool in the study of neurodegenerative disorders. This reagent is particularly relevant for research applications related to Alzheimer's disease and schizophrenia, where 5-HT6R signaling plays a significant role. -
5-HT2A Receptor Agonist
5-HT2A receptor agonist-5 is a potent agonist that targets the 5-HT2A receptor, exhibiting a Ki value of 0.017 µM. It has been shown to demonstrate antidepressant activity, making it a valuable tool for research into mood disorders and the mechanisms of serotonergic signaling. This compound may be beneficial in studies aimed at understanding the therapeutic potential of 5-HT2A receptor modulation. -
Stable Isotope
Deulumateperone is a deuterated derivative of Lumateperone, serving as a stable isotope for research applications. Lumateperone acts as a selective antagonist of the 5-HT2A receptor (Ki = 0.54 nM) and modulates dopamine receptors, demonstrating significant antipsychotic and antineoplastic properties. This reagent is valuable for studies involving receptor interactions, pharmacokinetics, and metabolic profiling in various biological systems. -
5-HT6 Receptor Antagonist
SB357134 is a potent and selective antagonist of the 5-HT6 receptor, demonstrating significant brain penetration and oral bioavailability. This compound has been shown to enhance memory and learning capabilities while increasing seizure thresholds in rodent models. It is valuable for research applications focused on neuropharmacology, cognitive function, and the modulation of serotonergic signaling pathways. -
Light-Activated Caged 5-HT
BHQ-O-5HT is a light-activated caged form of serotonin (5-HT), utilizing a BHQ group for protection. Upon irradiation with light at wavelengths of either 365 or 740 nm, BHQ-O-5HT undergoes photolytic cleavage, releasing 5-HT via one or two-photon excitation. This reagent is valuable for time- and spatially-resolved studies, enabling researchers to investigate the multifaceted roles of 5-HT in mood regulation, appetite control, memory processes, learning, and other cognitive functions. -
5-HT Receptor Antagonist
Elzasonan is a selective antagonist of the 5-hydroxytryptamine 1B (5-HT1B) receptor. This compound exhibits significant biological activity by inhibiting 5-HT1B receptor signaling, which plays a crucial role in the regulation of mood and anxiety. Elzasonan is primarily utilized in research focused on the pathophysiology of depression and the development of novel antidepressant therapies. -
5-HT Receptor
(R)-RS 56812 hydrochloride is a selective antagonist of the 5-HT3 receptor, demonstrating significant effects on cognitive function. Research shows that the (R) isomer provides more consistent enhancements in performance on delayed matching tasks in primates compared to its (S) counterpart. This compound presents potential therapeutic applications in conditions associated with cognitive decline. -
5-HT7 Receptor Ligand
PZ-1129 is a selective ligand for the 5-HT7 receptor, exhibiting a Ki of 7 nM, with moderate affinity for 5-HT1A and D2 receptors (Ki values of 159 nM and 24 nM, respectively). This compound effectively inhibits constitutive cAMP production via the Gs signaling pathway, with an EC50 of 13.7 nM. PZ-1129 is suitable for research into emotional disorders, including depression and bipolar disorder, providing a valuable tool for understanding the underlying mechanisms of these conditions. -
5-HT1A Receptor Antagonist
UH 301 hydrochloride is a selective antagonist of the 5-HT1A receptor. This compound has been shown to modulate the consolidation of learning processes in both normal and cognitively impaired rodent models. UH 301 hydrochloride is primarily utilized in research applications focused on Alzheimer's disease and various forms of amnesia, providing insights into therapeutic interventions for cognitive enhancement. -
Dopamine/5-HT Receptor Inhibitor
Loxapine hydrochloride is an orally active inhibitor of dopamine receptors and an antagonist of 5-HT receptors. This dibenzoxazepine compound exhibits significant antipsychotic properties, making it valuable for research into psychotropic effects and therapeutic interventions for schizophrenia and other psychiatric disorders. Its dual receptor activity contributes to its efficacy in modulating dopaminergic and serotonergic pathways. -
5-HT1A Receptor Partial Agonist
Adatanserin hydrochloride is a selective partial agonist of the 5-HT1A receptor, exhibiting high affinity with a Ki value of 1 nM. Additionally, it acts as a moderate affinity antagonist at the 5-HT2 receptor with a Ki of 73 nM. This compound demonstrates significant anxiolytic and antidepressant effects, making it valuable for research into anxiety and depression models. -
5-HT Receptor Antagonist
Alverine hydrochloride is a potent antagonist of the 5-HT1A receptor, exhibiting an IC50 value of 101 nM. This compound is primarily utilized in gastrointestinal research to investigate its effects on smooth muscle contraction and motility. Its role in modulating serotonin signaling makes it valuable for studies related to gastrointestinal disorders and therapeutic interventions targeting 5-HT receptors. -
5-HT Receptor Agonist
Flesinoxan hydrochloride is a selective agonist for the 5-hydroxytryptamine 1A (5-HT1A) receptor, exhibiting high affinity with an EC50 value of 24 nM. It demonstrates significant anxiolytic and antidepressant properties, contributing to its potential as a therapeutic agent in mood and anxiety disorders. This compound is valuable for research focused on neuropharmacology and the modulation of serotonergic pathways. -
5-HT1 Receptor Antagonist
SB-272183 is a selective antagonist of the 5-HT1A, 5-HT1B, and 5-HT1D receptors, demonstrating high binding affinity with pKi values of 8.0, 8.1, and 8.7, respectively, in both human recombinant and native tissues. Its primary mechanism targets serotonin receptors, making it a valuable tool for studying the role of serotonin signaling in various biological processes. SB-272183 is particularly relevant in antidepressant research, aiding in the exploration of potential therapeutic pathways for mood disorders. -
5-HT3 Receptor Partial Agonist
RS-56812 is a partial agonist of the 5-HT3 receptor, known to significantly enhance colonic propulsive peristalsis. By indirectly promoting cholinergic neurotransmission, RS-56812 has also been shown to improve working memory performance in non-human primates. This compound is utilized in research investigating diarrheal disorders, colon motility, and cognitive impairments, including Alzheimer's disease. -
5-HT2A Agonist
25N-N1-Nap is a β-arrestin-biased agonist of the 5-HT2A receptor. It has demonstrated the ability to antagonize phencyclidine-induced hyperactivity in male C57BL/6 J mice, indicating its potential use in research on psychostimulant behaviors. This compound is valuable for studies investigating serotonin receptor signaling and its implications in neuropsychiatric disorders. -
5-HT2 Antagonist
Methiothepin maleate is a potent and non-selective antagonist of the 5-HT2 receptor family, demonstrating affinity with pKis of 8.50 for 5-HT2A, 8.68 for 5-HT2B, and 8.35 for 5-HT2C. This compound effectively inhibits various serotonin receptor subtypes, including 5-HT1A through 5-HT7, making it a valuable tool for studying serotonin signaling pathways. Methiothepin maleate is commonly used in neuropharmacology research to investigate the role of serotonin in mood regulation, psychosis, and related disorders. -
5-HT1A Receptor Agonist
SSR-181507 hydrochloride is a selective 5-HT1A receptor agonist with additional activity as a dopamine D2 receptor antagonist. It has demonstrated the ability to inhibit Apomorphine-induced climbing behavior in mice and reduce stereotypic behaviors in rats. This compound is employed in research focused on understanding and treating conditions such as depression and anxiety. -
5-HT Receptor Antagonist
Alprenolol benzoate serves as a non-selective β-adrenoceptor antagonist with an additional mechanism as a 5-HT1A and 5-HT1B receptor antagonist. This compound exhibits significant biological activity in reducing blood pressure, alleviating angina, and managing arrhythmias. It is essential for research focused on cardiovascular conditions and the modulation of serotonin receptors in various physiological and pathological contexts. -
5-HT1A Receptor Modulator
Galanin (1-15) (porcine, rat) is a peptide fragment consisting of the N-terminal 15 amino acids of the neuropeptide galanin, primarily acting as a modulator of the 5-HT1A receptor. This compound has been shown to interact with the 5-HT1A receptors in the dorsal hippocampus of the rat brain, effectively reducing their affinity and influencing serotonin neuronal networks. Galanin (1-15) is valuable for research applications related to neurobiology, particularly in studies investigating serotonin modulation and its effects on mood and anxiety disorders. -
5-HT2 Receptor Antagonist
DOAM is a selective antagonist of the 5-HT2 receptor, modulating serotonergic signaling pathways. This compound is primarily utilized in research focused on neuropharmacology and psychiatric disorders, providing insights into the effects of serotonin in various biological systems. Its inhibition of 5-HT2 receptor activity makes it a valuable tool for studying the mechanisms underlying mood regulation and related pharmacological interventions. -
5-HT1A Receptor Antagonist
S-14489 is a selective antagonist of the postsynaptic 5-HT1A receptor, exhibiting a high affinity with a pKi of 9.2. This compound can function as an agonist at 5-HT1A autoreceptors and effectively inhibit the accumulation of 5-hydroxytryptophan in the striatum. S-14489 is primarily employed in neurological research, particularly for studying disorders related to serotonin signaling. -
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.
