Catalog No.
Product Name
Application
Product Information
Citations
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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. -
5-HT2A Receptor Agonist
5-HT2A receptor agonist-8 is a highly effective agonist of the 5-HT2A receptor, exhibiting an EC50 of 0.6784 nM. This compound is valuable for investigating the neuropharmacological mechanisms underlying depressive disorders and bipolar disorders. Its potency makes it a significant tool for research in psychiatric and neurological studies focused on serotonin signaling pathways. -
5-HT2A/D4 Antagonist
Pipamperone dihydrochloride is a potent antagonist of the 5-HT2A (pKi=8.2) and D4 (pKi=8.0) receptors, derived from the butyrophenone class. It exhibits low-affinity antagonism at the D2 receptor (pKi=6.7) and is known to influence neurotransmitter systems, contributing to its antipsychotic effects. This compound is utilized in research focused on mental health disorders, including autism-related behavioral conditions and Alzheimer's disease. -
MT1/2 Agonist and 5-HT2C Antagonist
7-Desmethyl-3-hydroxyagomelatine is an MT1/2 agonist and a 5-HT2C antagonist. As a metabolite of Agomelatine, it demonstrates reduced biological activity compared to its parent compound. This reagent can be utilized in research focusing on circadian rhythms, mood regulation, and the interaction of melatonergic and serotonergic pathways in neuropharmacology. Its unique profile makes it a valuable tool for studying various neuropsychiatric disorders. -
5-HT2B Antagonist
VU0530244 is a highly potent antagonist of the serotonin 5-HT2B receptor, exhibiting an IC50 of 17.3 nM. Due to its predicted properties, VU0530244 is expected to have minimal brain penetration in human subjects and is likely a substrate for P-glycoprotein-mediated efflux. This compound is useful for research applications focused on serotonin receptor signaling and its implications in various physiological and pathological processes. -
5-HT Receptor
Renzapride hydrochloride is a benzamide derivative primarily targeting 5-HT receptors. It exhibits antagonistic activity at 5-HT(3) receptors and agonistic activity at 5-HT(4) receptors, which contributes to its efficacy in treating irritable bowel syndrome. Additionally, Renzapride hydrochloride shows antagonistic properties at 5-HT(2B) receptors and demonstrates significant affinity for 5-HT(2A) and 5-HT(2C) receptors, making it a valuable tool in gastrointestinal research and the study of serotonin receptor mechanisms. -
Stable Isotope
Arotinolol-d5 hydrochloride is a deuterated analog of Arotinolol, a nonselective α/β-adrenergic receptor blocker with vasodilatory properties. This compound exhibits notable activity in inhibiting the binding of the radioligand 125I-ICYP to 5HT1B serotonergic receptor sites. Arotinolol serves as an effective antihypertensive agent and is utilized in research related to various cardiovascular and non-cardiovascular diseases. -
5-HT2 Antagonist
AT1015 hydrochloride is a potent antagonist of the 5-HT2 receptor, exhibiting a pKi value of 7.94. This compound has been shown to inhibit vasoconstriction and effectively block platelet aggregation, making it a valuable research tool for studies related to cardiovascular and hemostatic functions. Its properties render it suitable for investigating the physiological and pathological roles of serotonin signaling in various biological systems. -
5-HT6 Agonist
WAY-181187 oxalate is a selective full agonist of the 5-HT6 receptor, exhibiting a binding affinity with a Ki of 2.2 nM and an effective concentration for half-maximal activation (EC50) of 6.6 nM. This compound engages 5-HT6 receptor-mediated signaling pathways, influencing cAMP, Fyn, and ERK1/2 kinase activity. It serves as a valuable tool for research into neuropharmacology and potential therapeutic applications targeting cognitive disorders. -
TAAR1/5-HT1A Agonist
SEP-363856 mesylate is a selective agonist for the trace amine-associated receptor 1 (TAAR1) and the 5-HT1A receptor, exhibiting unique psychotropic effects through a non-dopaminergic mechanism of action. This compound demonstrates antipsychotic-like activity, making it a valuable tool for investigating the pathophysiology and treatment of schizophrenia. Its distinct mechanism provides a novel approach to research in mental health disorders, particularly in areas where traditional therapies may be ineffective. -
5-HT Receptor Antagonist
Xylamidine is a peripheral 5-HT receptor antagonist that serves as a valuable tool for studying the appetite suppressant effects associated with 5-hydroxytryptophan (5-HTP) and fenfluramine. Experimental results indicate that xylamidine attenuates the decrease in food intake caused by 5-HT and 5-HTP, while showing no significant effect on fenfluramine. This suggests that the appetite-suppressing properties of 5-HTP may be mediated partially through peripheral 5-HT receptors. Additionally, xylamidine has been shown to reverse the impact of 5-HTP on food intake rate, highlighting its role in dissecting the underlying mechanisms of peripheral appetite regulation. -
5-HT2C Receptor Agonist
Org37684 is a potent agonist of the 5-HT2C receptor, displaying a pEC50 value of 8.17. It demonstrates a preferential selectivity, being approximately 2.5 times more potent at the 5-HT2C receptor compared to the 5-HT2B receptor (pEC50=7.96) and ten times more potent than the 5-HT2A receptor (pEC50=7.11). This compound is utilized in research applications focused on the regulation of mood, appetite, and other neuropharmacological processes mediated by serotonin receptors. -
5-HT1AR Agonist/α1-Adrenergic Receptor Antagonist
Enciprazine dihydrochloride is an orally active non-benzodiazepine anxiolytic that functions as a 5-HT1A receptor agonist and α1-adrenergic receptor antagonist. This compound demonstrates key biological activity by inducing electroencephalogram changes, characterized by a reduction in δ and θ wave power and an increase in α and fast β wave power. Enciprazine dihydrochloride exhibits anti-aggressive properties, alongside minimal sedative and ataxic effects. It also modulates plasma corticosterone levels and activates the hypothalamic-pituitary-adrenal axis, making it a valuable reagent for research into anxiety disorders, generalized anxiety syndrome, and psychosis. -
5-HT Receptor
Gevotroline is a potent antagonist of the 5-HT receptor. It demonstrates significant affinity for this target, making it a valuable tool in researching psychotomimetic effects. This compound is particularly useful in studies exploring the modulation of serotonin-related pathways and their impact on neurological functions. -
5-HT Receptor Antagonist
Alosetron-d3 is a deuterium-labeled derivative of Alosetron, which acts as a serotonin 5-HT3 receptor antagonist. This compound plays a critical role in the study of gastrointestinal disorders, particularly in research focused on irritable bowel syndrome (IBS). Its unique isotopic labeling allows for advanced utilization in pharmacokinetic and metabolic studies, enhancing the understanding of drug behavior in biological systems. -
5-HT Receptor Agonist
Lesopitron (E-4424) is a potent agonist of the 5-HT receptor, exhibiting significant anxiolytic-like effects. It inhibits forskolin-stimulated adenylate cyclase activity with an IC50 value of 125 nM, making it a valuable tool for research in neuropharmacology and anxiety disorders. This compound is suitable for studies investigating serotonin signaling pathways and their impact on mood regulation. -
5-HT3 Receptor Antagonist
(S)-Ramosetron is an orally active antagonist of the 5-hydroxytryptamine 5-HT3 receptor. It exhibits significant antiemetic properties, making it valuable for research into conditions associated with nausea and vomiting, as well as irritable bowel syndrome (IBS). Its antagonistic action allows for investigations into the modulation of gastrointestinal motility and neurochemical signaling pathways involved in these disorders. -
5-HT1A Receptor Inhibitor
LY 178210 is a selective partial agonist of the 5-HT1A receptor, exhibiting Ki values of 0.67 nM for 5-HT1A and 380 nM for 5-HT1D receptors, thereby demonstrating its specificity. Its minimal activity against α₂-adrenergic receptors, 5-HT₂, and other neurotransmitter receptors makes it a valuable tool in neuropharmacology. Additionally, LY 178210 effectively inhibits forskolin-stimulated cyclase activity, though with lower potency compared to full agonists like 8-OH-DPAT. This compound is significant for studies on serotonergic modulation, as it markedly reduces 5-hydroxyindoleacetic acid (5-HIAA) levels in the hypothalamus while increasing serum corticosterone concentrations. -
5-HT2A Antagonist
AT-1015 is a selective, orally active antagonist of the 5-HT2A serotonin receptor. It demonstrates significant antithrombotic properties by prolonging arterial occlusion time in thrombus formation. Additionally, AT-1015 inhibits platelet aggregation and vasoconstriction, making it a valuable compound for research in cardiovascular and hematological applications. -
5-HT4 Receptor Ligand
R 116712 is a selective ligand for the 5-HT4 receptor, demonstrating high affinity and specificity. This compound plays a key role in research applications related to neuropharmacology and gastrointestinal motility. Additionally, R 116712 can be utilized in the development of isotopic markers to further enhance studies in receptor pharmacology and signaling pathways. -
Dopamine Receptor Antagonist
Zicronapine fumarate is a potent dopamine receptor antagonist primarily targeting D1 and D2 receptors, as well as serotonin 5-HT2A receptors. It exhibits significant pro-cognitive effects in preclinical models, positioning it as a promising candidate for the treatment of various neurological and psychiatric disorders. Research applications include the exploration of its therapeutic potential in conditions such as schizophrenia and mood disorders. -
5-HT1A Receptor Agonist
Org 13011 is a selective 5-HT1A receptor agonist that acts on the central nervous system. It has been shown to induce conditioned taste aversion, making it a valuable tool for studying the mechanisms underlying learning and memory processes. This compound is relevant for research focused on anxiety, depression, and other neuropsychiatric disorders. -
5-HT Receptor Modulator
ML10375 is a modulator of the 5-HT4 and 5-HT2 serotonin receptors, impacting gap junction coupling in rat atrial myocytes. It plays a significant role in the regulation of intracellular cAMP levels and influences L-type calcium currents. This compound is useful for investigating serotonergic pathways and their effects on cardiac physiology. -
5-HT4 receptor Antagoinst
GR125487 is a highly selective antagonist of the 5-HT4 receptor, exhibiting a Kd value of 0.1 nM. It demonstrates minimal binding affinity for 5-HT3 receptors (Kd > 1 μM), ensuring specificity in its action. GR125487 effectively inhibits the memory-enhancing effects of BIMU1 without significantly affecting baseline social memory. This compound is valuable for investigating mechanisms underlying social olfactory memory and related cognitive processes. -
5-HT Receptor Agonist
(RS)-Minesapride is a selective agonist of the 5-HT receptor, primarily targeting the serotonin pathways involved in gastrointestinal motility. This compound demonstrates potential therapeutic efficacy in treating irritable bowel syndrome with predominant constipation (IBS-C). Its pharmacological profile makes it a valuable tool for research into gastrointestinal disorders and the modulation of serotonin receptor activity. -
5-HT1A Receptor Agonist
AP-521 free base is a benzothienopyridine derivative that functions as a potent agonist of the 5-HT1A receptor. Its primary mechanism involves enhancing serotonergic transmission, leading to significant anxiolytic effects in the medial prefrontal cortex (mPFC). This compound holds promise for research applications focused on anxiety disorders and related neurobiological mechanisms. -
5-HT1A Receptor Agonist
LY-228729 is a selective agonist of the 5-HT1A receptor, known for its significant effects on behavior. This compound has been shown to decrease rearing frequency and overall activity in rats during open field tests, as well as reduce immobility and enhance swimming time in forced swim tests. LY-228729 serves as a valuable tool in the investigation of neurological disorders and the modulation of serotonin-related pathways. -
5-HT2A Receptor Inhibitor
Belaperidone is a selective 5-HT2A receptor inhibitor, demonstrating significant antidopaminergic and antiserotonergic properties. This compound is primarily employed in research related to neuropsychiatric disorders and may provide insight into therapeutic strategies for conditions such as schizophrenia and depression. Its mechanism of action makes Belaperidone a valuable tool in studying serotonin and dopamine receptor interactions within the central nervous system.
