Catalog No.
Product Name
Application
Product Information
Citations
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5-HT1A Antagonist
Lecozotan hydrochloride is a selective antagonist of the 5-HT1A receptor, exhibiting a Ki of 4.5 nM for the cloned human receptor. This compound enhances the stimulated release of glutamate and acetylcholine in the hippocampus, demonstrating cognitive-enhancing properties. Lecozotan hydrochloride is a valuable tool for research into mild-to-moderate Alzheimer's disease (AD) and other cognitive disorders. -
Dopamine receptor Agonist, 20S proteasome Activator
Apomorphine hydrochloride is a potent dopamine receptor agonist and a known activator of the 20S proteasome. It enhances proteasomal and insulin-degrading enzyme activities, facilitating the degradation of intracellular amyloid-beta (Aβ), phosphorylated tau (p-tau), and p53, thereby reducing their levels in neuronal cells. This compound is particularly relevant for research focused on neurodegenerative disorders such as Alzheimer's disease and psychiatric conditions including schizophrenia. -
5-HT Transporter Inhibitor
LY393558 is a potent, orally active inhibitor of the serotonin transporter (5-HT transporter) and an antagonist of the 5-HT1B and 5-HT1D receptors. This compound significantly increases extracellular serotonin levels in the frontal cortex of mouse models. LY393558 is valuable for research focused on depression and related serotonin modulation studies. -
5-HT4 Receptor Agonist
Usmarapride free base is a selective partial agonist of the 5-HT4 receptor, exhibiting a potent activity with an EC50 of 44 nM. This compound is orally active and can penetrate the blood-brain barrier, making it suitable for investigations into cognitive deficits related to Alzheimer's disease. Its mechanism of action supports research aimed at understanding and potentially mitigating Alzheimer's-associated cognitive impairments. -
MAO-A/5-HT2AR Inhibitor
MAO-A/5-HT2AR-IN-1 is a potent dual inhibitor of monoamine oxidase A (MAO-A) and serotonin receptor 2A (5-HT2AR), exhibiting IC50 values of 0.004 μM and 0.014 μM, respectively. This compound demonstrates significant potential in the field of antidepressant research, contributing to the modulation of serotonin levels and receptor activity. It is a valuable tool for investigating the pharmacological impact of MAO-A and 5-HT2AR inhibition in neuropsychiatric disorders. -
5-HT Receptor Antagonist
SB 206553 hydrochloride is a selective antagonist targeting the 5-HT2B and 5-HT2C receptors. It exhibits high affinity, with a rat 5-HT2B pA2 value of 8.89 and a human 5-HT2C pKi value of 7.92, indicating its effectiveness in modulating serotonin pathways. This compound demonstrates anxiolytic-like properties, making it a valuable tool in research exploring anxiety disorders and related therapeutic interventions. -
5-HT4 Receptor Agonist
BIMU 8 is a highly selective agonist of the 5-HT4 receptor, demonstrating EC50 values of 18 nM for the wild type receptor, 77 nM for the T3.36A mutant, and 540 nM for the W6.48A mutant. This compound facilitates research into serotonin signaling pathways and may have applications in studying gastrointestinal motility and cognitive disorders related to the 5-HT4 receptor. Scientists can leverage BIMU 8's potency and selectivity for detailed pharmacological investigations. -
D1-like Dopamine-Receptor Antagonist
SKF-83566 hydrobromide is a selective antagonist of the D1-like dopamine receptors, exhibiting high blood-brain barrier permeability and oral bioavailability. This compound functions as a competitive inhibitor of the dopamine transporter (DAT), with an IC50 of 5.7 μM, and demonstrates a weaker antagonistic effect on the vascular 5-HT2 receptor (Ki=11 nM). Additionally, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it a valuable tool for studying Parkinson's disease and nicotine dependence. -
5-HT Receptor Agonist
Befiradol hydrochloride is a selective agonist of the 5-HT1A receptor. This compound exhibits significant influence on serotonergic signaling and is used in neuropharmacological research to explore its effects on mood regulation and anxiety-related behaviors. Its application extends to investigations of potential therapeutic interventions for disorders linked to serotonin dysregulation. -
5-HT4 Receptor Antagonist
RS 39604 is a potent and selective antagonist of the 5-HT4 receptor, exhibiting a pKi of 9.1 in guinea pig striatal membranes. It demonstrates minimal affinity for other serotonin receptors, including 5-HT1A, 5-HT2C, and 5-HT3, as well as for various adrenergic, dopaminergic, muscarinic, angiotensin, and opioid receptors. RS 39604's distinctive profile makes it a valuable tool in research focusing on gastrointestinal motility disorders and neuropharmacology. -
5-HT2A Antagonist
4F 4PP oxalate is a selective antagonist of the 5-HT2A receptor, demonstrating a high binding affinity with a Ki value of 5.3 nM. Its specificity is notable, exhibiting significantly lower affinity for the 5-HT2C receptor (Ki = 620 nM). This distinct profile makes 4F 4PP oxalate a valuable tool for research applications in neuropharmacology, particularly in the study of serotonin-related pathways and potential therapeutic interventions for psychiatric disorders. -
5-HT2C Receptor Antagonist
SB 243213 dihydrochloride is a selective and high-affinity antagonist of the 5-HT2C receptor, exhibiting a pKi of 9.37 and a pKb of 9.8 for the human 5-HT2C receptor. This compound displays over 100-fold selectivity for the 5-HT2C receptor relative to various neurotransmitter receptors, enzymes, and ion channels. SB 243213 dihydrochloride is noted for its improved anxiolytic profile and holds potential for therapeutic applications in schizophrenia and motor disorders. -
5-HT1D Agonist
L694247 is a selective agonist of the 5-HT1D receptor, exhibiting high affinity with a pIC50 value of 10.03. It shows lower potency against other serotonin receptors, with pIC50 values of 8.64 for 5-HT1A, 6.42 for 5-HT1C, and 5.66 for 5-HT1E. This compound is valuable for research applications focusing on serotonergic signaling and its implications in neurological disorders. -
5-HT Receptor Agonist
Capeserod is a potent agonist of the serotonin 5-HT4 receptor, exhibiting a Ki of 0.6 nM. It is known to enhance the expression of key proteins such as phosphorylated cAMP-response element binding protein (p-CREB), vascular endothelial growth factor (VEGF), brain-derived neurotrophic factor (BDNF), and B cell lymphoma-2 (Bcl-2) in the hippocampus. Capeserod demonstrates potential antidepressant-like efficacy in Wistar rat models, making it a valuable tool for research in neuropsychiatric disorders and serotonin signaling pathways. -
5-HT Receptor Inhibitor
Mirtazapine-d3 is a deuterated form of Mirtazapine, functioning primarily as a 5-HT receptor inhibitor. This compound exhibits potent noradrenergic and specific serotonergic antidepressant activity by selectively blocking 5-HT2 and 5-HT3 receptors. Mirtazapine-d3 is valuable for pharmacokinetic studies, metabolic profiling, and research into serotonergic modulation in neuropharmacology. -
5-HT4 Agonist/5-HT3 Antagonist
(+-Norcisapride) functions primarily as a 5-HT4 agonist and a 5-HT3 antagonist. This compound exhibits significant biological activity in promoting gastrointestinal motility and has demonstrated effectiveness in animal models of constipation. It is a valuable reagent for research focused on gastrointestinal disorders and the modulation of serotonergic signaling pathways. -
5-HT3/5-HT4 Receptor Antagonist
Fabesetron is an orally active antagonist of both the 5-HT3 and 5-HT4 receptors. It exhibits significant biological activity in mitigating both acute and delayed emesis associated with cancer chemotherapy. This compound is valuable for research applications focusing on antiemetic therapies and the modulation of serotonin receptors in gastrointestinal motility. -
5-HT1A/5-HT1B/5-HT1D Agonist
FPT is a 2-aminotetralin that acts primarily as a partial agonist at the 5-HT1A receptor, and as a full agonist at both 5-HT1B and 5-HT1D receptors, exhibiting EC50 values of 39.3 nM, 1.2 nM, and 0.5 nM, respectively. Additionally, FPT displays weak agonistic activity at the 5-HT7 receptor. This compound demonstrates in vivo efficacy as an antiepileptic agent in Fmr1 knockout mice and produces anxiolytic-like and prosocial behaviors in various mouse models, making it a valuable tool for researching serotonergic modulation and its implications in neurological disorders. -
5-HT2A Receptor Ligand
Iloperidone carboxylic acid is a ligand targeting the 5-HT2A receptor. This metabolite of Iloperidone demonstrates a strong affinity for the 5-HT2A receptor, with a pKi value of 8.15, while also showing moderate binding affinity to adrenergic receptors α1, α2B, and α2C. It serves as a valuable reagent for research exploring neuropharmacology and the modulation of serotonergic signaling in various biological contexts. -
5-HT Receptor Inhibitor
Strictosidinic acid is a glycoside indole monoterpene alkaloid that functions as a 5-HT receptor inhibitor. It acts by inhibiting precursor enzymes involved in the biosynthesis of serotonin (5-HT), subsequently reducing overall serotonin levels. This compound demonstrates significant peripheral analgesic and antipyretic effects in murine models, making it a valuable tool for researchers studying pain mechanisms and serotonin modulation. -
5-HT1A Receptor Agonist
EMD 56551 is a potent and selective agonist of the 5-HT1A receptor, exhibiting significant anxiolytic properties. This compound is widely used in research to investigate its potential therapeutic effects on anxiety disorders and related neurological conditions. Its selective action on the 5-HT1A receptor makes it a valuable tool for studying serotonin signaling pathways and their impact on mood regulation. -
5-HT2A Antagonist
4,4-Diphenylbutylamine hydrochloride is a potent antagonist of the 5-HT2A receptor, exhibiting a binding affinity with a Ki value of 2589 nM. Additionally, it also interacts with the H1 receptor, with a Ki of 1670 nM. This compound is primarily used in research focused on serotonin receptor modulation and the study of related neuropharmacological effects. -
5-HT4 Receptor Agonist
Felcisetrag is a potent and selective agonist of the 5-HT4 receptor, exhibiting significant gastrointestinal prokinetic activity. With a high affinity for human 5-HT4(c) receptors (pKi = 9.4), Felcisetrag is utilized in research focused on gastrointestinal motility disorders and related pathophysiological conditions. Its oral bioavailability and selectivity make it a valuable tool for exploring therapeutic strategies in digestive health. -
5-HT Receptor Antagonist
(-)-Eseroline fumarate is a potent 5-HT receptor antagonist that effectively disrupts cellular activities in various biological systems. It is known to induce cell death by promoting the release of adenine nucleotides and 5-hydroxytryptamine (5-HT) from neuronal cells, alongside eliciting lactic acid dehydrogenase (LDH) leakage from cancer cells. Additionally, (-)-Eseroline fumarate inhibits electrically evoked contractions in the mouse vas deferens and guinea pig ileum, making it a valuable tool for investigating neuropharmacological effects and potential therapeutic applications in cancer research. -
5-HT6 Antagonist
PRX-07034 hydrochloride is a selective and potent antagonist of the 5-HT6 receptor, exhibiting a Ki range of 4-8 nM and an IC50 of 19 nM. This compound is utilized in research to investigate its potential effects on enhancing working memory and cognitive flexibility, making it a valuable tool for studying cognitive functions and neuropharmacology. -
5-HT1A Receptor Agonist
4-Methylamphetamine hydrochloride is a selective agonist of the 5-HT1A receptor, known for inducing hypothermia in rodent models. It enhances the extracellular concentrations of norepinephrine, dopamine, and serotonin by interacting with their respective transporters. This compound is valuable in researching neurological disorders and understanding serotonergic and dopaminergic system dynamics. -
5-HT1A agonist
S-14506 hydrochloride is a potent agonist of the 5-HT1A receptor and acts as an antagonist at the 5-HT2A and 5-HT2C receptors. This compound also demonstrates dopamine antagonist activity through the inhibition of D2 receptors. S-14506 hydrochloride has been shown to inhibit the in vivo binding of [3H]raclopride in the striatum and olfactory bulbs. This reagent is valuable for research into anxiolytic agents and the modulation of serotonin and dopamine systems. -
5-HT1B Receptor Antagonist
GR 55562 dihydrochloride is a selective antagonist of the 5-HT1B receptor. It is primarily utilized in research exploring serotonergic pathways and their role in various neurological disorders. This compound may provide insights into the mechanisms underlying nerve-related diseases and potential therapeutic targets. -
5-HT2C Agonist
(-)-5-HT2C agonist-3 is a selective agonist for the 5-HT2C receptor, preferentially activating Gq signaling pathways. It exhibits EC50 values of 103 nM for 5-HT2C, 570 nM for 5-HT2B, and 72 nM for 5-HT2A, indicating its specificity towards the 5-HT2C receptor. This compound is valuable for research applications in the field of antipsychotic drug development and the study of serotonergic system modulation. -
5-HT2C Receptor Antagonist
SB 243213 hydrochloride is a selective antagonist of the 5-HT2C receptor with high affinity, exhibiting a pKi of 9.37 and a pKb of 9.8 for the human receptor. This compound demonstrates over 100-fold selectivity for the 5-HT2C receptor compared to various neurotransmitter receptors, enzymes, and ion channels. Its anxiolytic properties indicate potential applications in research related to schizophrenia and motor disorders. -
5-HT2 Receptor Antagonist
(S)-Volinanserin is a selective antagonist of the 5-HT2 receptor, exhibiting a high affinity with a Ki of 0.36 nM. This compound demonstrates a remarkable 300-fold selectivity for the 5-HT2 receptor compared to 5-HT1c, alpha-1, and dopamine D2 receptors. Due to its potent antipsychotic properties, (S)-Volinanserin is a valuable tool for research into psychiatric disorders and related pharmacological studies. -
5-HT2C Antagonist
Mesulergine hydrochloride is a potent antagonist of the 5-HT2C receptor. This compound has been shown to induce hyperphagia, making it relevant for studies investigating appetite regulation. Additionally, Mesulergine hydrochloride may play a role in the exploration of cognitive processes and related neurobiological mechanisms. -
5-HT6R Agonist
EMD386088 is a highly potent and selective agonist of the 5-HT6 receptor (5-HT6R) with an EC50 of 1.0 nM. This compound exhibits minimal activity against other serotonin receptors, displaying an IC50 of 34 nM primarily at the 5-HT3R. EMD386088 is known to modulate ERK1/2 activity, indicating its potential role in signaling pathways. This reagent is relevant for research applications related to Alzheimer's disease and schizophrenia, providing insight into neuropsychiatric disorders and their treatment. -
5-HT Receptor Agonist
25C-NBOH hydrochloride is a potent agonist targeting 5-HT receptors, specifically exhibiting a strong preference for the 5-HT2A receptor over the 5-HT2C receptor, with EC50 values of approximately 0.40 nM and 15 nM, respectively. This compound is a derivative of 2C-C featuring an N-(2-hydroxybenzyl) substitution at the amine position. 25C-NBOH hydrochloride plays a significant role in neuropharmacological research, facilitating the investigation of serotonin signaling pathways and their implications in various neurological disorders. -
Sigma/5-HT1A Receptor Agonist
OPC-14523 free base is a potent sigma and 5-HT1A receptor agonist. With a high affinity for sigma receptors (σ1/2 IC50=47/56 nM) and the 5-HT1A receptor (IC50=2.3 nM), along with activity at the 5-HT transporter (IC50=80 nM), it exhibits significant antidepressant-like effects. This compound is valuable for research applications investigating mood disorders and serotonergic signaling pathways. -
5-HT2C Receptor Agonist
Org-12962 is a selective agonist of the 5-HT2C receptor, demonstrating a pEC50 value of 7.01. In addition to its primary target, Org-12962 shows significant efficacy for the 5-HT2A and 5-HT2B receptors with pEC50 values of 6.38 and 6.28, respectively. This compound is notable for its anti-aversive effects observed in rat models of panic-like anxiety, making it a valuable tool for investigating anxiety disorders and related neuropharmacology. -
5-HT1A Receptor Agonist
Repinotan is a potent and selective agonist of the 5-HT1A receptor, exhibiting strong brain penetration and oral bioavailability. With Ki values of 0.19 nM in the calf hippocampus, 0.25 nM in rat and human cortex, and 0.59 nM in rat hippocampus, it displays high affinity for target sites while maintaining weak interaction with other related receptors. Repinotan is recognized for its significant neuroprotective properties, making it valuable for research in neuroscience and related therapeutic applications. -
5-HT3 Receptor Antagonist
(R)-Mirtazapine is a selective 5-HT3 receptor antagonist known for its antinociceptive properties demonstrated in animal models of acute thermal nociception. This R( )-enantiomer of Mirtazapine contributes to various neurological studies, particularly in the context of pain modulation and serotonin pathway interactions. (R)-Mirtazapine undergoes metabolism primarily by the enzyme CYP3A4, making it a relevant compound for pharmacokinetic studies in drug metabolism. -
5-HT4 Agonist
ML 10302 is a potent 5-HT4 receptor agonist with a Ki value of 1.07 nM. This compound enhances gut motility by stimulating cholinergic pathways, leading to significant prokinesia in both the small intestine and colon. Additionally, ML 10302 holds potential for research applications in neurological diseases, providing insights into therapeutic mechanisms targeting the gastrointestinal and nervous systems. -
5-HT Agonist
PNU-22394 hydrochloride is a potent agonist for the 5-hydroxytryptamine (5-HT) receptors, specifically engaging the 5-HT2C and 5-HT2A receptor subtypes with Ki values of 6.1 nM and 10 nM, respectively. This compound is valuable for studying the roles of 5-HT in neurobiology and its implications in various psychiatric disorders. Its selective action on serotonin receptors makes it a useful tool for investigating serotonin signaling pathways and potential therapeutic interventions. -
5HT3A Receptor Antagonist Ligand
GR119566X is a high-affinity antagonist of the 5HT3A receptor, effectively inhibiting receptor activity. This compound is suitable for use in affinity purification experiments involving 5-HT3 receptors, providing a valuable tool for investigating receptor function and pharmacology. Its specificity for the 5HT3A receptor makes it useful for diverse applications in neurobiology and drug discovery research. -
5-HT2 Receptor Antagonist
Fananserin is a potent and selective antagonist of the 5-hydroxytryptamine 2 (5-HT2) receptor, exhibiting a Ki value of 0.37 nM for the rat 5-HT2A receptor. Additionally, Fananserin serves as a selective antagonist for the dopamine D4 receptor, with a Ki of 2.93 nM for the human variant. This compound is valuable for research exploring the modulation of serotonin and dopamine pathways, offering insights into potential therapeutic applications in neuropsychiatric disorders. -
5-HT Receptor Antagonist
5-HT2A antagonist 1 is a selective antagonist of the 5-HT2A receptor, playing a crucial role in modulating serotonin signaling. This compound demonstrates potential in alleviating gastrointestinal disorders and may also have applications in addressing circulatory system irregularities. Its pharmacological profile makes it a valuable tool for research in serotonergic pathways and their implications in various biological systems. -
5-HT4 Receptor Partial Agonist
CJ033466 is a selective partial agonist of the 5-HT4 receptor, exhibiting an EC50 of 9 nM. This compound demonstrates significant gastroprokinetic effects, making it a valuable tool for research applications related to gastrointestinal motility and related disorders. Its specificity towards the 5-HT4 receptor aids in elucidating receptor-mediated pathways and potential therapeutic interventions. -
α2-adrenoceptor Antagonist/5-HT Receptor re-uptake Inhibitor
Napamezole (hydrochloride) functions as an α2-adrenoceptor antagonist and a serotonin (5-HT) reuptake inhibitor, exhibiting Ki values of 28 nM and 93 nM for rat α2 and α1 adrenergic receptors, respectively. This compound is particularly relevant for research into depression and related neuropsychiatric disorders, facilitating studies on serotonin modulation and adrenergic signaling pathways. Its dual action can provide insights into the mechanisms underlying mood regulation and therapeutic interventions. -
5-HT1A Agonist
R(+)-8-OH-DPAT hydrobromide is a selective agonist of the 5-HT1A receptor, known for its significant efficacy in modulating serotonergic signaling. This compound enhances dopamine release in the medial prefrontal cortex, thereby providing valuable insights into the relationship between serotonin and dopamine neurotransmission. R(+)-8-OH-DPAT is widely utilized in research focused on neuropharmacology and behavioral studies related to mood disorders and cognition. -
5-HT Receptor
(R,R)-Palonosetron Hydrochloride is a selective antagonist of the 5-HT3 receptor. This compound exhibits significant antiemetic properties, making it valuable in the prevention of chemotherapy-induced nausea and vomiting. Its high affinity for the 5-HT3 receptor can also facilitate research on serotonin signaling pathways and their role in gastrointestinal function and neurological disorders. -
5-HT Receptor Agonist
Revexepride is a selective agonist of the 5-HT4 receptor, exerting effects on gastrointestinal motility and potentially influencing CYP3A4 enzyme induction. Its primary biological activity includes the enhancement of gastrointestinal function, making it a candidate for research in digestive disorders such as gastroesophageal reflux disease. This compound is relevant for studies investigating serotonergic modulation in gastrointestinal diseases and the metabolic implications associated with CYP3A4 activity. -
5-HT2C Receptor Agonist
Ro60-0175 fumarate acts as a potent and selective agonist of the 5-HT2C receptor, which is involved in various neurophysiological processes. This compound has demonstrated significant activity in modulating serotonin signaling pathways, making it a valuable tool for research into mood regulation, anxiety, and appetite control. It is suitable for studies focused on the pathophysiology of psychiatric disorders and the development of novel therapeutic strategies. -
D3R/5-HT2AR Antagonist/5-HT1AR Agonist
D3/5-HT receptor modulator-1 is a selective antagonist for dopamine D3 receptors and 5-HT2A receptors, while also functioning as a partial agonist at 5-HT1A receptors. With measured Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the respective targets, this compound exhibits a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. Its unique pharmacological profile suggests potential applications in the development of atypical antipsychotic therapies and for studying dopaminergic and serotonergic signaling pathways.
