Catalog No.
Product Name
Application
Product Information
Citations
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5-HT Receptor Agonist
Anpirtoline hydrochloride is a selective agonist of the 5-HT1B receptor, exhibiting binding affinities of 28 nM for 5-HT1B, 150 nM for 5-HT1A, and 1.49 μM for 5-HT2 receptors. This compound demonstrates serotonergic activity and displays antinociceptive and antidepressant-like effects. It is valuable for research in neuropharmacology, particularly in studying the role of serotonin receptors in pain modulation and mood disorders. -
5-HT2C Receptor Antagonist
3-Hydroxy agomelatine-d3 is a deuterium-labeled analog of 3-Hydroxy agomelatine, acting as a selective antagonist of the 5-HT2C receptor. This compound demonstrates an IC50 value of 3.2 μM and a Ki of 1.8 μM, indicating its capacity to effectively inhibit receptor activity. It is valuable in research applications focused on neuropharmacology, particularly in studying mood disorders and the modulation of serotonergic signaling pathways. -
5-HT Receptor Agonist
5-Carboxamidotryptamine (5-CT) is a potent agonist of the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5A, and 5-HT7 serotonin receptors. With a Ki value of 4.6 nM for the human cloned 5-HT5A receptor, it exhibits significant biological activity. Research applications include studies on serotonin signaling pathways and investigations into temperature regulation in animal models, evidenced by its ability to induce a dose-dependent decrease in rectal temperature in mice. -
5-HT2C/5-HT2A Receptor Modulator
JPC0323 is a dual positive allosteric modulator of the 5-HT2C and 5-HT2A receptors. It demonstrates on-target properties, with favorable plasma exposure and effective brain penetration. This compound is suitable for research applications focusing on neurological diseases and mechanisms involving serotonin receptor modulation. -
Sigma/5-HT1A Receptor Agonist
OPC-14523 hydrochloride is a potent agonist of the 5-HT1A receptor, exhibiting high affinity for sigma receptors (σ1/2 IC50=47/56 nM) and the serotonin transporter (IC50=80 nM). This compound demonstrates notable antidepressant-like activity and is valuable for research into mood disorders and neuropharmacology. Its pharmacological profile makes it a useful tool for studies investigating the role of serotonin receptors in depression and anxiety. -
Antidepressant Agent
Etoperidone is an antidepressant agent that functions as an orally active antagonist of serotonin and noradrenaline reuptake. It exhibits Kd values of 36 nM, 38 nM, 85 nM, and 570 nM for the 5-HT2 receptor, α1-adrenergic receptor, 5-HT1A receptor, and α2-adrenergic receptor, respectively. Due to its unique pharmacological profile, Etoperidone is utilized in research focused on the mechanisms of mood regulation and the treatment of depressive disorders. -
NE/5-HT Inhibitor
Ampreloxetine TFA is a potent inhibitor of norepinephrine (NE) and serotonin (5-HT) reuptake. This compound is primarily utilized in research targeting conditions such as neurogenic orthostatic hypotension. Its selective action on neurotransmitter pathways presents valuable insights into synaptic transmission and related disorders. -
Dopamine D2/D3 Receptor Antagonist
Esamisulpride is a potent antagonist of the dopamine D2 and D3 receptors, exhibiting Ki values of 4.43 nM for D2R and 0.72 nM for D3R. Additionally, it functions as a 5-HT7 receptor antagonist with a Ki of 900 nM. This compound is primarily employed in research related to schizophrenia and depression, providing valuable insights into dopaminergic and serotonergic system modulation. -
5-HT1A Receptor Antagonist
p-MPPI hydrochloride is a selective antagonist of the 5-HT1A receptor, exhibiting high affinity for this target. This compound effectively crosses the blood-brain barrier and demonstrates notable antidepressant and anxiolytic-like properties. p-MPPI hydrochloride is utilized in various research applications focused on neuropharmacology and the study of anxiety and depression-related disorders. -
5-HT Antagonist
Ketanserinol is a selective competitive antagonist of serotonin (5-HT) receptors. It exhibits significant biological activity against 5-HT in various vascular tissues, with KB values of 6.5 in large coronary arteries and 6.4 in pulmonary arteries. This compound serves as a valuable tool in cardiovascular research, particularly in studies examining the role of serotonin in vascular function and associated disorders. -
Sigma Receptor Antagonist
BMY-14802 hydrochloride is a selective antagonist of the sigma receptor, exhibiting an IC50 of 112 nM. It also functions as an agonist for the 5-HT1A and adrenergic α1 receptors. BMY-14802 hydrochloride demonstrates antipsychotic activity, making it a valuable tool for research in neuropharmacology and the investigation of psychiatric disorders. -
5-HT1A Receptor Modulator
Ipsapirone is a selective modulator of the 5-HT1A receptor, functioning primarily as a partial agonist. This compound is recognized for its anxiolytic properties and can exhibit antagonistic effects on the 5-HT1A receptor at higher concentrations. Additionally, at elevated doses, Ipsapirone may inhibit 5-HT2 receptor activity and α1-adrenergic signaling. It serves as a valuable tool in neuropharmacological research, particularly in studies related to anxiety and mood disorders. -
5-HT Receptor Inhibitor
Davidigenin is a selective inhibitor of the 5-HT receptor, exhibiting significant antidiabetic properties along with antitumor, antispasmodic, and antioxidant activities. This compound effectively inhibits duodenal contractions triggered by acetylcholine or histamine, making it a valuable tool for research into gastrointestinal motility and related disorders. Its multifaceted biological activities suggest potential applications in studying metabolic and gastrointestinal diseases. -
5-HT6 Antagonist
Cerlapirdine is a selective and potent full antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. This compound demonstrates significant biological activity in modulating neurotransmitter systems, making it a valuable reagent for studying neurodegenerative disorders, particularly Alzheimer's disease. Cerlapirdine's antagonistic properties facilitate research into cognitive functions and the underlying mechanisms associated with synaptic plasticity and memory. -
5-HT/dopamine receptor Antagonist
Ziprasidone amino acid is a known impurity of Ziprasidone, functioning primarily as a 5-HT (serotonin) and dopamine receptor antagonist. This compound demonstrates significant antipsychotic activity, making it valuable in the study of neurological disorders. Its unique properties can aid researchers in investigating the mechanisms of antipsychotic effectiveness and receptor interactions in related drug development. -
5-HT Receptor
1-(Carboxymethyl)cyclohexanecarboxylic acid functions as a precursor for the synthesis of serotonin (5-HT) receptor subtype 5-HT2A antagonists. This compound is recognized as a potential impurity in commercial preparations of the antiepileptic agent Gabapentin. Its relevance in scientific research extends to studying the modulation of serotonergic pathways, making it valuable for investigations into neuropharmacology and related fields. -
5-HT2A Receptor Agonist
AL-34662 is a selective agonist of the 5-HT2A receptor, exhibiting an IC50 of 0.77 nM for the rat receptor and 1.5 nM for the human receptor. In addition to its primary activity, AL-34662 demonstrates weak α-1D adrenergic agonist properties with an EC50 of 0.4 μM. This compound is primarily studied for its ocular hypotensive effects and has potential applications in the treatment of glaucoma and other ocular conditions. -
5-HT Agonist/D2 Antagonist
Quetiapine-d4 fumarate is a deuterium-labeled derivative of Quetiapine fumarate, primarily acting as a 5-HT receptor agonist and D2 dopamine receptor antagonist. This compound exhibits significant antidepressant and anxiolytic effects, making it valuable for research into mood disorders and anxiety-related conditions. Quetiapine-d4 fumarate is useful in pharmacokinetic studies and drug metabolism research, providing insights into the bioavailability and therapeutic potential of the parent compound. -
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.
