Catalog No.
Product Name
Application
Product Information
Citations
-
5-HT receptor antagonist
R-96544 is an orally active antagonist of the 5-HT2A receptor. It exhibits significant biological activity by inhibiting platelet aggregation in vitro, making it a valuable reagent for research in pharmacology and cardiovascular studies. Its selective targeting of the 5-HT2A receptor positions R-96544 as an important tool for exploring serotonin-related pathways and their implications in various biological processes. -
5-HT2C Inverse Agonist
SB 206553 is an inverse agonist of the 5-HT2C receptor, demonstrating significant biological activity with pKi values of 5.6 nM, 7.7 nM, and 7.8 nM for the 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively, in HEK-293 and CHO-K1 cell lines expressing human recombinant receptors. This compound has been shown to attenuate methamphetamine-seeking behavior in rat models. SB 206553 is valuable for research into psychostimulant abuse disorders and the underlying mechanisms of serotonergic signaling. -
5-HT Receptor Inhibitor
Iprindole is a tricyclic indole compound that functions primarily as a 5-HT receptor inhibitor. It exhibits weak inhibitory effects on the reuptake of noradrenaline and serotonin (5-HT), making it relevant in the study of mood disorders and antidepressant mechanisms. This reagent is particularly useful in research applications focused on neuropharmacology and the modulation of serotonergic systems. -
5-HT Receptor Agonist
Phenylbiguanide hydrochloride is a selective agonist for the 5-HT3 receptor, exhibiting an EC50 of 3.0 ± 0.1 μM. This compound is primarily utilized in pharmacological studies investigating serotonin neurotransmission and its role in various physiological processes. It serves as a valuable tool for assessing the functional responses of 5-HT3 receptors in neurological and gastrointestinal research. -
5-HT4 Receptor Agonist
Usmarapride is a selective agonist of the 5-HT4 receptor, exhibiting potent activity with an EC50 of 27.5 nM. This compound is orally active and demonstrates the ability to penetrate the blood-brain barrier, making it a valuable tool for investigating cognitive deficits related to Alzheimer's disease. Usmarapride is primarily utilized in research focused on neuropsychological disorders and related therapeutic strategies. -
NE/serotonin 5-HT Inhibitor
Ampreloxetine is a potent and orally bioavailable norepinephrine (NE) and serotonin 5-HT inhibitor. It exhibits significant potential for investigating neurogenic orthostatic hypotension and related disorders. This compound may facilitate research on neurotransmitter modulation and its effects on blood pressure regulation. -
5-HT3 Receptor Agonist
YM-31636 free base is a potent and selective agonist of the 5-HT3 receptor, exhibiting a Ki value of 0.2 nM. This compound effectively induces contraction in isolated guinea pig distal colon, suggesting its role in gastrointestinal motility. Additionally, YM-31636 free base demonstrates tachycardia through a relative intrinsic activity of approximately 0.23 in isolated guinea pig right atrium, indicating potential applications in research focusing on constipation and related gastrointestinal disorders. -
Antipsychotic Agent
Cariprazine-d6 is a deuterium-labeled derivative of the antipsychotic agent, Cariprazine. It functions primarily as a potent antagonist at the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) dopamine receptors, while also exhibiting moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM). This compound is valuable for research into the mechanisms of antipsychotic action and the pharmacokinetics of labeled compounds. -
5-HT Agonist/D2 Antagonist
Quetiapine-d4 hemifumarate is a deuterated form of Quetiapine, functioning as a 5-HT receptor agonist and a D2 dopamine receptor antagonist. This compound exhibits notable antidepressant and anxiolytic properties, making it valuable for research into mood disorders and anxiety treatment. Its unique isotopic labeling allows for advanced studies in pharmacokinetics and metabolic pathways of Quetiapine. -
5-HT1A Antagonist
WAY-100135 dihydrochloride is a selective antagonist of the 5-HT1A receptor, exhibiting an IC50 value of 34 nM in the rat hippocampal model. This compound is of significant interest for research into its potential antipsychotic properties and its role in neurological studies. The inhibition of both presynaptic and postsynaptic 5-HT1A receptors suggests its application in investigating serotonergic signaling and related pathophysiological conditions. -
5-HT2A Receptor Antagonist
Iferanserin is a selective antagonist of the 5-HT2A receptor, exhibiting high affinity for this serotonin receptor subtype. Its biological activity suggests potential applications in the treatment of internal hemorrhoid disease, making it a valuable tool for research on gastrointestinal disorders and serotonin-mediated signaling pathways. -
5HT2A antagonist
5-HT2A Antagonist 2 is a selective antagonist that targets the 5-HT2A receptor, demonstrating an IC50 value of 14 nM. This compound exhibits favorable chemical stability and retains activity in hepatocyte and plasma environments, while showing negligible cytotoxicity across several cell lines, including VERO, HFL-1, L929, NIH3T3, and CHO-K1. It is suitable for research applications related to neuropharmacology, psychiatric disorders, and other areas involving serotonin receptor modulation. -
5-HT4 Receptor Agonist
Naronapride is a potent agonist of the 5-HT4 receptor, primarily involved in gastrointestinal motility regulation. Its biological activity enhances prokinetic effects, making it valuable for research pertaining to gastrointestinal diseases and disorders. Naronapride serves as a critical tool for understanding the mechanisms underlying gastrointestinal function and potential therapeutic interventions. -
5-HT Agonist
Quipazine dimaleate is a potent 5-HT agonist, demonstrating a Ki value of 1.4 nM for displacing [3H]GR65630 from the 5-HT3 receptor in rat models. This compound exhibits antiviral activity against SARS-CoV-2, with an EC50 of 31.64 μM, and acts as a 5-HT3 receptor antagonist in peripheral models. Quipazine dimaleate is valuable for research in neurological diseases, providing insights into serotonin receptor modulation and antiviral mechanisms. -
5-HT Receptor Agonist
(Rac)-WAY-161503 hydrochloride is a selective agonist for the 5-HT2C receptor, exhibiting a high affinity with a Ki of 4 nM and an EC50 of 12 nM. This compound shows significantly higher affinity for the 5-HT2C receptor compared to the 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 hydrochloride is primarily used in research related to anti-obesity and antidepressant effects, making it a valuable tool in neuroscience and pharmacology studies. -
5-HT2B Antagonist
LY266097 hydrochloride is a selective antagonist of the 5-HT2B receptor, with pKis of 7.7, 9.8, and 7.6 for 5-HT2A, 5-HT2B, and 5-HT2C, respectively. The blockade of the 5-HT2B receptor by LY266097 is significant for investigating pathways associated with depression and other neuropsychiatric disorders. This compound provides valuable insights into serotonergic signaling and may aid in the development of therapeutic strategies targeting these receptors. -
5-HT1B/1D Receptors Agonist
Alniditan dihydrochloride is a selective agonist of the 5-HT1B and 5-HT1D receptors, exhibiting IC50 values of 1.7 nM and 1.3 nM, respectively, in HEK293 cells. This compound demonstrates significant efficacy in preventing migraines, making it a valuable tool in migraine research. Its potent action on serotonin receptors highlights its potential applications in the study of headache disorders and related therapeutics. -
5-HT1A Receptor Agonist
Repinotan hydrochloride is a potent and selective agonist of the 5-HT1A receptor, demonstrating strong brain penetration and oral bioavailability. With Ki values of 0.19 nM in calf hippocampus, 0.25 nM in rat and human cortex, and 0.59 nM in rat hippocampus, it exhibits a high affinity for its primary target while showing minimal interaction with other related receptors. This compound is known for its pronounced neuroprotective effects and is valuable in research applications related to neurological disorders and serotonergic signaling pathways. -
α1/5-HT2A Receptor Antagonist
MT-1207 is a highly selective antagonist of the adrenergic α1 and 5-HT2A receptors, demonstrating remarkable potency with IC50 values of <0.1 nM for α1A, 0.15 nM for α1B, 1.40 nM for α1D, and 0.27 nM for 5-HT2A. This compound effectively reduces blood pressure in the 2K2C rat model, preserving renal function. MT-1207 is a promising candidate for research into vasodilatation and related cardiovascular therapies. -
5-HT1A Receptor Ligand
S-15535 is a highly selective ligand for the 5-HT1A receptor, acting as an antagonist at postsynaptic receptors and an agonist at presynaptic receptors. This dual action contributes to its significant impact on serotonergic signaling. S-15535 is primarily utilized in research investigating psychiatric disorders, particularly in understanding mechanisms related to anxiety and mood regulation. -
5-HT7 Receptor Antagonist
Aramisulpride is a selective antagonist of the 5-HT7 receptor, exhibiting a Ki value of 22 nM. It also demonstrates antagonistic properties at D2 and D3 receptors, with Ki values of 140 nM and 13.9 nM, respectively. This compound is primarily utilized in psychiatric research, providing insights into the mechanisms of mood disorders and potential therapeutic interventions. -
D2/5-HT1A Agonist
Aripiprazole monohydrate is a potent partial agonist of the dopamine D2 receptor and an inverse agonist at the 5-HT2B and 5-HT2A receptors. Additionally, it exhibits partial agonist functionality at 5-HT1A, 5-HT2C, D3, and D4 receptors. This compound is primarily utilized in research focused on schizophrenia and has also been explored for potential applications in treating COVID-19. -
5-HT6 Receptor Agonist
WAY208466 dihydrochloride is a highly selective agonist of the 5-HT6 receptor, exhibiting an EC50 value of 7.3 nM for the human receptor. This compound is known to increase cortical GABA levels in the rat frontal cortex, contributing to its pharmacological profile. It demonstrates significant antidepressant and anxiolytic-like properties, making it a valuable tool for research in neuropharmacology and mood disorder studies. -
5-HT2A Receptor Agonist
5-HT2A receptor agonist-6 is a selective agonist targeting the 5-HT2A receptor, demonstrating a pEC50 value of 6.58. This compound is integral for studying serotonergic signaling pathways and is valuable in research related to neuropharmacology and psychiatric disorders. Its specificity for the 5-HT2A receptor makes it an important tool for investigating the receptor's role in various biological processes and therapeutic applications. -
5-HT2 Agonist
α-Methylserotonin is a potent and selective agonist of the 5-HT2 receptor. As a derivative of serotonin synthesized from α-methyltryptophan, it effectively mediates lymphatic smooth muscle contraction and inhibits the up-regulation of phosphoinositide hydrolysis associated with serotonin receptor activation. This compound is valuable for research applications related to neurotransmission, smooth muscle physiology, and receptor pharmacology. -
5-HT Inhibitor
Antidepressant agent 10 is a selective 5-HT inhibitor, demonstrating IC50 values of 190 nM for 5-HT1A and 110 nM for 5-HT2. This orally active compound is valuable in the study of serotonin-related pathways and their implications in mental disorders. Researchers may utilize Antidepressant agent 10 to explore its potential effects on mood regulation and therapeutic applications in depression. -
Dopamine Receptor Agonist
TDHL (Tergurid) is a potent dopamine receptor agonist, exhibiting a Kd of 0.39 nM for the D2 receptor, and functions as an orally bioavailable 5-HT2 receptor antagonist. Its dual mechanism of action allows for comprehensive exploration in neuropharmacology studies. TDHL is suitable for investigating the role of dopamine signaling in various neurological and psychiatric disorders. -
5-HT2C Receptor Antagonist
3-Hydroxy agomelatine is a metabolite of Agomelatine that functions as a selective antagonist of the 5-HT2C receptor. With an IC50 value of 3.2 μM and a Ki of 1.8 μM, it demonstrates significant affinity for this target. This compound is primarily utilized in research focusing on mood disorders and anxiety, exploring the serotonergic system's role in various neuropsychiatric conditions. -
5-HT6receptor
SB-258585 hydrochloride is a high-affinity ligand for the 5-HT6 receptor. It exhibits selective binding to a single population of 5-HT6 receptors expressed in human cell lines, making it a valuable tool for studying receptor dynamics. This compound can be utilized to label both recombinant and natural 5-HT6 receptors in various research applications, facilitating investigations into neuropharmacology and related fields. -
Stable Isotope
Brexpiprazole S-oxide-d8 is a deuterium-labeled analog of Brexpiprazole S-oxide, the primary metabolite of the atypical antipsychotic Brexpiprazole. This compound acts as a partial agonist at human 5-HT1A and dopamine receptors, with inhibition constants (Kis) of 0.12 nM and 0.3 nM, respectively. Additionally, it functions as an antagonist at the 5-HT2A receptor, exhibiting a Ki of 0.47 nM. Brexpiprazole S-oxide-d8 is valuable for pharmacokinetic studies and metabolic profiling in research applications focused on psychiatric disorders. -
5-HT3 Antagonist
E-3620 is a potent antagonist of the 5-HT3 receptor, known to modulate the effects of serotonin in the central and peripheral nervous systems. This compound demonstrates significant activity in the inhibition of dyskinesia and can be utilized in studies focused on gastrointestinal motility disorders. E-3620 serves as a valuable tool for researchers investigating mechanisms of action related to serotonin signaling and its implications in neuropharmacology. -
MT1/MT2 Receptor Agonist
Piromelatine is a selective agonist for the melatonin MT1 and MT2 receptors, alongside its activity as a serotonin 5-HT1A/5-HT1D agonist and a 5-HT2B antagonist. This compound exhibits various biological activities, including promoting sleep, providing analgesic effects, and demonstrating anti-neurodegenerative, anxiolytic, and antidepressant properties. Additionally, Piromelatine shows inhibitory effects on pain-associated channels such as P2X3, TRPV1, and Nav1.7, making it a valuable tool for research in neuropharmacology and pain management. -
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.
