Catalog No.
Product Name
Application
Product Information
Citations
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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. -
5-HT2C/2B Receptor Antagonist
SB228357 is a selective and potent antagonist of the 5-HT2C and 5-HT2B receptors, exhibiting pKi values of 6.9, 8.0, and 9.0 for the 5-HT2A, 5-HT2B, and 5-HT2C receptors, respectively. This compound demonstrates significant antidepressant and anxiolytic effects, making it valuable for research focused on mood disorders and anxiety-related conditions. Its oral bioavailability further enhances its utility in pharmacological investigations. -
5-HT Antagonist
(S)-WAY 100135 dihydrochloride is a highly selective and potent antagonist of the 5-HT 1A receptor, exhibiting an IC50 of 33.9 nM. This compound demonstrates anxiolytic effects in animal models, making it a valuable tool for research in anxiety disorders and related neuropharmacological studies. Its specificity for the 5-HT 1A target enables investigations into serotonin receptor-mediated signaling pathways and their implications in various psychiatric conditions. -
5-HT2A Receptor Agonist
LPH-5 is a selective agonist of the 5-HT2A receptor, exhibiting an EC50 of 190 nM. Through its activation of the 5-HT2A receptor, LPH-5 plays a critical role in modulating mood, perception, and various central nervous system processes. This compound is valuable for investigating the involvement of the 5-HT2A receptor in psychiatric disorders such as depression, anxiety, and substance use disorders. -
5-HT4 Receptor Agonist
Relenopride hydrochloride is a selective agonist of the 5-HT4 receptor, exhibiting a Ki value of 4.96 nM, which confirms its high affinity for this target. With significantly lower affinities for the 5-HT2A and 5-HT2B receptors, Relenopride hydrochloride is a valuable tool for studying gastrointestinal physiology. It is primarily utilized in research on enhancing gastrointestinal motility and investigating conditions related to digestive function. -
5-HT2C Agonist
5-HT2C agonist-3 is a selective agonist for the 5-HT2C receptor, exhibiting an EC50 of 24 nM and a Ki of 78 nM. This compound demonstrates antipsychotic-like properties and effectively inhibits amphetamine-induced hyperactivity. It serves as a valuable tool for research into neuropharmacology and the modulation of serotonergic systems. -
5-HT/Serotonin Receptors Ligand
1-(2-Methoxyphenyl)piperazine hydrochloride is a ligand targeting 5-HT (serotonin) receptors, crucial for the development of various antipsychotic agents. Its high affinity for serotonin receptors makes it a valuable compound in synthesizing pharmacological agents, such as Piperazine phosphate, Piperazine citrate, and Fluphenazine dihydrochloride. Additionally, this reagent can be utilized in the synthesis of Rifampicin, contributing to studies in neuroscience and psychiatric research. -
5-HT(6/7/2A)/ Dopamin D2 Receptors Antagonist
5-HT6/7 Antagonist 1 is a potent antagonist of the 5-HT6, 5-HT7, and D2 receptors, exhibiting selectivity that spares M1 receptors and hERG channels. This compound's multifunctional activity makes it valuable for research into neuropharmacology and the modulation of serotonergic and dopaminergic systems. It provides a useful tool for studying disorders related to these receptor pathways, including anxiety, depression, and schizophrenia. -
5HT-4/5HT-3 Antagonist
Lintopride is a benzamide that acts as a potent antagonist of the 5HT-4 receptor, with moderate antagonistic properties at the 5HT-3 receptor. This compound enhances gastric emptying, stimulates motility in the antrum and duodenum, and accelerates intestinal transit in animal models. Additionally, Lintopride significantly increases the basal tone of the lower oesophageal sphincter, highlighting its potential applications in gastrointestinal research and therapy. -
5-HT5A Receptor Probe
UCSF648 is a chemical probe targeting the 5-HT5A serotonin receptor. It demonstrates weak activation of the ADRA2A and MTNR1A receptors, making it valuable for studies investigating serotonin signaling pathways. This reagent is suitable for research applications related to neuropharmacology and the modulation of serotonin receptor activity. -
5-HT1A Receptor Agonist
Tandospirone hydrochloride is a selective partial agonist of the 5-HT1A receptor, exhibiting a Ki value of 27 nM. This compound displays notable anxiolytic and antidepressant properties, making it valuable in the study of central nervous system disorders. Its unique action at the 5-HT1A receptor contributes to the understanding of underlying mechanisms related to anxiety and depression, facilitating research aimed at developing novel therapeutic approaches. -
Dopamine D2/D3/5-HT7 Receptor Inhibitor
LB-102 is an orally bioavailable inhibitor of dopamine D2, D3, and 5-HT7 receptors. It exhibits significant antagonistic activity, making it a valuable tool for investigating the neurochemical pathways involved in schizophrenia and other psychiatric disorders. This compound is useful for studies aimed at understanding the role of these receptors in various neuropsychiatric conditions. -
5-HT/DA Receptor Antagonist
Ziprasidone mesylate trihydrate is an orally active antagonist of serotonin (5-HT) and dopamine (DA) receptors, primarily targeting the 5-HT2A and D2 receptor subtypes. With a high affinity for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM), and 5-HT1A (Ki=3.4 nM), this compound is significant for studies related to mood disorders, schizophrenia, and neuropharmacology. Ziprasidone mesylate trihydrate serves as a valuable tool for exploring receptor mechanisms and assessing therapeutic effects in relevant biological models. -
TAAR1/5-HT1A Agonist
Ulotaront is a novel TAAR1 and 5-HT1A agonist that operates through a distinct mechanism separate from traditional D2 and 5-HT2A pathways. This compound exhibits significant antipsychotic-like properties, making it a valuable tool for researching schizophrenia and related neuropsychiatric disorders. Its unique profile allows for exploration of alternative treatment strategies that may enhance therapeutic options for psychiatric conditions. -
5-HT Receptor Antagonist
Clocapramine is a selective antagonist of the 5-HT2A receptor, with additional inhibitory effects on D2 dopamine receptors. This compound exhibits notable properties in modulating serotonin and dopamine signaling, making it relevant for neuropharmacological research. Clocapramine can be utilized in studies related to psychiatric disorders, including depression and schizophrenia, as well as the characterization of receptor interactions in neural pathways. -
5-HT Receptor Inhibitor
Metrenperone is a selective inhibitor of the 5-HT2 receptor, exhibiting significant antagonist activity on α1 and α2 adrenergic receptors, as well as anti-H1 and anti-dopaminergic effects. It demonstrates notable biological activities, including the reduction of blood pressure, enhancement of bradycardia during peripheral ischemia, and inhibition of serotonin-induced platelet aggregation. Additionally, Metrenperone antagonizes serotonin-mediated vasoconstriction and is involved in promoting the repair of acutely damaged collagen tissue, making it valuable for various research applications in cardiovascular and vascular biology. -
5-HT Metabolite
5-Hydroxy NMT oxalate is a metabolite of serotonin (5-HT) that functions as a neuromodulator. This compound has been implicated in various neurophysiological processes and is associated with cocaine addiction, as elevated plasma levels have been observed in affected individuals. Its utility in research extends to the study of serotonergic signaling pathways and addiction-related behaviors. -
5-HT2A Inverse Agonist
N-Desmethyl Pimavanserin is a potent inverse agonist of the 5-HT2A receptor, serving as an active metabolite of Pimavanserin. With high affinity demonstrated by a pIC50 of 8.73 and pKd of 9.3, this compound has significant implications in research focused on psychiatric disorders, such as schizophrenia and Parkinson's disease psychosis. Its role in modulating serotonergic signaling makes it an important reagent for studies investigating the therapeutic potential of 5-HT2A antagonism. -
MAO-A And 5-HT-uptake Inhibitor
Sercloremine hydrochloride is a selective and reversible inhibitor of monoamine oxidase A (MAO-A) and serotonin (5-HT) uptake. This compound is primarily utilized in research related to depression, offering insights into the modulation of serotonin levels and its effects on mood regulation. Its dual mechanism of action makes it valuable for exploring therapeutic approaches in depressive disorders. -
5-HT Reuptake Inhibitor
Clomipramine is a potent 5-HT reuptake inhibitor with an IC50 value of 1.5 nM. As a tricyclic antidepressant, it is primarily utilized in research investigating the mechanisms of depression and obsessive-compulsive disorder (OCD). Its ability to influence serotonin levels makes it a valuable tool for studying various neuropsychiatric conditions. -
5-HT2A Antagonist
Glemanserin is a potent and selective antagonist for the serotonin receptor 5-HT2A, exhibiting nanomolar affinity in various species (Ki values of 2.89, 0.54, and 2.5 nM for rat, rabbit, and human 5-HT2A, respectively). This compound is primarily utilized in neuropharmacological research to study the role of 5-HT2A receptors in various physiological and pathological conditions. Its antagonistic activity contributes to investigations into mood disorders, anxiety, and other CNS-related ailments. -
5-HT/NE Reuptake Inhibitor
Dextromilnacipran is a selective serotonin and norepinephrine (5-HT/NE) reuptake inhibitor, derived from the enantiomeric form of milnacipran. This compound also functions as a human alpha-adrenergic receptor antagonist, exhibiting an IC50 value of 3.4 μM. Dextromilnacipran is primarily utilized in research applications targeting mood disorders and neuropharmacology, facilitating investigations into its psychiatric and physiological effects. -
5-HT Uptake Blocker
Indalpine, a selective 5-HT uptake blocker, demonstrates significant potency in inhibiting serotonin transport. With an IC50 value of 36 μM, it effectively displaces ^3H-5-HT bound to brain membranes. This compound may have applications in the study of antidepressant mechanisms and is valuable for research in neuropharmacology. -
Noradrenaline And 5-HT Uptake Blocker
Clemeprol is an orally active noradrenaline and 5-HT uptake blocker. It effectively inhibits the depletion of brain noradrenaline induced by 6-Hydroxydopamine and demonstrates a dose-dependent inhibition of reserpine-induced hypothermia. Clemeprol is applicable in the investigation of depression and related neurochemical pathways. -
5-HT1 Agonist
2-Aminotetralin is a selective agonist of the serotonin 5-HT1 receptor subtypes, including 5-HT1A, 5-HT1B, and 5-HT1D. This compound demonstrates high affinity, with a Ki value of 25 nM or lower, and exhibits significant stereoselectivity, showing over a 50-fold preference for specific receptor configurations. 2-Aminotetralin is utilized in research exploring serotonin signaling pathways and their implications in neuropharmacology and mood disorders. -
5-HT Transporter Inhibitor
6-Nitroquipazine is a highly potent and selective inhibitor of the serotonin transporter (5-HT transporter), exhibiting a Ki value of 0.17 nM. This compound significantly impacts serotonin reuptake, making it a valuable tool for investigating the pathophysiology and treatment of psychiatric disorders, including depression. Its ability to modulate serotonin levels can be instrumental in research aimed at understanding mood regulation and therapeutic interventions in related conditions. -
DA/NE/5-HT Inhibitor
Tesofensine is a triple monoamine reuptake inhibitor targeting dopamine (DA), norepinephrine (NE), and serotonin (5-HT). It effectively inhibits the reuptake of these neurotransmitters in the synaptic cleft, exhibiting IC50 values of 6.5 nM for DA, 1.7 nM for NE, and 11 nM for 5-HT. Tesofensine is primarily studied for its potential as an anti-obesity agent and may be useful in related central nervous system research applications. -
5-HT Derivative
5-Propargyltryptamide (5-PT) is an alkyne-functionalized derivative of serotonin (5-HT), serving as a substrate for serotonylation in living cells. This reagent enables the conjugation of biotin, facilitating the identification of serotonylated proteins through copper-catalyzed click chemistry and mass spectrometry. 5-PT selectively labels and isolates serotonylated proteins in alveolar epithelial cells, making it a valuable tool for proteomic analysis in the study of bronchopulmonary dysplasia and related respiratory conditions. -
5-HT/Norepinephrine Reuptake Inhibitor
Desvenlafaxine is a selective 5-HT and norepinephrine reuptake inhibitor, primarily targeting the serotonin transporter (hSERT) and norepinephrine transporter (hNET) with IC50 values of 47.3 nM and 531.3 nM, respectively. This orally active compound effectively penetrates the blood-brain barrier, making it applicable in the treatment of major depressive disorders. Additionally, Desvenlafaxine exhibits weak binding affinity to the human dopamine transporter, with 62% inhibition observed at 100 μM, which may have implications for its overall pharmacological profile. -
5-HT Receptor Agonist
Serotonin is a monoamine neurotransmitter that acts as an endogenous agonist at 5-HT receptors. It plays a critical role in various physiological processes, including mood regulation and cognitive function. Additionally, serotonin functions as a catechol O-methyltransferase (COMT) inhibitor, exhibiting a Ki value of 44 μM. This compound is essential for studies related to neuroscience, pharmacology, and the understanding of mood disorders. -
5-HT4 Receptor Agonist
Tryptamine is a selective agonist of the 5-HT4 receptor, with an EC50 of 1-3 mM, and also functions as an endogenous ligand for the aryl hydrocarbon receptor (AHR), exhibiting a Kd of 10-50 nM. This compound enhances intestinal anion secretion and fluid transport by activating G protein-coupled receptors (GPCRs), thereby promoting gastrointestinal motility. Additionally, tryptamine plays a role in modulating Th17/Treg balance to inhibit neuroinflammation, influences central nervous system activity through competitive binding to 5-HT receptors, and participates in neuromodulation related to temperature and spinal reflexes. Tryptamine is useful for researching gastrointestinal disorders such as functional constipation and demonstrates efficacy in preclinical models of multiple sclerosis. -
5-HT3 receptor antagonist
(R)-RS 56812 is a selective antagonist of the 5-HT3 receptor. This compound has been shown to enhance cognitive performance in primate models, particularly in tasks involving delayed matching. The (R) isomer exhibits greater efficacy in facilitating cognitive function compared to its (S) counterpart, suggesting potential therapeutic applications in conditions associated with cognitive decline.
