Catalog No.
Product Name
Application
Product Information
Citations
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5-HT4 Receptor Agonist
SC-53116 is a selective agonist of the 5-HT4 receptor, demonstrating an EC50 value of 23 nM. This compound is pivotal in research on gastrointestinal motility and cognitive function due to its role in enhancing the activity of serotonergic signaling pathways. SC-53116 is utilized in studies exploring the therapeutic potential for conditions associated with serotonin dysregulation. -
5-HT2 Receptor Antagonist
LY108742 is a potent 5-HT2 receptor antagonist, exhibiting IC50 values of 9.3 nM in rat models and 57.2 nM and 56.8 nM in pig and monkey models, respectively. This compound is primarily utilized in research to explore serotonin receptor signaling pathways and their role in neuropharmacology. Its inhibitory effects on the 5-HT2 receptor make it valuable for studies related to mood disorders and other psychiatric conditions. -
Stable Isotope
Loxapine-d8 hydrochloride is a deuterated derivative of Loxapine, primarily acting as a D2 and D4 dopamine receptor inhibitor. This stable isotope is utilized in research to study pharmacokinetics and metabolic pathways of Loxapine. Its serotonergic receptor antagonism further facilitates investigations into the neuropharmacological effects associated with dibenzoxazepine anti-psychotic agents. -
5-HT Receptor Control
3C-B-FLY hydrochloride is an α-methylated analog of 2C-B-FLY that selectively targets the 5-HT receptor. This compound exhibits significant serotonergic activity, making it a valuable tool for research into neuropharmacology and the effects of psychoactive substances on serotonin signaling. Its unique properties enable investigations into receptor interactions and lead compounds for potential therapeutic applications. -
D3 Receptor Ligand
Dopamine D3 Receptor Ligand-5 is a selective ligand for the dopamine D3 receptor, exhibiting a Ki value of 0.14 nM, indicating high affinity. Additionally, it also demonstrates significant interaction with the D2 receptor, possessing a Ki value of 2.85 nM. This compound is primarily utilized in neurological research to investigate dopamine signaling pathways and their implications in neuropsychiatric disorders. Its specificity for the D3 receptor makes it a valuable tool for studies on receptor pharmacology and therapeutic development. -
5-HT2 Inhibitor
Cloroperone is a potent 5-HT2 receptor inhibitor with a Ki value of 4.5 nM. It demonstrates significant biological activity in modulating serotonin signaling pathways, making it useful in the study of psychiatric disorders. Cloroperone's inhibitory effects on the 5-HT2 receptor can aid in research focused on understanding the mechanisms underlying various neuropsychiatric conditions. -
5-HT1AR Agonist
5-MeO-pyr-T (5-Methoxy pyrrolidinyltryptamine) serves as an agonist for the 5-HT1A receptor, demonstrating binding affinities (Kis) of 0.577 μM for 5-HT1A and 373 μM for 5-HT2A. This compound inhibits serotonin (5-HT) uptake and promotes 5-HT release, thereby influencing serotonergic signaling. The hypolocomotor effects induced by 5-MeO-pyr-T make it a valuable tool for investigating functions related to serotonin pathways and their implications in neuropsychopharmacology. -
5-HT4 Receptor Antagonist
SB-203186 is a highly selective antagonist of the 5-HT4 receptor. It demonstrates a potent competitive antagonistic effect, as evidenced by its pKB value of 8.3 in the isolated right atrium model of piglets. The compound effectively shifts the serotonin-induced tachycardia curve to the right in a dose-dependent manner without inhibiting the maximum response. While SB-203186 shows significant antagonistic activity in pig and human atria, it does not exhibit substantial effects in rat atria, making it valuable for investigating conditions such as arrhythmias and abnormal myocardial contraction. -
5-HT Receptor Antagonist
LY86057 is a selective antagonist of the 5-HT2 receptors, exhibiting notable affinity for porcine, squirrel monkey, and human 5-HT2 receptor subtypes. This ergoline derivative provides valuable insights into species-specific receptor recognition, demonstrating a higher selectivity for 5-HT2 receptors compared to other compounds. Researchers can utilize LY86057 in studies examining serotonergic signaling and its implications in various biological processes and psychiatric disorders, facilitating a deeper understanding of receptor dynamics across different species. -
5-HT7 Receptor Ligand
SEP-4199 is a potent 5-HT7 receptor ligand with a Ki value of 66 nM for the human 5-HT7 receptor and 16 nM for the human D2 receptor. It has demonstrated antidepressant activity and is particularly relevant for studies focused on bipolar depression. This compound serves as a valuable research tool for exploring serotonergic and dopaminergic pathways in mood disorders. -
5-HT2A Receptor Activator
ETH-LAD (N-Ethyl-nor-LSD) is a selective activator of the 5-HT2A receptor, exhibiting a binding affinity with a Ki value of 5.1 nM. Additionally, it demonstrates affinity for dopamine receptors D1 and D2, with Ki values of 22.1 nM and 4.4 nM, respectively. ETH-LAD is utilized in research exploring psychoactive effects and receptor pharmacology in various models, including rat studies. -
5-HT Receptor Agonist
2-Methyl-5-HT maleate is a potent and selective agonist of the 5-HT3 receptor, which plays a crucial role in neurotransmission related to mood regulation. This compound has demonstrated anti-depressive-like effects in various models, making it a valuable tool for studies aimed at understanding serotonin signaling and its implications in mood disorders. It is suitable for research applications investigating the role of 5-HT3 receptors in both physiological and pathophysiological conditions. -
5-HT1A Agonist
F 13714 is a prototypical agonist of the 5-HT1A receptor, featuring a pKi of 10.23. This compound is known to induce significant calcium (Ca2+) responses, making it a valuable tool for studying serotonin receptor signaling. Its application in research includes investigations into neuropharmacology and the modulation of serotonergic pathways. -
5-HT Receptor Agonist
RU 27849 is a selective agonist of the 5-HT receptor, specifically targeting the 5-HT2A subtype. This compound is instrumental in investigating tryptamine recognition site interactions and understanding serotonin signaling pathways. It is utilized in research focused on neuropharmacology and the role of serotonin in various physiological and pathological processes. -
5-HT Receptor Agonist
(Rac)-S 16924 is a partial agonist of the 5-HT1A receptor. This compound modulates signaling by stabilizing the receptor in its G-protein-coupled state, influencing intracellular signaling pathways linked to the 5-HT1A receptor. (Rac)-S 16924 is particularly valuable for investigating the role of the 5-HT1A receptor in mental health disorders, including schizophrenia. -
Asenapine Metabolite
N-Desmethyl asenapine is a primary metabolite of Asenapine, an atypical antipsychotic agent. This compound functions as an antagonist at multiple receptor sites, including serotonin, adrenoceptors, dopamine receptors, and histamine receptors. N-Desmethyl asenapine is valuable for research into psychopharmacology and the pharmacokinetics of antipsychotic drugs. Its role in studying the therapeutic and side effects associated with Asenapine makes it a significant reagent in the field. -
Stable Isotope
Quetiapine-d8 fumarate is a deuterated derivative of Quetiapine, primarily functioning as a stable isotope for enhanced analytical studies. This compound acts as a 5-HT receptor agonist, exhibiting a pEC50 of 4.77 for the human 5-HT1A receptor, while also serving as a dopamine receptor antagonist with a pIC50 of 6.33 for the human D2 receptor. Quetiapine-d8 fumarate demonstrates moderate to high affinity for multiple receptors, including human D2, 5-HT1A, 5-HT2A, and 5-HT2C, with respective pKis of 7.25, 5.74, 7.54, and 5.55, making it valuable for research into antidepressant and anxiolytic pharmacology. -
5-HT Receptor Inhibitor
4-CAB hydrochloride is a potent 5-HT receptor inhibitor that acts as an analog of p-chloroamphetamine. It demonstrates significant inhibition of serotonin reuptake with an IC50 value of 330 nM, alongside dopamine reuptake inhibition with an IC50 of 2.3 μM. This compound is valuable for research focusing on serotonergic and dopaminergic neurotransmission, as well as investigations into the neuropharmacology of psychoactive substances. -
5-HT/NE Inhibitor
(R)-Indeloxazine benzenesulfonate is a potent inhibitor of serotonin (5-HT) and norepinephrine (NE) reuptake, exhibiting IC50 values of 0.35 μM and 3.3 μM, respectively. This compound demonstrates notable analgesic effects reminiscent of curative outcomes and may enhance nerve function by improving neurotrophic support. It is valuable for research applications focusing on pain management and the exploration of neurological disorders. -
5-HT Receptor Control
4-Iodoamphetamine hydrochloride is a chemical compound that acts primarily on serotonin (5-HT) receptors. It selectively induces the release of serotonin and inhibits its reuptake in rat brain synaptosomes, making it a valuable tool for studying serotonergic signaling. This compound has applications in neuropharmacological research, particularly in the investigation of mood disorders and other conditions related to serotonin dysregulation. -
5-HT4 Receptor Agonist
SC-53116 hydrochloride is a selective agonist of the 5-HT4 receptor, exhibiting an EC50 value of 23 nM. This compound effectively modulates serotonin signaling pathways, making it valuable for researching gastrointestinal motility and cognitive function. Its specificity for the 5-HT4 receptor facilitates investigations into neuropharmacology and potential therapeutic applications in disorders related to serotonin dysregulation. -
5-HT1A receptor partial Agonist
Revospirone is a partial agonist of the 5-HT1A receptor, exhibiting a Ki value of 2 nmol/L. This compound effectively inhibits adenylate cyclase activity with an IC50 of 124 nmol/L. Revospirone is utilized in research applications targeting neuropharmacology and may aid in studying anxiety and mood disorders through its influence on serotonergic signaling pathways. -
5-HT2 Receptor Agonist
7-Methyl DMT (7-TMT) is a potent agonist of the 5-HT2 receptor, a subtype of the serotonin receptor family. As a tryptamine derivative, it exhibits significant biological activity relevant to neuropharmacology and the study of neurological diseases. This compound serves as an analytical reference standard for psychoactive substances, including DOM, and is utilized in research to further understand the mechanisms underlying serotonin-mediated signaling and associated neurological conditions. -
5-HT1AR Agonist
CUMI-101 is a potent agonist of the 5-HT1A receptor, exhibiting a binding affinity with a Ki of 0.15 nM and an EC50 of 0.1 nM demonstrated in the [35S]GTPγS binding assay. This compound is valuable for research into neurological disorders, where modulation of serotonin signaling may play a crucial role in therapeutic strategies. Its strong biological activity makes it a useful tool for exploring the underlying mechanisms of 5-HT1A receptor function in various brain-related conditions. -
5-HT Receptor Control
Palonosetron N-oxide functions as a metabolite of the serotonin (5-HT) receptor subtype 5-HT3 antagonist, Palonosetron. It primarily interacts with 5-HT receptors, contributing to modulation of serotonergic signaling. This compound is relevant for research involving nausea and vomiting as well as gastrointestinal motility disorders. -
5-HT Inhibitor
Femoxetine functions as a serotonin (5-HT) inhibitor, exhibiting potential antidepressant properties. By blocking the reabsorption of serotonin in nerve cells, it elevates serotonin concentrations in the synaptic cleft, thereby enhancing serotonin signaling. This compound is instrumental in researching the involvement of serotonin in depression and other affective disorders, as well as examining the effects of 5-HT reuptake inhibitors on mood regulation and behavioral responses. -
5-HT Receptor Antagonist
Fluperlapine is a potent antagonist of the 5-HT receptor, primarily involved in serotonergic signaling pathways. This compound exhibits significant activity in modulating neurochemical processes, making it a valuable tool for research into antidepressant mechanisms and potential therapeutic interventions for mood disorders. Its specificity and efficacy provide researchers with a reliable reagent for exploring the role of 5-HT receptors in neuropharmacology. -
D2 Receptor/5HT2A Receptor Antagonist
5-HT2A Antagonist 4 Methanesulfonate is a selective antagonist of both dopamine D2 receptors and serotonin 5HT2A receptors. This compound is primarily utilized in research concerning central nervous system disorders, facilitating the exploration of neuropharmacology and the modulation of neurotransmitter activity. Its dual receptor targeting makes it a valuable tool for studying the pathophysiology and treatment strategies for various neuropsychiatric conditions. -
5-HT Receptor Agonist
N-Desmethyl Zolmitriptan is an active metabolite that selectively targets the serotonin (5-HT) receptor subtypes 5-HT1B and 5-HT1D. It acts as an agonist of the 5-HT1B receptor, facilitating vasoconstriction in isolated human cerebral arteries, with an EC50 of approximately 100 nM. This compound is valuable for research into migraine mechanisms and the exploration of serotonin signaling pathways. -
5-HT Receptor Inhibitor
5-IAI hydrochloride is a selective 5-HT receptor inhibitor that modulates serotonin signaling. This compound has been shown to significantly reduce serotonin uptake sites and decrease hippocampal serotonin levels in rat models. It serves as an important tool for research into serotonin-related pathways and their implications in neuropharmacology. -
5-HT1A Receptor Agonist
Xaliproden free base is a selective agonist of the 5-HT1A receptor, exhibiting oral bioactivity. This compound demonstrates significant analgesic effects in models of acute tonic nociceptive pain and possesses neuroprotective properties. Additionally, Xaliproden free base effectively mitigates paclitaxel-induced mechanical allodynia by reducing the hyperactive responses of primary afferent neurons, making it valuable in pain and neuroprotection research. -
5HT Receptor Antagonist
ICI 169369 free base is a selective and non-competitive antagonist of the 5-HT receptor. This compound effectively diminishes vasopressin responses to insulin-induced hypoglycemia without affecting ACTH, prolactin, or growth hormone release. ICI 169369 also modulates centrally mediated 5-HT activity and has been shown to reduce portal pressure in portal hypertensive models, making it a valuable tool for research in neuroendocrine regulation and vascular physiology. -
5-HT3 Antagonist
Zacopride is a potent orally active antagonist of the 5-HT3 receptor, with a Ki value of 0.38 nM, and an agonist of the 5-HT4 receptor, exhibiting a Ki of 373 nM. This compound demonstrates significant biological activities, including the regulation of gastrointestinal motility, modulation of cardiac function, and the provision of anxiolytic and antiemetic effects. Zacopride is primarily utilized in research focusing on gastrointestinal disorders, cardiovascular conditions, and psychiatric diseases such as anxiety. -
5-HT Receptor Agonist
25E-NBOMe hydrochloride is a potent agonist of the 5-HT2A receptor, derived from 2C-E with an N-(2-methoxybenzyl) modification at the amine. It exhibits significant binding affinity for the 5-HT receptor family, making it useful in neuropharmacological research. This compound serves as a valuable tool for studying receptor mechanism and the physiological impacts of serotonergic signaling. -
5-HT2 Receptor Antagonist
LY53857 is a potent antagonist of the 5-HT2 receptor, effectively inhibiting vasoconstriction mediated by serotonin. In preclinical studies, LY53857 demonstrated the ability to block the depressor response to serotonin without significantly affecting mean arterial blood pressure in spontaneously hypertensive rats. Furthermore, LY53857 enhances neurotransmitter release in rat vas deferens and guinea pig ileal nerves, indicating its potential utility in elucidating serotonergic signaling pathways and exploring therapeutic applications in related cardiovascular and neural disorders. -
5-HT1A Receptor Agonist
Binospirone is a selective agonist of the 5-HT1A receptor. It exhibits significant anxiolytic activity, making it useful in the exploration of anxiety-related conditions. Additionally, Binospirone serves as a valuable tool in research investigating movement disorders, providing insights into the underlying mechanisms of these conditions. -
5-HT Receptor Inhibitor
PF-05212377 is a selective inhibitor of the serotonin receptor 5-HT6. This compound serves as a substrate for the P-glycoprotein non-BCRP human transporter and demonstrates blood-brain barrier permeability in non-human primates. PF-05212377 holds potential for research applications related to Alzheimer's Disease, enabling exploration of its role in neurodegenerative mechanisms and therapeutic strategies. -
5-HT Receptor Agonist
Pumosetrag is a selective 5-HT receptor agonist that modulates serotonin activity in the central nervous system. This compound exhibits notable biological activity in neuropharmacological research, serving as a valuable tool in studies related to mood disorders, anxiety, and other serotonin-related conditions. Pumosetrag's mechanism of action provides insights into receptor function and potential therapeutic pathways in serotonergic signaling. -
5-HT2 Receptor Antagonist
Tiospirone is a potent 5-HT2 receptor antagonist, demonstrating additional affinity for D2, 5-HT1A, 5-HT7, and sigma receptors. This compound has been shown to decrease ethanol consumption while enhancing food intake in rat models. Additionally, Tiospirone can diminish the reinforcing effects of cocaine, as evidenced in the conditioned place preference paradigm, making it a valuable tool for research into addiction and feeding behavior. -
5-HT1a Receptor Ligand
MDL 72832 (hydrochloride) is a selective ligand for the 5-HT1a receptor, a crucial target in neuropharmacology. This compound exhibits high affinity for the receptor, making it a valuable tool for studying serotonergic signaling pathways. It is primarily utilized in research applications related to anxiety, depression, and other neuropsychiatric disorders. -
Stable Isotope
Melperone-d4 hydrochloride is a deuterium-labeled derivative of Melperone hydrochloride, a butyrophenone with atypical antipsychotic properties. It acts as a multireceptor antagonist, exhibiting binding affinities (Kd values) of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Additionally, Melperone-d4 displays weak interactions with several other receptors and inhibits CYP2D6. This reagent is particularly valuable for investigating schizophrenia and managing agitation in geriatric populations. -
D2/5-HT2 Antagonist
Iloperidone hydrochloride is a dual D2 and 5-HT2 receptor antagonist. It is classified as an atypical antipsychotic and is primarily utilized in the treatment of schizophrenia symptoms. This compound is valuable for research focused on neuropharmacology and the elucidation of antipsychotic mechanisms. -
5-HT2 Receptor Antagonist
W-2451 is a selective antagonist of the serotonin 5-HT2 receptor. It exhibits potential neuroprotective effects, making it a valuable tool for investigating neurological disorders and their underlying mechanisms. This compound may aid in the elucidation of serotonin-related pathways in various neurological contexts. -
5-HT Receptor Agonist
2,6-DMA hydrochloride is a selective agonist for the serotonin 5-HT2 receptor, demonstrating an apparent pA2 value of 5.09. This compound plays a significant role in neurotransmission and has applications in studying serotonergic signaling pathways. It is useful in research investigating mood disorders, anxiety, and various neuropsychiatric conditions. -
5-HT2C Agonist
WAY 629 is a potent and selective agonist of the 5-HT2C receptor, demonstrating an EC50 of 426 nM for 5-HT2C and a significantly higher EC50 of 260,000 nM for 5-HT2A. This compound has been shown to effectively reduce feeding behavior, making it a valuable tool for studies related to appetite regulation and metabolic research. Its specificity and efficacy underscore its potential for use in pharmacological investigations involving serotonergic modulation. -
5-HT3 Receptor Antagonist
Lurosetron is a potent 5-HT3 receptor antagonist, specifically developed as a 6-fluoro analogue of Alosetron. This compound demonstrates significant biological activity through the inhibition of recombinant cytochrome P450 isoforms, including rbtCYP1A2 with an IC50 of 0.1 μM, as well as rbtCYP2C9 and rbtCYP3A4, exhibiting IC50 values ranging from 3.5 μM to 16 μM. Lurosetron is primarily utilized in research focused on gastrointestinal disorders and the modulation of serotonin pathways. -
5-HT6 Receptor Agonist
WAY 208466 is a selective agonist of the 5-HT6 receptor, exhibiting an EC50 of 7.3 nM. This compound promotes the elevation of GABA levels in the dorsolateral frontal cortex following both acute and chronic administration in rat models. WAY 208466 is primarily utilized in research related to anxiety disorders, particularly obsessive-compulsive disorder (OCD). -
5-HT1AR Regulator
Cannabidiolic acid methyl ester is a potent regulator of the 5-HT1A receptor. This orally active analogue enhances receptor activation and promotes the expression of c-Fos and NeuN in certain hypothalamic nuclei in rat models. Its biological activity suggests potential applications in anti-nausea, anti-anxiety, and tissue injury studies. -
5-HT4 Receptor Agonist
ML 10302 hydrochloride is a highly selective agonist for the 5-HT4 receptor, exhibiting an EC50 of 4 nM. This compound demonstrates over 680-fold selectivity for the 5-HT4 receptor compared to the 5-HT3 receptor in binding assays. ML 10302 hydrochloride is useful for research applications related to gastrointestinal motility disorders and central nervous system function, providing insights into the therapeutic potential for conditions influenced by serotonergic signaling. -
5-HT6 Receptor Antagonist
NPS ALX Compound 4a dihydrochloride is a highly potent and selective antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor, demonstrating an IC50 of 7.2 nM and a Ki of 0.2 nM. This compound is valuable for research applications targeting neuropsychiatric disorders, where modulation of 5-HT6 receptor activity may be of therapeutic interest. Its specificity and potency make it an essential tool for elucidating the role of the 5-HT6 receptor in various biological processes.
