Catalog No.
Product Name
Application
Product Information
Citations
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5-HT Receptor Ligand
2-Methyl-N,N-dimethyltryptamine acts as a ligand for the serotonin (5-HT) receptors, exhibiting a pA2 value of 6.04. Its affinity for these receptors positions it as a valuable tool in the study of neuropharmacology and neurological diseases. Researchers can utilize this compound to investigate serotonin signaling pathways and their implications in various neurological conditions. -
5-HT1A/1B Autoreceptor Antagonist
SB-649915 is a potent antagonist of the 5-HT1A and 5-HT1B autoreceptors, demonstrating pKi values of 8.6 and 8.0, respectively. This compound also acts as a serotonin reuptake inhibitor in native tissue systems, making it valuable for investigating the mechanisms underlying antidepressant therapies. Its ability to modulate serotonergic signaling supports its role in research related to mood disorders and other neuropsychiatric conditions. -
5-HT1 Agonist
IS-159 is a potent agonist of the serotonin 5-HT1 receptor. This compound demonstrates significant biological activity in modulating serotonergic signaling, making it a valuable tool for researching migraine pathophysiology and potential therapeutic interventions. Its selective action on the 5-HT1 receptor provides insights into serotonin-related mechanisms in migraine and other related disorders. -
5-HT3 Receptor Antagonist
Cilansetron is a selective 5-HT3 receptor antagonist that inhibits serotonin-mediated signaling at this receptor subtype. It is primarily utilized in research focused on gastrointestinal disorders, particularly in studies of irritable bowel syndrome. Cilansetron's ability to modulate gut motility and visceral hypersensitivity makes it a valuable tool for investigating therapeutic strategies for related conditions. -
5-HT2 Ligand
4-Bromo-2,5-DMMA is a selective ligand for the 5-HT2 receptor. It demonstrates a significant affinity for 5-HT2 binding sites, with an effective dose (ED50) of 0.82 mg/kg observed in rat discrimination tests. This compound is utilized in pharmacological research focusing on serotonergic signaling and its implications in neuropsychopharmacology. -
5-HT1BR Inverse Agonist
SB-236057 is an inverse agonist of the 5-HT1B receptor, known for its significant impact on skeletal development in animal models. This compound influences gene expression during embryonic development by disrupting the Notch signaling pathway and interacting with r-esp1. In preclinical studies, SB-236057 has been shown to cause somatic patterning and tail extension defects in rat embryos, making it a valuable tool for investigating developmental biology and teratogenicity. -
5-HT3 Antagonist
MCI-225 is a selective antagonist of the 5-HT3 receptor, with notable activity as a noradrenaline reuptake inhibitor. This compound exhibits antidepressant effects in vivo, making it valuable for research focused on mood disorders and neuropharmacology. Its unique mechanism can aid in the investigation of therapeutic strategies addressing serotonergic and noradrenergic system interactions. -
5-HT Uptake Inhibitor
Litoxetine is a selective 5-HT uptake inhibitor that functions primarily through its action on serotonin transporters. It also acts as a 5-HT3 receptor antagonist, exhibiting a Ki value of 85 nM for cerebral 5-HT3 receptors. This compound is utilized in research related to depression and nausea, showcasing its potential as an antidepressant and antiemetic agent. -
5-HT1A Partial Agonist
Zalospirone is a cyclic imide and a partial agonist of the 5-HT1A receptor. It exhibits antidepressant-like activity, making it a valuable candidate for research into mood disorders. Its mechanism of action may provide insights into neuropharmacology and potential therapeutic applications in the treatment of depression. -
5-HT3/5-HT4 Receptor Antagonist
Fabesetron hydrochloride is an orally active antagonist of the 5-HT3 and 5-HT4 receptors. This compound demonstrates significant efficacy in mitigating both acute and delayed emesis associated with cancer chemotherapy. Fabesetron hydrochloride serves as a valuable tool in research on anti-emetic therapies and the management of nausea and vomiting in oncological treatments. -
5-HT Receptor
WAY 163909 hydrochloride is a selective agonist of the 5-hydroxytryptamine receptor 2C (5-HT2C) with an EC50 of 8 nM and maximum efficacy reaching 90%. Exhibiting minimal interaction with 5-HT2A receptors, it demonstrates a Ki value of 10.5 nM for 5-HT2C, while showing much higher Ki values of 212 nM for 5-HT2A, 343 nM for 5-HT7, and 485 nM for 5-HT2B. This specificity makes it a valuable tool for studying the physiological and pharmacological roles of the 5-HT2C receptor in various biological systems. -
5-HT6 Receptor Modulator/Lp-PLA2 Inhibitor
Goxalapladib is a selective modulator of the 5-HT6 receptor that also serves as an inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2). Its mechanism of action suggests potential applications in the investigation of atherosclerosis-related cardiovascular diseases. This compound facilitates research into the modulation of lipid metabolism and inflammation, making it a valuable tool for studies focused on cardiovascular health. -
5-HT Antagonist
p-MPPF dihydrochloride is a selective 5-HT antagonist that effectively inhibits the reduction of phosphorylated Erk1/2 levels in the hippocampus caused by 8-OH-DPAT in rat models. This compound is valuable for studying the neurochemical pathways involved in neurological diseases, making it a key reagent in neuroscience research. -
5-HT1/D2 Agonist
Sarizotan dihydrochloride is a potent agonist of the serotonin 5-HT1A receptor and dopamine receptors. It demonstrates strong activity with IC50 values of 6.5 nM for rat 5-HT1A, 0.1 nM for human 5-HT1A, 15.1 nM for rat D2, 17 nM for human D2, 6.8 nM for human D3, and 2.4 nM for human D4.2. Sarizotan dihydrochloride is utilized in research to explore neuropharmacology, behavior, and potential therapeutic effects on psychiatric disorders. -
5-HT3 Receptor Antagonist
Itasetron is a selective 5-HT3 receptor antagonist known for its potent antiemetic properties. This compound has been shown to enhance spatial learning and memory in aged rat models, making it relevant for studies on age-related cognitive decline. Research applications include investigations into memory degeneration and the therapeutic potential of 5-HT3 receptor modulation in cognitive disorders. -
5-HT Receptor Agonist
25I-NBMD hydrochloride is a potent agonist of the 5-HT2A receptor, a key target in serotonin signaling pathways. This compound enhances the affinity and activity at this receptor, making it valuable for research investigating serotonin-related effects and behaviors. Its unique structure positions it as a useful tool for exploring the pharmacological properties of hallucinogenic compounds and their influence on neuropsychiatric conditions. -
5-HT Receptor Control
8-Hydroxy mirtazapine primarily targets 5-HT receptors, functioning as a significant metabolite of the antidepressant Mirtazapine. It is produced through the enzymatic action of cytochrome P450 isoform CYP2D6. This compound is utilized in research focused on serotonin receptor modulation and its implications in mood disorders. -
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. -
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. -
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. -
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.
