Catalog No.
Product Name
Application
Product Information
Citations
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5-HT1B Agonist
CP 93129 is a potent and selective agonist of the 5-HT1B receptor. This compound exhibits significant biological activity in modulating serotonergic signaling, making it a valuable tool in the study of various neurological conditions. CP 93129 is particularly relevant for research applications related to Parkinson's disease, where serotonergic pathways are implicated in disease progression and symptomatology. -
Quetiapine Metabolite
Quetiapine sulfone is a primary metabolite of Quetiapine, acting predominantly as a serotonin (5-HT) receptor agonist and a dopamine receptor antagonist. This compound is essential for studying the pharmacokinetics and efficacy of Quetiapine in various neurological disorders, including schizophrenia and bipolar disorder. Its role in modulating neurotransmitter systems makes it a valuable reagent for researchers exploring antipsychotic mechanisms and drug metabolism. -
5-HT4(e) Receptor Partial Agonist
Capeserod hydrochloride is a potent partial agonist of the 5-HT4(e) receptor, demonstrating a Ki value of 0.6 nM. This compound effectively stimulates cAMP production in cells expressing both 5-HT4(b) and 5-HT4(e) splice variants, with IC50 values of 244 nM and 29 nM, respectively. Capeserod hydrochloride is primarily utilized in research focused on cognitive enhancement, memory impairment, and dementia-related studies. -
D2/5-HT2A Receptors Antagonist
Clocapramine dihydrochloride hydrate is a potent antagonist of the D2 and 5-HT2A receptors. It demonstrates significant biological activity by inhibiting the signaling pathways associated with these receptors, making it valuable for pharmacological research. This compound is particularly useful in studies related to neuropharmacology, psychopharmacology, and the development of therapeutic agents targeting psychiatric disorders. -
5-HT2C Receptor Agonist
PF-04781340 is a potent and selective agonist of the 5-HT2C receptor. This compound exhibits oral bioavailability and demonstrates effective penetration of the central nervous system. PF-04781340 is relevant for research applications involving mood regulation, appetite control, and other neuropsychiatric disorders, making it a valuable tool for studies exploring serotonin receptor modulation. -
GlyT2/5HT2A Antagonist
Opiranserin is a dual antagonist of the glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), exhibiting IC50 values of 0.86 μM and 1.3 μM, respectively. Additionally, it demonstrates antagonistic activity on the recombinant P2X3 receptor with an IC50 of 0.87 μM. This compound is being developed as an injectable analgesic for the management of postoperative pain, highlighting its potential utility in pain research and pharmacological studies. -
5-HT Receptor Agonist
Deramciclane fumarate is a selective inverse agonist of the 5-HT2C receptor, exhibiting an IC50 of 168 nM. This compound modulates serotonin receptor activity, leading to decreased basal phosphoinositide hydrolysis. Deramciclane fumarate is utilized in research applications focused on neuropharmacology and the investigation of serotonin-related pathways. -
5-HT2A Receptor Agonist
5-HT2A Receptor Agonist-9 is a β-arrestin-biased agonist specifically targeting the 5-HT2A receptor. This compound exhibits significant biological activity associated with modulation of serotonin pathways, making it a valuable tool in the study of neurological disorders, including antidepressant effects and psychedelic research. Its unique mechanism offers potential insights into receptor signaling dynamics relevant to neuropharmacology. -
5-HT/Dopamine Antagonist
BGC20-761 is a selective antagonist of the 5-HT6 and dopamine receptors, exhibiting human receptor Ki values of 20 nM for 5-HT6, 69 nM for 5-HT2A, and 140 nM for D2. It has demonstrated the ability to enhance long-term memory, suggesting its potential utility in cognitive enhancement therapies. Additionally, BGC20-761 may serve as a promising candidate for the development of antipsychotic agents, supporting research in neuropharmacology and mental health disorders. -
5-HT1A Antagonist
5-HT1A Antagonist 2 is a selective antagonist of the 5-hydroxytryptamine 1A (5-HT1A) receptor. This compound is instrumental in investigating the physiological and pharmacological roles of the 5-HT1A receptor in disorders such as depression and attention deficit hyperactivity disorder (ADHD). Its ability to modulate serotonin signaling makes it a valuable tool in neuropharmacological research. -
5-HT Agonist
Tiflucarbine is a potent agonist of serotonin receptors (5-HT), specifically acting on both 5-HT1 and 5-HT2 subtypes. As a derivative of tetrahydrothieno-7-carboline, Tiflucarbine exhibits significant antidepressant properties through its interaction with central 5-HT binding sites. This compound is valuable for research applications focused on depression, anxiety disorders, and other conditions linked to serotonin dysregulation. -
5-HT Receptor
R 50595 hydrochloride is a selective noncompetitive antagonist of the 5-HT receptor. This compound effectively inhibits the actions of cisapride and BRL 24924, demonstrating a complete blockade of 5-HT effects at concentrations up to 3 X 10(-7) M without influencing responses to electrical stimulation. R 50595 hydrochloride is valuable for researchers investigating serotonin receptor signaling and related pathways in pharmacological studies. -
5-HT2A Agonist
5-HT2A Agonist 7 is a highly selective agonist for the serotonin receptor 2A (5-HT2A), exhibiting an EC50 value of 12 nM. This compound demonstrates significant biological activity and is particularly relevant for research into psychiatric disorders, including depression. Its oral bioavailability enhances its potential for in vivo studies, making it a valuable tool for investigating the role of 5-HT2A in neuropsychiatric conditions. -
5-HT Receptor Agonist
Rizatriptan hemisulfate hemihydrate is a potent agonist of the 5-HT1B and 5-HT1D serotonin receptors. It exhibits peripheral vasoconstrictive properties and effectively crosses the blood-brain barrier, making it valuable for modulating pain neurotransmission within the central nervous system. This compound is primarily used in research related to migraine pathophysiology and the study of serotonin receptor mechanisms. -
5-HT2A Agonist
5-HT2A receptor agonist-7 is a selective agonist for the 5-HT2A receptor. It demonstrates a compelling biological activity with an EC50 value of less than 100 nM, making it a potent tool for the modulation of serotonergic signaling. This compound is useful in research applications focused on understanding mood disorders, psychotropic drug actions, and neuropharmacology involving serotonergic pathways. -
5-HT Receptor Agonist
2C-TFM hydrochloride is a potent agonist of the 5-HT receptor subtypes 5-HT2A and 5-HT2C, known for its para-trifluoromethyl substitution on a 5-dimethoxyphenethylamine framework. This compound exhibits significant biological activity related to serotonin receptors, making it valuable for research in neuropharmacology and the study of serotonergic signaling pathways. It may be utilized in investigations of mood disorders, anxiety, and other conditions influenced by serotonin receptor modulation. -
5-HT4 Receptor Agonist
THRX-194556 is a 5-HT4 receptor agonist that enhances gastrointestinal motility and may play a role in cognitive function. Its primary biological activity makes it a valuable tool for studying gastrointestinal functional disorders and Alzheimer's disease. This compound can help elucidate the therapeutic potential of 5-HT4 receptor modulation in various pathological conditions. -
5-HT6R Antagonist
SGS-518 is a selective antagonist of the 5-HT6 receptor. It exhibits potential therapeutic effects in the study of cognitive impairments, including amnesia, anxiety, and depression. Additionally, SGS-518 has been shown to provide protective effects in mouse retina at elevated doses, offering valuable insights for neuroprotective research applications. -
5-HT2CR Agonist
5-HT2CR agonist 1 is a selective partial agonist of the 5-HT2C receptor, displaying an effective maximum response (Emax) of 71.09% and an EC50 of 121.5 nM. This compound has been shown to exhibit specificity, with no activity towards 5-HT2A or 5-HT2B receptors. Furthermore, it demonstrates no recruitment activity for β-arrestin and minimal inhibition of hERG channels at 10 μM. This profile makes 5-HT2CR agonist 1 a valuable tool for research in neuropharmacology and receptor signaling pathways. -
D2 Antagonist
Clozapine dihydrochloride is an antipsychotic compound that primarily functions as a dopamine D2 receptor antagonist, exhibiting a Ki of 75 nM. It demonstrates significant affinity for muscarinic M1 and serotonin 5HT2A receptors, with Kis of 9.5 nM and 4 nM, respectively. Additionally, Clozapine acts as a potent and selective agonist at the muscarinic M4 receptor, with an EC50 of 11 nM. This compound is crucial for research into schizophrenia and related neuropsychiatric disorders. -
5-HT7/5-HT1A Receptor Agonist
E-55888 is a selective and potent agonist of the 5-HT7 and 5-HT1A receptors, exhibiting Ki values of 2.5 nM and 700 nM, respectively. This compound demonstrates significant analgesic and antinociceptive properties, effectively reducing the nociceptive response in capsaicin-sensitized mice. E-55888 serves as a valuable tool for researchers investigating pain mechanisms and therapeutic approaches to pain management. -
Triple Reuptake Inhibitor
Tedatioxetine is a serotonin and norepinephrine-preferring triple reuptake inhibitor (TRI) that also functions as an antagonist of 5-HT2A, 5-HT2C, 5-HT3, and α1A-adrenergic receptors. This compound exhibits significant biological activity in modulating neurotransmitter levels, making it relevant for research in neuropharmacology. Its mechanism of action positions it as a valuable tool in studies related to mood disorders and anxiety. -
5-HT2A Receptor Agonist
5-HT2A receptor agonist-2 is a potent agonist targeting the serotonin 5-HT2A receptor. It demonstrates high affinity with EC50 values of 1.7 nM for 5-HT2A, 0.58 nM for 5-HT2B, and 0.50 nM for 5-HT2C receptors. This compound is valuable for research into serotonin signaling pathways and their implications in neuropsychiatric disorders, as well as in studies evaluating receptor pharmacology and function. -
5-HT1A Receptor Antagonist
MM 77 dihydrochloride is a selective antagonist of the 5-HT1A receptor, primarily exhibiting an inhibitory effect on postsynaptic serotonin signaling. This compound demonstrates notable anxiolytic-like properties, making it valuable for research exploring anxiety disorders and related neuropharmacological mechanisms. Its specificity for the 5-HT1A receptor positions it as a useful tool in investigating serotonin receptor functions and therapeutic interventions in psychiatric conditions. -
5-HT4 Receptor Antagonist
SC-53606 is a potent and selective antagonist of the 5-HT4 receptor, exhibiting a pA2 value of 8.13. It effectively inhibits the 5-HT4 receptor-mediated relaxation in Carbachol-induced contractions, making it valuable for studying gastrointestinal motility and related disorders. This compound is useful in research focused on neuropharmacology and the serotonergic system. -
Piperazine
1-(3-Fluorophenyl)piperazine (hydrochloride) is a selective blocker of the 5-HT receptor 1A and an adrenergic receptor antagonist. This compound exhibits significant biological activity relevant to research in neuropharmacology, particularly in the study of serotonergic and adrenergic signaling pathways. It can be utilized in various applications, including the investigation of anxiety, depression, and other mood disorders. -
5-HT Receptor
WAY-100135 is a serotonergic compound that acts primarily as a potent antagonist of the 5-HT1A receptor and a partial agonist of the 5-HT1D receptor, exhibiting minimal activity at the 5-HT1B receptor. This compound is valuable in research applications focused on serotonin receptor signaling and its implications in neuropharmacology. WAY-100135 is commonly used to investigate the role of serotonergic pathways in various physiological and pathological conditions. -
5-HT1B Agonist
CP94253 is a selective agonist of the serotonin receptor 1B (5-HT1B) that operates through competitive binding at the receptor site. This compound demonstrates notable biological activities including inducing satiety, anorexia, weight loss, and hyperlocomotion in rat models. Its binding affinities to various serotonin receptors, including 5-HT1A, 5-HT1D, 5-HT1C, and 5-HT2, make it valuable for research in appetite regulation and behavioral studies. -
(5-HT)3-receptor Antagonist
YM114 is a highly selective antagonist of the 5-HT3 receptor, demonstrating notable potency in inhibiting receptor activity. It has been shown to disrupt the Bezold-Jarisch reflex induced by 2-methyl-5-HT without affecting bradycardia resulting from Veratridine or electrical stimulation in anesthetized rats. This compound offers valuable insights into cardiovascular and neuropharmacological research applications, particularly in understanding the role of 5-HT3 receptors in vagal afferent nerve signaling. -
5-HT2B Inhibtor
EGIS-7625 is a selective competitive inhibitor of the 5-HT2B receptor, exhibiting pKi values of 9.0 for 5-HT2B, and 6.2 and 7.7 for 5-HT2A and 5-HT2C, respectively. This compound has been shown to partially counteract m-chlorophenylpiperazine-induced hypomotility and hypophagia. EGIS-7625 is a valuable tool for investigating the role of 5-HT2B in various physiological and pathological processes, making it suitable for research in neuropharmacology and behavioral studies. -
5-HT1B/1D Receptor Agonist
Avitriptan is a selective agonist of the 5-HT1B and 5-HT1D receptors, exhibiting pKis of 7.44 for 5-HT1B in rats, 7.68 for 5-HT1B in humans, and 8.36 for 5-HT1D in humans. This compound induces vasoconstriction in isolated coronary arteries, suggesting its relevance in cardiovascular research. Avitriptan is primarily utilized in the treatment of migraines, providing insights into serotonergic pathways and their role in headache disorders. -
5-HT1A Receptor Agonist
Osemozotan hydrochloride is a selective 5-HT1A receptor agonist, known for its ability to modulate serotonin signaling. This compound has been shown to reduce the number of c-Fos-positive cells induced by MAMP in murine models, indicating its potential neuroprotective effects. Osemozotan hydrochloride is primarily utilized in research related to depressive disorders. -
5-HT2A Agonist
VU6067416 is a highly potent agonist of the 5-HT2A receptor, exhibiting an EC50 of 189 nM. Its ability to penetrate the blood-brain barrier makes it particularly valuable for neuropharmacological studies. This compound is useful for investigating the role of 5-HT2A receptor activation in various neurological and psychiatric disorders. -
5-HT2 Receptor Antagonist
Sergolexole maleate is a potent antagonist of the 5-HT2 receptor, which plays a crucial role in various serotonin-mediated physiological processes. This compound exhibits significant inhibitory effects on serotonin-enhanced platelet aggregation, making it relevant for research into cardiovascular function and platelet behavior. Its role in modulating serotonin activity positions Sergolexole maleate as a valuable tool for exploring mechanisms associated with mood disorders and thrombotic conditions. -
5-HT Receptor Antagonist
JNJ-18038683 free base is a potent antagonist of the 5-Hydroxytryptamine Type 7 (5-HT7) receptor, demonstrating pKis of 8.19 and 8.20 for rat and human 5-HT7 receptors, respectively, in HEK293 cell assays. This compound exhibits significant biological activity relevant for the investigation of psychiatric disorders and neuropharmacology. It serves as a valuable tool for researchers exploring the therapeutic potential of 5-HT7 receptor modulation. -
5-HT2C Agonist
5-HT2C agonist-4 is a selective agonist for the 5-HT2C receptor with an EC50 of 5.7 nM. This compound has demonstrated the ability to reduce locomotor activity in zebrafish larval models, making it a valuable tool for studies on neuropharmacology and behavior. Its use in research may facilitate investigations into the role of serotonin receptors in various physiological and pathological processes. -
5-HT2A Agonist
AC-90179 is a selective 5-HT2A receptor agonist, exhibiting a Ki value of 2.1 nM. This compound also acts as a 5-HT2C antagonist, suggesting its potential utility in the development of antipsychotic therapies. Its modulation of serotonergic signaling supports its application in investigating psychiatric disorders and related biological processes. -
5-HT Receptor
NAN-190 is a selective antagonist of the serotonin 5-HT receptor, primarily targeting the 5-HT1A subtype. It exhibits significant biological activity by blocking serotonin-mediated signaling, making it a valuable tool for investigating the role of serotonin in various physiological processes. NAN-190 is commonly utilized in research related to neuropharmacology and anxiety disorders, providing insights into the effects of serotonin modulation on behavior and mood regulation. -
5-HT1F Receptor Ligand
LY302148 is a partial agonist of the 5-HT1F receptor, demonstrating significant interaction with this target. In the [35S]GTPγS binding assay for human 5-HT1F receptors, it exhibits a potent EC50 value of 5.23 nM. This compound is of interest for research applications related to migraine pathophysiology and the potential development of therapeutic strategies. -
5-HT Receptor Agonist
VRX-03011 is a selective 5-HT receptor agonist that has shown promise in enhancing memory and modulating acetylcholine release in the hippocampus. This compound may influence APP metabolism, making it a valuable tool for research in neuropharmacology and cognitive function studies. Notably, VRX-03011 is associated with minimal gastrointestinal side effects, providing a safer alternative for in vivo applications. -
5HT1A Receptor Agonist
Piclozotan is a selective 5HT1A receptor agonist that has demonstrated potential in the treatment of motor complications associated with Parkinson's disease. By activating the 5HT1A receptor, Piclozotan may enhance dopaminergic transmission and alleviate symptoms in relevant preclinical models. This compound serves as a valuable tool for research into neurodegenerative disorders and the modulation of serotonergic pathways. -
5-HT1A Agonist
S-14671 is a potent agonist of the 5-HT1A receptor, exhibiting a high affinity with a pKi of 9.3. This compound plays a crucial role in the study of neurological disorders, particularly in the exploration of therapeutic strategies for anxiety and depression. Its specific targeting of the 5-HT1A receptor makes it a valuable tool for advancing research in neuropharmacology and related fields. -
5-HT4 Antagonist
SB 204070A is a selective antagonist of the 5-hydroxytryptamine receptor subtype 4 (5-HT4). It effectively inhibits 5-HT4 receptor activity, making it valuable for studies investigating serotonergic signaling pathways. Additionally, SB 204070A can be utilized to assess the functional roles of 5-HT4 receptors in various biological systems, contributing to research on gastrointestinal motility and cognitive function. -
5HT-4/5HT-3 Antagonist
Lintopride hydrochloride is a benzamide derivative that acts as a potent antagonist of the 5HT-4 receptor and exhibits moderate antagonistic effects on the 5HT-3 receptor. This compound enhances gastric emptying, stimulates antral and duodenal motility, and accelerates intestinal transit in preclinical models. Additionally, Lintopride hydrochloride significantly elevates the basal tone of the lower esophageal sphincter, making it valuable for research on gastrointestinal motility and related disorders. -
5-HT6 Receptor Antagonist
SB-773812 is a high-affinity antagonist of the serotonin 5-HT6 receptor, exhibiting a pKi of 8.1. Additionally, it demonstrates moderate to high affinity for dopamine receptors 2 and 3, with pKi values of 7.4 and 8.5, respectively. This compound is primarily used in research investigating central nervous system disorders, particularly those involving serotonin and dopamine signaling pathways. Its profile suggests potential applications in studying neuropharmacology and related therapeutic areas. -
5-HT1D Receptor Agonist
L 775,606 is a potent and selective agonist of the 5-HT1D receptor. This compound is primarily utilized in the investigation of migraine headache mechanisms and therapeutic approaches, demonstrating its significant role in modulating serotonergic signaling pathways relevant to headaches. Its specificity for the 5-HT1D receptor makes it an important tool in pharmacological research on migraine treatments. -
5-HT3/6 Receptor Antagonist
FPPQ is a dual-acting antagonist of the 5-HT3 and 5-HT6 receptors, demonstrating high affinity with Ki values of 0.9 nM and 3 nM, respectively. This compound exhibits significant antipsychotic and procognitive effects, making it a valuable tool for research into neuropsychiatric disorders. Its ability to modulate serotonergic signaling positions FPPQ as a promising candidate for studies focused on cognitive enhancement and the treatment of mental health conditions. -
5-HT2C Antagonist
FR260010 free base is a selective antagonist of the 5-HT2C receptor, exhibiting a Ki value of 1.1 nM. This compound is instrumental in research applications focused on elucidating the role of 5-HT2C receptors in various physiological and pathological processes, including anxiety and mood disorders. Its specificity makes it a valuable tool for investigating serotonergic signaling pathways and developing therapeutic strategies targeting the serotonergic system. -
5-HT1A receptor Agonist
CSP-2503 is a highly selective agonist of the 5-HT1A receptor, exhibiting an EC50 of 0.15 μM and a Ki value of 4.1 nM. This compound demonstrates significant selectivity against α1-adrenoceptors, 5-HT4 receptors, and benzodiazepine receptors, with Ki values exceeding 1000 nM. CSP-2503 reduces cAMP levels in vitro and displays anxiolytic effects in vivo, making it a valuable tool for investigating anxiety-related disorders. -
5-HT7 Antagonist
DR4485 hydrochloride is a selective antagonist of the 5-HT7 receptor, demonstrating a potent pKi of 8.14. This compound is utilized in various research applications focused on neuropharmacology and the modulation of serotonergic signaling pathways. Its oral bioavailability makes it a valuable tool for in vivo studies investigating the role of the 5-HT7 receptor in neurological disorders.
