Catalog No.
Product Name
Application
Product Information
Citations
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5-HT3 Antagonist
Zacopride hydrochloride is a potent 5-HT3 receptor antagonist with a Ki value of 0.38 nM and a 5-HT4 receptor agonist with a Ki value of 373 nM. This compound demonstrates significant biological activities, including modulation of gastrointestinal motility, influence on cardiac function, and the potential to offer anxiolytic and antiemetic effects. Zacopride hydrochloride is primarily utilized in research related to gastrointestinal disorders, cardiovascular conditions, and psychiatric disorders such as anxiety. -
5-HT Uptake Inhibition
Gentisein (NSC 329491) is a potent inhibitor of serotonin uptake, demonstrating significant biological activity with an IC50 value of 4.7 µM. This compound serves as a valuable tool in neuropharmacological research, particularly in studies exploring serotonin-related pathways and their implications in mood disorders and neurobiology. Its role as a major metabolite of Mangiferin further emphasizes its relevance in investigations into natural product-derived pharmacological effects. -
5-HT1B/D Antagonist
SB-216641A is a selective antagonist of the 5-HT1B and 5-HT1D receptors. This compound exhibits high affinity and specificity for the human 5-HT1B receptor while demonstrating minimal activity at the 5-HT1D receptor. SB-216641A is utilized in research applications aimed at understanding serotonergic signaling and the modulation of neuropsychological disorders. Additionally, it has been shown to inhibit the function of SKF-99101H, providing insights into receptor interactions and pharmacological effects. -
5-HT2A Receptor Agonist
5-HT2A receptor agonist-3 specifically targets the 5-HT2A receptor with a binding affinity represented by a Ki value of 2.5 nM. This compound demonstrates 124-fold selectivity for the 5-HT2A receptor over the closely related 5-HT2C receptor. Due to its high selectivity and potency, 5-HT2A receptor agonist-3 is valuable for studying serotonergic signaling pathways and exploring therapeutic applications in neuropsychiatric disorders. -
5-HT2A Receptor Agonist
5-HT2A receptor agonist-1 is a selective agonist of the 5-HT2A receptor, exhibiting an EC50 of 5.54 nM. This compound is valuable for investigating the role of the 5-HT2A receptor in mood disorders, making it a useful tool in neuropharmacological research. Its specificity allows for in-depth studies of serotonin signaling pathways and their implications in various psychological conditions. -
D2 Receptor Inhibitor, D3 Receptor Inhibitor, 5-HT1A Receptor Inhibitor, 5-HT2B Receptor Inhibitor
Desmethyl cariprazine is a potent inhibitor of the D2 and D3 dopamine receptors, as well as the 5-HT1A and 5-HT2B serotonin receptors. It demonstrates a pEC50 of 8.90 at D2 receptors, 8.09 at D3 receptors, and 6.28 at 5-HT1A receptors, significantly inhibiting forskolin-induced cAMP production and serotonin-induced Ca2+ release. This compound is valuable for research focused on psychiatric disorders such as schizophrenia and bipolar disorder type I. -
5-HT1B/1D Receptor Agonist
Frovatriptan succinate hydrate is a selective agonist for the 5-HT1B and 5-HT1D receptors, exhibiting a pK50 value of 8.2. It demonstrates over 10-fold selectivity for these serotonin receptors compared to 5-HT1A, 5-HT1F, and 5-HT7, and exhibits greater than 1000-fold selectivity over other serotonin, dopamine, histamine H1, and α1-adrenoceptors. This compound is valuable for research into migraine pathophysiology and therapeutic applications. -
5-HT1A/1B/1D/5/7 Receptor Agonist
5-Carboxamidotryptamine maleate is a potent agonist of the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT5, and 5-HT7 serotonin receptors. This compound demonstrates significant biological activity in modulating serotonergic signaling pathways, making it valuable in neuropharmacological research. It is utilized in studies investigating the role of serotonin receptors in various physiological and pathological processes. -
5-HT1B Receptor Antagonist
GR 55562 hydrochloride is a selective antagonist of the 5-HT1B receptor. It is primarily utilized in research studying neurological disorders and the role of serotonin signaling in various pathophysiological conditions. This compound provides valuable insights into the therapeutic potential of modulating serotonergic pathways in neurobiological research. -
5-HT Receptor Binder
Altanserin is a selective binder for the 5-HT2 receptors, primarily utilized in neuropharmacological research. It demonstrates high affinity for these receptors, making it valuable for studying serotonergic signaling in the brain. This compound supports investigations into neuropsychiatric disorders and provides insights into receptor dynamics through imaging techniques. -
5-HT1/D2 Agonist
Sarizotan is a potent agonist of the serotonin 5-HT1A receptor and dopamine D2 receptor. It demonstrates high affinity with IC50 values of 0.1 nM for human 5-HT1A, 15.1 nM for rat D2, and 2.4 nM for human D4.2, among others. Its biological activity makes it suitable for research applications involving neuropharmacology and psychiatric disorders, contributing to the understanding of serotonergic and dopaminergic functions. -
5-HT2 Receptor Antagonist
Amperozide is a 5-HT2 receptor antagonist with a Ki value of 26 nM. This atypical antipsychotic exhibits low affinity for D2 receptors, making it a potential candidate for research into the modulation of serotonergic pathways. Amperozide is primarily used in studies related to neuropharmacology and behavioral research, particularly in the exploration of antipsychotic effects and serotonin receptor interactions. -
5-HT2B Receptor Antagonist
LY-272015 hydrochloride is a specific antagonist of the 5-HT2B receptor. It effectively inhibits ERK2 phosphorylation triggered by serotonin (5-HT) or BW723C86, highlighting its role in modulating signaling pathways associated with serotonin receptors. Additionally, this compound demonstrates antihypertensive properties in models of DOCA-salt-induced hypertension, making it a valuable tool for research in cardiovascular and neuropharmacological studies. -
5HT1B Receptor Agonist
CP 93129 dihydrochloride is a potent agonist of the 5HT1B receptor, known for its role in modulating serotonin signaling pathways. This compound is primarily utilized in research applications related to neurological disorders, including Parkinson's disease, to explore the impacts of serotonin receptor activation on motor control and neuroprotection. -
Dopamine/5-HT Modulator
Brilaroxazine is a potent multimodal modulator targeting dopamine (DA) and serotonin (5-HT) receptors. It acts as a partial agonist at DA D2, D3, and D4 receptors, and 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM) receptors, while exhibiting antagonist properties at 5-HT2B (Ki=0.19 nM) and 5-HT7 (Ki=2.7 nM) receptors. As an atypical antipsychotic, Brilaroxazine demonstrates promise in enhancing cognitive function in various neuropsychiatric and neurological conditions in vivo. -
5-HT4 Receptor Antagonist
RS 23597-190 is a selective antagonist of the 5-HT4 receptor, demonstrating high affinity for this target. It exhibits significant inhibitory effects on serotonin-induced tachycardia, making it valuable for cardiovascular research. Additionally, RS 23597-190 effectively inhibits superoxide production in high glucose conditions, highlighting its potential application in studies related to oxidative stress and metabolic disorders. -
5-HT1A Agonist
Xaliproden hydrochloride is a potent, selective agonist of the 5-HT1A receptor, demonstrating high affinity for specific binding sites in the rat hippocampus (IC50 = 3 nM). Additionally, it acts as a selective antagonist of the dopamine D2 receptor with moderate affinity (IC50 = 0.1-1 μM). Xaliproden hydrochloride exhibits significant anti-depressant and anti-anxiety effects, making it a valuable compound for investigating therapeutic approaches in neurodegenerative disease research. -
5-HT1D Receptor Agonist
PNU-142633 is a selective and orally bioavailable agonist of the 5-HT1D receptor, exhibiting a high affinity with a Ki of 6 nM for the human 5-HT1D receptor. In contrast, it demonstrates minimal interaction with the human 5-HT1B receptor, with a Ki value exceeding 18,000 nM. This compound is primarily utilized in research related to migraine therapy, showcasing its potential anti-migraine efficacy. -
Antipsychotic Agent
Melperone is a butyrophenone class compound that functions primarily as an atypical antipsychotic agent. It acts as a multireceptor antagonist, with binding affinities (Kd values) of 102 nM, 180 nM, 180 nM, and 150 nM for the 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. With lower binding affinity for histamine H1 and various serotonin receptors, Melperone also exhibits inhibitory effects on CYP2D6. This compound is valuable for research into schizophrenia and behavioral disturbances in elderly populations. -
5-HT2A Inverse Agonist
Remlifanserin is a potent inverse agonist of the 5-HT2A serotonin receptor. This compound demonstrates significant activity in modulating serotonin signaling pathways, making it valuable for research related to neuropsychiatric disorders. Its application includes studying the roles of 5-HT2A receptors in various biological processes, contributing to the understanding of mental health and potential therapeutic developments. -
5-HT1D Receptor Agonist
GR-46611 is a selective agonist for the 5-HT1D receptor. It plays a crucial role in modulating neurotransmission and is implicated in the research of bladder hyperactivity and leukemia. This compound is valuable for studies aiming to understand the mechanisms underlying these conditions and may contribute to the development of therapeutic strategies. -
Metabolite Of Cariprazine
Didesmethyl cariprazine is a metabolite of Cariprazine that acts as a partial agonist at D2 and D3 dopamine receptors while serving as a full agonist at the 5-HT1A receptor and an antagonist at the 5-HT2B receptor. With Ki values of 1.41 nM, 0.056 nM, 1.7 nM, and 0.52 nM for human D2L, human D3, human 5-HT1A, and human 5-HT2B, respectively, Didesmethyl cariprazine demonstrates significant interactions with these targets. This compound has been shown to dose-dependently inhibit the spontaneous activity of rat midbrain dopaminergic neurons, making it valuable for research in neuropharmacology and behavioral studies. -
5-HT2B/2C Receptor Antagonist
SB-200646A is a selective antagonist of the 5-HT2B and 5-HT2C receptors, exhibiting pKi values of 7.5 for 5-HT2B, 6.9 for 5-HT2C, and 5.2 for 5-HT2A, highlighting its specificity. This compound is orally active and demonstrates significant electrophysiological and anxiolytic effects in vivo, making it a valuable tool for research in neuropharmacology and the study of serotonin receptor-mediated pathways. -
Dopamine Receptor Antagonist
Nemonapride is a highly potent antagonist of the dopamine D2 receptor, exhibiting a Ki of 0.06 nM. Additionally, it activates the 5-HT1A receptor with an IC50 of 34 nM. This compound functions as an antipsychotic and efficiently crosses the blood-brain barrier, demonstrating significant neuroleptic effects in animal models. It is valuable for research focused on neuropharmacology and the mechanisms underlying psychiatric disorders. -
5-HT/SERT Inhibitor
Zimelidine dihydrochloride is a potent and selective inhibitor of serotonin uptake via the serotonin transporter (SERT). This compound exhibits significant antidepressant properties, making it valuable for research in the field of mood disorders and serotonin-related pathways. Its role in modulating serotonin levels can aid in the exploration of various neuropharmacological mechanisms. -
5-HT2C Receptor Agonist
(S)-Bexicaserin is a selective agonist of the 5-HT2C receptor, demonstrating potential therapeutic applications in the study of obesity and various psychiatric disorders. This compound plays a key role in modulating serotonin signaling, which may contribute to appetite regulation and mood stabilization. Researchers can utilize (S)-Bexicaserin to investigate its effects on metabolic pathways and neurobehavioral outcomes in relevant preclinical models. -
5-HT2C Receptor Agonist
Ro60-0175 is a highly selective agonist of the 5-HT2C receptor, known for its significant potency. This compound has been demonstrated to reduce self-administration, suggesting potential applications in addiction research and neuropharmacology. Ro60-0175 serves as a valuable tool for studying the physiological and behavioral effects mediated by the 5-HT2C receptor. -
5-HT Receptor Agonist
Geissoschizine methyl ether is a potent agonist of the 5-HT1A receptor, derived from the indole alkaloid profile of Uncaria hook. This compound exhibits notable psychotropic effects and is a key active component in the traditional herbal formulation Yokukansan. Its biological activity makes it a valuable reagent for research into serotonergic signaling and neuropharmacology. -
5-HT Receptor Agonist
5-Methoxytryptamine hydrochloride is a nonselective agonist of the 5-HT receptors, primarily involved in serotonin signaling. This compound, a metabolite of melatonin, demonstrates significant antioxidant properties and offers radioprotective effects. It serves as a valuable tool for studying serotonin-related pathways and assessing antioxidant mechanisms in various biological contexts. -
Stable Isotope
Chlorpromazine-d6 hydrochloride is a deuterated derivative of Chlorpromazine, primarily functioning as a dopamine receptor antagonist. This stable isotope is utilized in biochemical and pharmacological research to explore the interactions and mechanisms of action of antipsychotic agents. Its ability to inhibit serotonin receptors, potassium channels, and sodium channels makes it valuable for studying neuropharmacology and drug metabolism. -
5-HT Receptor Agonist
LY 165163 is a potent agonist of the 5-HT presynaptic receptor. It has been shown to significantly decrease 5-HTP accumulation while increasing DOPA levels in both the cortex and striatum. This compound is useful for studies related to neurotransmitter regulation and the modulation of serotonergic signaling pathways. Research applications include investigations into serotonin-related disorders and their effects on dopamine neurotransmission. -
5-HT Receptor Agonist
Flesinoxan is a potent and selective agonist of the 5-hydroxytryptamine 1A (5-HT1A) receptor, exhibiting an EC50 value of 24 nM. This compound functions primarily as a hypotensive agent and demonstrates significant anxiolytic and antidepressant properties. It is primarily utilized in research applications investigating anxiety, depression, and related mood disorders. -
5-HT1α/ α2-adrenergic Antagonist
Spiroxatrine is a selective dual antagonist of the 5-HT1α and α2-adrenergic receptors, exhibiting Ki values of 3.94 nM for 5-HT1α, 224,000 nM for 5-HT1β, and 118.5 nM for 5-HT2. This compound demonstrates notable sedative effects, making it relevant for research into anxiety and depressive disorders. Spiroxatrine is valuable for studies exploring the modulation of serotonergic and adrenergic signaling pathways. -
5-HT1A Receptor Agonist
F 13714 fumarate is a selective 5-HT1A receptor agonist known for its antidepressant-like properties. It has been shown to exhibit significant efficacy in murine models of chronic mild stress following a single administration. This compound is valuable for research applications related to mood disorders and the neuropharmacology of serotonin receptors. -
5-HT Receptor Antagonist
Bemesetron is a selective 5-HT3 receptor antagonist with a reported IC50 of 0.33 nM. It exhibits neuroprotective effects, making it a valuable tool in research focused on neuropharmacology and gastrointestinal disorders. This compound can be utilized in studies examining serotonin modulation and its implications in various disease models. -
5-HT1B/1D-Receptor Agonist
Almotriptan is a selective agonist of the 5-HT1B/1D receptors. It is primarily utilized in the study of migraine pathophysiology and the pharmacological management of migraine attacks. This compound's specific action on serotonin receptors enables researchers to investigate its effects on vasodilation and neurotransmission related to migraine episodes. -
5-HT2A Serotonin Receptor Agonist
IHCH-7113 is a selective agonist of the 5-HT2A serotonin receptor, demonstrating significant antidepressant activity. This compound shows potential in the investigation of antipsychotic agents and their mechanisms of action. Its ability to modulate serotonergic signaling makes it a valuable tool in neuropharmacological research. -
5-HT2 Agonist
α-Methylserotonin maleate is a potent and selective agonist of the 5-HT2 receptor. This serotonin analogue, derived from α-Methyltryptophan, effectively mediates lymphatic smooth muscle contraction and inhibits the up-regulation of serotonin receptor-mediated phosphoinositide hydrolysis. Its key biological activity makes it valuable for research applications involving serotonergic signaling and smooth muscle physiology. -
5-HT2A Receptor Antagonist
Eplivanserin hemifumarate is a potent and selective antagonist of the 5-HT2A receptor, exhibiting an IC50 of 5.8 nM in rat cortical membranes and a Kd of 1.14 nM. It demonstrates greater than 20-fold selectivity for the 5-HT2A subtype over 5-HT2B and 5-HT2C receptors. This compound is valuable for research focused on neuropharmacology and the modulation of serotonergic pathways in various biological processes. -
5-HT2B Receptor Antagonist
5-HT2B antagonist-1 is an orally active antagonist of the 5-HT2B receptor, exhibiting an IC50 value of 33.4 nM. This compound is useful for investigating the role of 5-HT2B receptor signaling in various pathologies, including hepatocellular carcinoma, cardiovascular disorders, and gastrointestinal diseases. It provides a valuable tool for researchers studying the therapeutic potential of targeting 5-HT2B receptors in disease models. -
5-HT2 Receptor Antagonist
Cinanserin hydrochloride is a potent and selective antagonist of the 5-HT2 receptor, exhibiting a binding affinity with a Ki of 41 nM. This compound demonstrates a much higher selectivity for the 5-HT2 receptor compared to the 5-HT1 receptor, which has a Ki value of 3500 nM. Additionally, Cinanserin hydrochloride inhibits the 3C-like proteinase of the severe acute respiratory syndrome coronavirus, effectively reducing viral replication in vitro. This dual functionality makes it a valuable tool for research in neuropharmacology and virology. -
5-HT2 Serotonin Receptor Antagonist
Pirenperone is a selective antagonist of the 5-HT2 serotonin receptor. It demonstrates modest anxiolytic activity, making it a valuable tool for investigating anxiety-related disorders. Its unique pharmacological profile positions it for research applications in neuropharmacology and the study of serotonin-mediated pathways. -
5-HT Receptor Modulator
Eltoprazine hydrochloride is a potent modulator of the 5-HT receptor family, functioning as an agonist for both 5-HT1A and 5-HT1B receptors while acting as an antagonist at 5-HT2C receptors. This compound has demonstrated significant antiaggressive and anxiogenic effects, making it a valuable tool for research into neuropharmacology and the treatment of anxiety-related disorders. Its unique mechanism of action allows for exploration into the therapeutic potential for various psychiatric conditions. -
5-HT4R Agonist
Velusetrag is a potent and selective agonist of the serotonin 5-HT4 receptor (5-HT4R), demonstrating a pKi of 7.7. It exhibits minimal affinity for 5-HT2A and 5-HT2B receptors, ensuring a specific receptor interaction. This compound is primarily utilized in research related to gastrointestinal disorders and Parkinson's disease, contributing to the understanding of serotonergic modulation in these conditions. -
5-HT1A/1B Antagonist
l-Pindolol is a reversible, competitive antagonist of the 5-HT1A and 5-HT1B receptors, exhibiting partial agonistic activity at β-adrenoceptors. This compound is primarily utilized in research investigating neurological diseases, due to its ability to modulate serotonergic signaling pathways. Its pharmacological properties make it a valuable tool in the study of various neuropharmacological effects. -
5-HT1D/5-HT1B Receptor Antagonist
GR127935 is a selective antagonist for the 5-HT1D and 5-HT1B receptors, exhibiting a pKi of 8.5 for both isoforms. This compound demonstrates a significant 100-fold selectivity for the 5-HT1B and 5-HT1D receptors over 5-HT1A, 5-HT2A, and 5-HT2C receptors. GR127935 is primarily utilized in research focused on neurological disorders, aiding in the exploration of serotonergic signaling pathways. -
5-HT1A Agonist
Gepirone hydrochloride is a selective 5-HT1A receptor agonist. By binding specifically to the 5-HT1A receptor, Gepirone exhibits antidepressant activity, making it relevant for research in anxiety and major depressive disorder. Its mechanistic profile provides valuable insights into serotonergic signaling and potential therapeutic approaches in psychiatric disorders. -
5-HT2C Receptor Modulator
VA012 is a positive allosteric modulator of the serotonin 5-HT2C receptor. It is shown to effectively reduce food intake and prevent body weight gain in preclinical models, without inducing central nervous system-related side effects during subchronic administration. This compound is valuable for research applications focused on obesity and metabolic disorders. -
5-HT4R Agonist
Velusetrag hydrochloride is a selective agonist of the serotonin 5-HT4 receptor (5-HT4R) with a reported pKi of 7.7, demonstrating potent activity in modulating serotonin pathways. This compound shows negligible affinity for 5-HT2A and 5-HT2B receptors (Ki > 10 μM), making it suitable for specific therapeutic investigations. Velusetrag hydrochloride is particularly relevant for research into gastrointestinal disorders and Parkinson's disease, contributing to the understanding and potential treatment of these conditions. -
Dopamine Receptor Antagonist
LE 300 is a potent and selective antagonist of the dopamine D1-like receptors, demonstrating inhibition constants (Kis) of 1.9 nM and 7.5 nM for human dopamine D1 and D5 receptors, respectively. Additionally, LE 300 acts as an antagonist of the 5-HT2A receptor, with a pA2 value of 8.32 in rat tail artery assays. This compound is valuable for research into dopamine receptor signaling pathways and neuropharmacology.
