Catalog No.
Product Name
Application
Product Information
Citations
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5-HT2B Receptor Agonist
(+)-Norfenfluramine hydrochloride is a selective agonist of the 5-HT2B receptor, exhibiting a Ki value of 11.2 nM. This compound effectively stimulates the hydrolysis of inositol phosphates and enhances intracellular calcium levels. Its biological activity makes it a valuable tool for studies related to primary pulmonary hypertension and valvular heart disease. -
Rat 5-HT1B Antagonist
NAS-181 dimesylate is a selective antagonist of the rat 5-HT1B receptor, exhibiting a Ki value of 47 nM. With a notable 13-fold selectivity for the r5-HT1B receptor compared to the bovine equivalent (Ki=630 nM), NAS-181 effectively enhances serotonin (5-HT) turnover and improves synaptic 5-HT concentration by blocking terminal r5-HT1B autoreceptors. This compound is valuable for research involving serotonin modulation and related neuropharmacological studies. -
5-HT Receptor Inhibitor
Ansofaxine hydrochloride is a potent triple reuptake inhibitor that targets the serotonin, dopamine, and norepinephrine transporters. It demonstrates inhibition with IC50 values of 723 nM for serotonin, 491 nM for dopamine, and 763 nM for norepinephrine. This compound is primarily used in research to investigate the mechanisms underlying mood disorders and has potential applications in studies focused on neuropharmacology and the treatment of depression and anxiety. -
β-arrestin-biased 5-HT2AR Agonist
IHCH-7086 is a partial β-arrestin-biased agonist of the 5-HT2A receptor, exhibiting a Ki value of 12.59 nM, and capable of crossing the blood-brain barrier. This compound has demonstrated effectiveness in blocking D-lysergic acid diethylamide-induced head-twitch responses in murine models and alleviating depression-like behaviors in mice subjected to acute restraint stress or corticosterone administration. IHCH-7086 is particularly relevant for research focused on depression and related neuronal signaling pathways. -
α/β-Adrenergic Receptor Blocker
Arotinolol is a nonselective α/β-adrenergic receptor blocker that also acts as a vasodilating β-blocker. It exhibits significant inhibitory activity against the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is primarily utilized as an antihypertensive agent in the management of various cardiovascular conditions, as well as for certain non-cardiovascular diseases, facilitating research in cardiovascular pharmacology and receptor interaction studies. -
Dopamine Receptor Antagonist
2-Bromo-LSD (BOL-148; Bromolysergide) is a potent dopamine receptor antagonist specifically targeting dopamine neurons in the substantia nigra and neostriatum. It enhances the hydroxylation of tyrosine within the striatum and mitigates the reduction of Apomorphine-induced DOPA accumulation. Additionally, 2-Bromo-LSD inhibits 5-HT receptor-mediated DOPA formation, making it valuable for research on neurotransmitter regulation and potential therapeutic applications in neuropharmacology. -
5HT4 Agonist
Mosapride citrate dihydrate is a 5-HT4 receptor agonist that serves as a gastroprokinetic agent. It enhances gastrointestinal motility by selectively stimulating upper gastrointestinal function. Additionally, Mosapride demonstrates a concentration-dependent inhibition of Kv4.3 channels, with an IC50 value of 15.2 μM, making it valuable in research related to various gastrointestinal disorders. -
5-HT Agonist
Quipazine is a potent 5-HT3 receptor agonist, exhibiting a Ki value of 1.4 nM for the displacement of [3H]GR65630 from the receptor in rat models. In addition to its central nervous system applications, Quipazine demonstrates antiviral activity against SARS-CoV-2, with an EC50 of 31.64 μM. This compound is valuable for investigating neurological diseases and understanding serotonergic signaling pathways. -
5-HT1D/5-HT1B Receptor Antagonist
GR127935 hydrochloride is a potent antagonist of the 5-HT1D and 5-HT1B receptors, demonstrating pKis of 8.5 for both isoforms. It exhibits a significant 100-fold selectivity for the 5-HT1B and 5-HT1D receptors compared to other serotonin receptor subtypes, including 5-HT1A, 5-HT2A, and 5-HT2C. This compound is valuable for research involving neurological diseases and exploring serotonin receptor dynamics. -
5-HT7 Agonist
LP44 hydrochloride is a selective agonist of the 5-HT7 receptor, exhibiting a Ki value of 0.22 nM. This compound induces a dose-dependent hypothermic response when administered via intracerebroventricular injection, although it does not elicit significant hypothermia when given intraperitoneally. LP44 hydrochloride is valuable for studying the physiological roles of 5-HT7 receptors and their potential therapeutic applications in neurological research. -
5-HT2B Receptor Agonist
(+)-Norfenfluramine is a selective agonist of the 5-HT2B receptor, with a binding affinity (Ki) of 11.2 nM. This compound effectively stimulates the hydrolysis of inositol phosphates, resulting in enhanced intracellular calcium levels. (+)-Norfenfluramine is utilized in research focused on primary pulmonary hypertension and valvular heart disease, providing insight into pathology and potential therapeutic avenues. -
5-HT1A Modulator
5-HT1A modulator 2 hydrochloride is a selective modulator of the serotonin 5-HT1A receptor, demonstrating a Ki value of 53 nM for 5-HT1A binding. This compound is primarily utilized in research related to neuropharmacology and psychiatric disorders, providing insights into serotonin signaling pathways. Its modulation of the 5-HT1A receptor makes it a valuable tool for studying anxiety, depression, and other mood-related conditions. -
5-HT7 Receptor Agonist
AS19 is a highly potent and selective agonist of the 5-HT7 receptor, with an IC50 value of 0.83 nM and a Ki of 0.6 nM. It demonstrates significant selectivity over other serotonin receptors, including 5-HT1A, 5-HT1B, 5-HT1D, and 5-HT5A, with Kis values ranging from 6.6 nM to 490 nM. AS19 has been shown to enhance memory consolidation and effectively reverse amnesia induced by Scopolamine or Dizocilpine, making it a valuable tool for research in cognitive function and neuropharmacology. -
GlyT2/5HT2A Antagonist
Opiranserin hydrochloride is a dual antagonist targeting glycine transporter type 2 (GlyT2) and serotonin receptor 2A (5HT2A), exhibiting IC50 values of 0.86 and 1.3 μM, respectively. In addition, it demonstrates antagonistic activity on recombinant P2X3 receptors with an IC50 of 0.87 μM. This compound is under development as an injectable analgesic for postoperative pain management, making it relevant for research in pain pathways and therapeutic interventions. -
5-HT Modulator
13,14-Dihydro-15-keto-PGE2 functions as a 5-HT modulator, playing a crucial role in the serotonergic pathway. This compound has been demonstrated to alleviate opioid-induced constipation by modulating gastrointestinal activity through the action on 5-HT receptors. It is valuable in research applications related to gastrointestinal motility and the management of opioid side effects. -
Dopamine D2/5-HT2A Receptor Antagonist
Spiperone hydrochloride is a potent antagonist of dopamine D2 and 5-HT2A receptors, exhibiting Ki values of 0.06 nM and 1 nM, respectively. In addition, it selectively antagonizes the α1B-adrenoceptor and activates calcium-activated chloride channels (CaCC). This compound has demonstrated significant antipsychotic and anti-inflammatory properties, making it a valuable tool for research in neuropharmacology and inflammation studies. -
5-HT2A receptor Antagonist
Pruvanserin is a selective antagonist of the 5-HT2A receptor, demonstrating significant potential in modulating serotonergic pathways. This compound has been shown to alleviate tactile allodynia in diabetic rat models, indicating its usefulness in pain research. Additionally, Pruvanserin is being explored for its applications in studying insomnia and related sleep disorders. -
5-HT2C Receptor Antagonist
SB 243213 is a selective and high-affinity antagonist of the 5-HT2C receptor, exhibiting a pKi of 9.37 and a pKb of 9.8 for the human receptor. This compound demonstrates over 100-fold selectivity against a variety of neurotransmitter receptors, enzymes, and ion channels. SB 243213 shows an improved anxiolytic profile, making it a potential candidate for research applications related to schizophrenia and motor disorders. -
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.
