Catalog No.
Product Name
Application
Product Information
Citations
-
5-HT Receptor Agonist
8-OH-DPAT hydrobromide is a potent and selective 5-HT1A receptor agonist with a high pIC50 of 8.19. This compound demonstrates exceptional selectivity, being nearly 1000 times more selective for the 5-HT1A subtype compared to other serotonin receptor subtypes. It is primarily utilized in neuropharmacological research to investigate serotonin-mediated signaling pathways and to explore its effects on various neurological conditions. -
5-HT1A Agonist
Gepirone is a selective 5-HT1A agonist that binds specifically to the 5-HT1A receptor binding site. Its primary biological activity includes acting as an antidepressant, making it a valuable tool in research related to anxiety and major depressive disorders. Gepirone can be utilized to explore the underlying mechanisms of these conditions and aid in the development of new therapeutic strategies. -
5-HT2A Receptor Antagonist
Lumateperone is a potent 5-HT2A receptor antagonist with a Ki of 0.54 nM, exhibiting dual action as a partial agonist of presynaptic D2 receptors and an antagonist of postsynaptic D2 receptors (Ki = 32 nM). Additionally, it modulates dopamine D1 receptors. This compound demonstrates significant antipsychotic properties and supports research in schizophrenia and bipolar depression, while also presenting potential anticancer activity. -
5-HT Receptor Agonist
2-Methyl-5-HT is a selective agonist for the 5-HT3 receptor. This compound exhibits significant biological activity, particularly in demonstrating anti-depressive-like effects in preclinical models. It is utilized in research to explore serotonergic pathways and contribute to studies on mood regulation and anxiety disorders. -
5-HT Receptor Agonist
Bretisilocin is a selective agonist for the 5-HT2A receptor and functions as a serotonin releaser. This compound demonstrates significant antidepressant activity, making it an important tool for the investigation of depression and related neuropsychiatric disorders. Its role in modulating serotonin pathways provides valuable insights into the underlying mechanisms of mood regulation and potential therapeutic approaches. -
5-HT3 Receptor Agonist
SR 57227A is a potent, orally active selective agonist of the 5-HT3 receptor, capable of crossing the blood-brain barrier. This compound exhibits binding affinities (IC50) ranging from 2.8 to 250 nM for 5-HT3 receptor sites in rat cortical membranes and NG 108-15 cell membranes. SR 57227A is primarily utilized in research focused on neuropharmacology and has demonstrated potential anti-depressant effects. -
5-HT Uptake Inhibitor
Norfluoxetine hydrochloride is a potent 5-HT uptake inhibitor, serving as an active N-demethylated metabolite of Fluoxetine. It inhibits serotonin reuptake and has been shown to inhibit CaV3.3 T current with an IC50 of 5 μM. Due to its mechanism of action, Norfluoxetine hydrochloride is relevant in research focusing on mood disorders and anticonvulsant activity, providing insights into serotonin modulation and potential therapeutic applications. -
5-HT4 Receptor Agonist
RS 67333 hydrochloride is a selective partial agonist of the 5-HT4 receptor, demonstrating a pKi of 8.7 in guinea pig striatum. This compound exhibits lower affinities for various other receptors, including 5-HT1A, 5-HT1D, 5-HT2A, 5-HT2C, dopamine D1, D2, and muscarinic M1-M3 receptors. RS 67333 hydrochloride is known for its neuroprotective properties, making it a valuable tool for research in Alzheimer's disease and related neurodegenerative disorders. -
5-HT Receptor Agonist
CP94253 hydrochloride is a selective agonist of the 5-HT1B receptor, demonstrating a Ki value of 2 nM in radioligand binding assays. It exhibits lower affinity for other serotonin receptor subtypes, with Ki values of 89 nM for 5-HT1A, 49 nM for 5-HT1D, 860 nM for 5-HT1C, and 1600 nM for 5-HT2. This compound is known for its central activity when administered systemically in vivo, making it valuable for research in neuropharmacology and the study of serotonin-related pathways. -
5-HT3 Agonist
m-CPBG hydrochloride is a selective agonist of the 5-HT3 receptor, influencing serotonin signaling pathways. It has demonstrated potential in research related to neurological diseases, allowing for the investigation of serotonin's role in various neurophysiological processes. This compound is valuable for studies aiming to elucidate the mechanisms underlying anxiety, depression, and other psychiatric conditions. -
5-HT Receptor Agonist
TCB2 is a potent agonist of the serotonin 5-HT2A receptor. It demonstrates significant activation of this receptor, crucial for mediating various psychological and physiological responses. TCB2 is utilized in research exploring the role of 5-HT2A activation in neuropsychiatric disorders and receptor signaling pathways. -
5-HT7 Receptor Antagonist
SB 258719 is a selective antagonist of the 5-HT7 receptor, exhibiting a high affinity with a pKi value of 7.5. This compound demonstrates significant potential in the research of various neurological disorders and cancer. Its targeted mechanism allows for the exploration of 5-HT7 receptor signaling pathways, contributing to a deeper understanding of their role in these diseases. -
5-HT2C Receptor Agonist
(Rac)-WAY-161503 is a selective agonist of the 5-HT2C receptor, exhibiting a Ki of 4 nM and an EC50 of 12 nM. This compound demonstrates significantly higher affinity for the 5-HT2C receptor compared to the 5-HT2A and 5-HT2B receptors. Due to its biological activity, (Rac)-WAY-161503 is valuable for research applications aimed at understanding obesity and depressive disorders. -
5-HT2C Receptor Antagonist
RS-102221 hydrochloride is a selective antagonist of the 5-HT2C receptor, exhibiting a Ki value of 10 nM. This compound demonstrates approximately 100-fold selectivity over the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride has been shown to stimulate the differentiation of new nerve cells and is associated with increased food intake and weight gain in rodent models, making it a useful tool for research in neurobiology and appetite regulation. -
5HT4 Agonist
Mosapride is a selective 5HT4 agonist known for its gastroenterokinetic properties. This compound enhances gastrointestinal motility and is used in research related to gastrointestinal diseases. Additionally, Mosapride acts as a CYP inducer and exhibits a concentration-dependent inhibitory effect on Kv4.3 with an IC50 value of 15.2 μM. Its pharmacological profile makes it a valuable tool for investigating gut-related disorders. -
Dopamine/5-HT2A Antagonist
Paliperidone palmitate is a competitive antagonist of dopamine D2 and 5-hydroxytryptamine 2A (5-HT2A) receptors with the capability to cross the blood-brain barrier. By binding to these receptors, it modulates the activity of dopamine and serotonin, thereby exerting antipsychotic effects. This compound is primarily utilized in research related to schizophrenia and other neuropsychiatric disorders, contributing to the understanding of antipsychotic mechanisms and therapeutic strategies. -
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. -
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.
