Catalog No.
Product Name
Application
Product Information
Citations
-
5-HT1A Receptor Agonist
LY 293284 is a highly selective agonist of the 5-HT1A receptor. It demonstrates notable biological activity by inducing a significant reduction in core temperature and increasing food intake in cholestatic rats following bile duct resection. This compound is valuable for research applications focused on the modulation of serotonergic pathways and studying the effects of 5-HT1A receptor activation in various physiological conditions. -
5-HT7 Receptor Ligand
5-HT7 receptor ligand 1 is a selective ligand targeting the 5-HT7 receptor, exhibiting a Ki value of 8 nM. This compound demonstrates significant biological activity and has potential applications in neuropharmacology research, particularly in exploring serotonin signaling pathways. Additionally, 5-HT7 receptor ligand 1 shows low hepatotoxicity and a moderate potential for interaction with agents metabolized by CYP3A4 or CYP2D6, making it suitable for various experimental conditions. -
5-HT6 Receptor Antagonist
5-HT6R antagonist 2 is a selective antagonist of the 5-HT6 receptor, a G protein-coupled receptor involved in central nervous system processes. This compound exhibits potential to modulate neurotransmission and is utilized in research on neurological and psychiatric disorders, including depression and cognitive dysfunction. Its role in investigating the therapeutic effects of serotonin modulation makes it a valuable tool for exploring novel treatment strategies. -
5-HT Receptor
LP-20 hydrochloride functions as a ligand for the 5-HT7 receptor, a subtype of the serotonin receptor family. This compound selectively modulates serotonin signaling pathways and has implications in the study of neuropsychiatric disorders and circadian rhythms. LP-20 hydrochloride can be utilized in research exploring the therapeutic potential of 5-HT7 receptor antagonism or agonism, contributing to a deeper understanding of serotonin-related mechanisms. -
5-HT1B Receptor Antagonist
AZD1134 is a highly selective antagonist of the 5-HT1B receptor, demonstrating oral bioavailability and significant brain penetration. With IC50 values of 2.9 nM in humans and 0.108 nM in guinea pigs, AZD1134 effectively increases synaptic serotonin levels, indicating its potential in modulating serotonergic activity. This compound is particularly relevant for research into psychiatric disorders, including depression and anxiety. -
5-HT2A Receptor Antagonist
Iferanserin hydrochloride is a selective 5-HT2A receptor antagonist. It exhibits significant potential in alleviating symptoms associated with internal hemorrhoids, including bleeding and pruritus, as evidenced by ongoing Phase IIb clinical trials. This compound is valuable for research applications focusing on serotonin modulation and gastrointestinal disorders. -
5-HT7/5-HT2A Receptor Antagonist
5-HT7/5-HT2A receptor antagonist 1 is a high-affinity ligand targeting both the 5-HT7 and 5-HT2A receptors, demonstrating oral bioavailability and significant brain permeability with a pKi of 8.1. This compound functions as an antagonist in in vitro assays for the 5-HT2A receptor and as an inverse agonist for the 5-HT7 receptor. In vivo studies have shown that it effectively blocks 5-Carboxamidotryptamine (5-CT)-induced hypothermia in rats and DOI-induced head-twitches in mice, while it also occupies 5-HT2A receptor binding sites in the frontal cortex. 5-HT7/5-HT2A receptor antagonist 1 is suitable for investigating neuropharmacological disorders. -
5-HT Agonist
5-MeO-MET (5-Methoxy-N-methyl-N-ethyltryptamine) functions primarily as a 5-HT1A and 5-HT2A receptor agonist. This compound exhibits significant psychoactive properties, demonstrating sedative effects and inhibition of locomotor activity in murine models. Due to its influence on serotonergic pathways, 5-MeO-MET is valuable for research into the role of serotonin in behavior and potential therapeutic applications in studying mood disorders. -
5-HT7 Receptor Antagonist
SB 258719 hydrochloride is a selective antagonist of the 5-HT7 receptor, exhibiting high affinity with a pKi of 7.5. This compound is instrumental in the exploration of various biological pathways, particularly in cancer research and the study of neurological disorders. Its unique mechanism of action makes it a valuable tool for investigating the therapeutic potential of 5-HT7 receptor modulation in relevant disease models. -
5-HT3 Receptor Antagonist
Dehydro Palonosetron is a potent and selective 5-HT3 receptor antagonist known for its oral activity. It effectively inhibits the 5-HT3 receptor without influencing the functions of 5-HT1, 5-HT2, or 5-HT4 receptors. This compound is widely utilized in research applications focusing on the management of nausea and vomiting, particularly in chemotherapy settings. Its specific targeting makes it a valuable tool for studies exploring serotonergic modulation in various physiological and pathological contexts. -
5-HT Receptor Agonist
(rac)-AL-37350A is a potent agonist of the 5-HT2 receptor, known for its ability to lower intraocular pressure. With a high affinity and selectivity for this receptor, (rac)-AL-37350A demonstrates significant efficacy in reducing intraocular pressure in conscious hypertensive cynomolgus monkeys. This compound is valuable for research applications exploring glaucoma treatments and the physiological mechanisms of 5-HT receptor activation. -
5-HT7 Receptor Antagonist
Aramisulpride hydrochloride is a potent 5-HT7 receptor antagonist with a Ki value of 22 nM, demonstrating significant affinity for the D2 and D3 dopamine receptors as well, with Ki values of 140 nM and 13.9 nM, respectively. This compound is primarily utilized in psychiatric research to investigate the roles of serotonin and dopamine pathways in mental health disorders. Its unique pharmacological profile makes it a valuable tool for exploring therapeutic interventions and understanding neurobiological mechanisms. -
Rat 5-HT1B Antagonist
NAS-181 free base is a potent and selective antagonist of the rat 5-HT1B receptor, exhibiting a Ki value of 47 nM. This compound demonstrates a 13-fold selectivity for the rat 5-HT1B over the bovine 5-HT1B receptor, which has a Ki of 630 nM. NAS-181 free base effectively enhances serotonin turnover and increases synaptic serotonin levels by inhibiting the terminal rat 5-HT1B autoreceptors, making it a valuable tool for research in neuropharmacology and serotonergic signaling. -
5-HT2A Agonist
5-HT2A agonist 9 is a potent agonist of the 5-HT2A receptor, exhibiting an EC₅₀ of 34 nM. This compound plays a crucial role in research focusing on mental disorders and central nervous system pathologies. Its ability to selectively activate the 5-HT2A receptor makes it a valuable tool for investigating the mechanisms underlying neuropsychiatric conditions. -
5-HT Receptor Agonist
CGS-12066 maleate is a selective agonist for the 5-HT receptor family, specifically targeting 5-HT1A, 5-HT1B, 5-HT1C, and 5-HT1D receptors with pEC50 values of 6.41, 7.56, 4.05, and 7.11, respectively. This compound exhibits significant biological activity in modulating serotonergic signaling and has been utilized in research focused on neurological disorders. CGS-12066 maleate provides valuable insights into the pharmacological role of serotonin receptors in various neurophysiological processes. -
5-HT4 Receptor Agonist
RS 67506 hydrochloride is a selective agonist of the 5-HT4 receptor, which is involved in neurotransmitter signaling in the central nervous system. With a pKi value of 8.8 for the 5-HT4 receptor in guinea pig striatum, this compound demonstrates significant binding affinity. RS 67506 hydrochloride is primarily used in neurobiology research to explore the role of 5-HT4 receptors in modulation of neuronal function and potential therapeutic applications in neuropsychiatric disorders. -
5-HT2BR Antagonist
MW073 is a potent and selective antagonist of the 5-HT2B receptor, exhibiting an IC50 of 70 nM. This compound inhibits receptor activity and β-arrestin-1 recruitment in a concentration-dependent manner. MW073 has demonstrated the ability to improve synaptic plasticity and alleviate behavioral deficits, including aggression, in mouse models of Alzheimer’s disease. It is suitable for research applications focused on Alzheimer’s disease and related neurological conditions. -
5-HT1A Antagonist
GSK-958108 is a highly selective antagonist of the 5-HT1A receptor. This compound exhibits significant biological activity in modulating serotonin pathways, making it valuable for research into various neurological conditions and disorders. Its specificity allows for detailed investigations into the role of 5-HT1A receptors in neuropharmacology and behavioral studies. -
5-HT4 Agonist
Y-36912 is a highly selective agonist of the 5-HT4 receptor, with a binding affinity of Ki = 1.5 nM. This compound is known to accelerate gastric emptying and increase bowel frequency and stool weight. Y-36912 is a valuable tool for research applications related to gastrointestinal disorders. -
5-HT2C Agonist
5-HT2C agonist-10 is a potent 5-HT2C receptor agonist with an EC50 of less than 10 nM. This compound is utilized in the investigation of psychiatric disorders, contributing to the understanding of serotonergic signaling and its implications in mental health research. Its strong efficacy makes it valuable for studies aimed at developing new therapeutic strategies targeting the 5-HT2C receptor. -
5-HT6/5-HT2A Receptor Antagonist
5-HT6/5-HT2A receptor ligand-1 is a dual antagonist targeting the 5-HT6 and 5-HT2A receptors, exhibiting Ki values of 2 nM and 11 nM, respectively. This compound is useful for studying neurological and psychiatric disorders, providing valuable insights into the modulation of serotonergic signaling pathways. Its ability to selectively inhibit these receptors makes it a promising tool for research in related therapeutic areas. -
5-HT Receptor Antagonist
SB 714786 is a potent and selective antagonist of the 5-hydroxytryptamine 1D (5-HT1D) receptor. Engineered from a series of dual 5-HT1 receptor selective reuptake inhibitors, it represents the first highly potent compound targeting specifically the 5-HT1D subtype. With pKi values of 6.5, 6.7, 9.1, and 6.5 for 5-HT1A, 5-HT1B, 5-HT1D, and SerT receptors, respectively, SB 714786 exhibits remarkable selectivity for the 5-HT1D receptor while showing minimal intrinsic activity against other receptor subtypes. This specificity makes it a valuable pharmacological tool for investigating the role of 5-HT1D receptors in various biological contexts and potential therapeutic applications. -
5-HT2A Receptor Agonist
5-HT2A receptor agonist-12 is a potent agonist of the 5-HT2A receptor, exhibiting an EC50 value of less than 100 nM for h5-HT2A. This compound is ideal for studying serotonergic signaling pathways and their role in various physiological and pathological processes. It is widely utilized in neuropharmacological research to investigate the effects of 5-HT2A receptor activation on neurodevelopment, behavior, and potential therapeutic applications in psychiatric disorders. -
5-HT7 Receptor Agonist
AGH-107 is a highly selective agonist of the 5-HT7 receptor, demonstrating a Ki of 6 nM and an EC50 of 19 nM. It exhibits considerable brain penetration, along with high selectivity for the 5-HT7 receptor over related CNS targets. AGH-107 has also been shown to possess high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures, making it a valuable tool for studying serotonergic signaling and its implications in neuropsychiatric disorders. -
5-HT(2C) Inverse Agonist
Tenilapine is a potent inverse agonist of the 5-HT(2C) receptor, exhibiting significant binding affinity in both rat and human models. Its activity on this receptor can have implications in the research of various neuropsychological conditions. This compound is valuable for studies exploring the modulation of serotonin pathways and their impact on mood and anxiety disorders. -
5-HT7 Receptor Antagonist
Pellotine is an alkaloid that acts as an inverse agonist targeting the 5-HT7 receptor, exhibiting an EC50 of 291 nM. This compound also demonstrates significant affinity for the 5-HT1DR and 5-HT6R receptors, with Ki values of 117 nM and 170 nM, respectively. Pellotine effectively decreases intracellular cAMP levels, leading to reduced neuronal excitability and neurotransmitter release, making it a valuable tool for research into neuropharmacology and serotonergic signaling pathways. -
5-HT1a Receptor Agonist
5-HT1A agonist 1 is a highly selective agonist for the 5-HT1A receptor, exhibiting an EC50 of 0.18 nM. This compound mimics serotonin binding, facilitating postsynaptic membrane hyperpolarization, which inhibits neuronal hyperexcitability and decreases the release of anxiety-related neurotransmitters. 5-HT1A agonist 1 is a valuable tool in research focused on neuropsychiatric disorders. -
5-HT2C Receptor Agonist
PF-4522654 is a selective agonist of the 5-HT2C receptor, exhibiting a potent EC50 of 16 nM and a Ki of 8 nM. This compound demonstrates negligible functional activity at the 5-HT2A and 5-HT2B receptors, thereby ensuring specificity. PF-4522654 is employed in research focused on stress urinary incontinence (SUI), making it a valuable tool for exploring potential therapeutic approaches in this area. -
5-HT2C Receptor Agonist
PF-03246799 is a selective agonist of the 5-HT2C receptor, exhibiting an EC50 of 190 nM and a Ki of 160 nM. This compound demonstrates a preference for the 5-HT2C receptor over 5-HT2A and 5-HT2B receptors. PF-03246799 is utilized in research related to stress urinary incontinence (SUI), providing insights into potential therapeutic mechanisms for this condition. -
5-HT Activator
5-Fluoro-α-methyltryptamine hydrochloride is a potent 5-HT activator that enhances intracellular levels of serotonin (5-HT) and subsequently promotes its release. This compound demonstrates significant efficacy with EC50 values of 37 nM for dopamine (DA), 14 nM for serotonin (5-HT), 78 nM for norepinephrine (NE), and 8.47 nM for the 5-HT2A receptor. Its application in research includes studying serotonin-related pathways and neuropharmacological effects, making it valuable for investigations in behavioral science and psychiatric disorders. -
5-HT2A/5-HT2C Agonist
5-HT2A&5-HT2C agonist-3 is a selective agonist targeting the 5-HT2A and 5-HT2C serotonin receptors. This compound facilitates an increase in intracellular calcium levels in cells that overexpress these receptors, demonstrating a lack of activity on 5-HT2B receptors. Its unique pharmacological profile makes 5-HT2A&5-HT2C agonist-3 a valuable tool for investigating neuropsychiatric disorders, supporting research in serotonin signaling pathways and related therapeutic areas. -
5-HT1A,1B Receptor Agonist
Batoprazine is a potent agonist of the 5-HT1A and 5-HT1B receptors. It has demonstrated the ability to replicate the behavioral effects of eltoprazine in two-lever operant discrimination tests in rats, with an effective dose (ED50) of 0.20 mg/kg. This compound is valuable for research focused on serotonergic signaling and its implications in behavioral studies and pharmacological assessments. -
5-HT2AR Inhibitor
5-HT2AR-IN-1 is a potent inhibitor of the 5-hydroxytryptamine 2A receptor (5-HT2AR) with demonstrated antidepressant activity. It effectively reduces both 5-HT2AR expression and serotonin transporter (SERT) protein levels. This compound is suitable for research into central nervous system disorders, including depression and addiction-related conditions, highlighting its potential in investigating therapeutic strategies for these ailments. -
5-HT1C/2 Antagonist
Amesergide is a potent antagonist of serotonin receptors 5-HT1C and 5-HT2. This compound has been shown to reduce progeny body weight gains in maternal animal models. It is primarily utilized in research focused on depression and serotonergic signaling pathways. -
5-HT Receptor Antagonist
LY-426965 is a selective antagonist of the serotonin 1A receptor, demonstrating full antagonistic activity without partial agonist effects. This arylpiperazine compound has shown potential in preclinical studies for pharmacological applications related to serotonin dysregulation, including therapeutic strategies for smoking cessation and depression-related disorders. Its specificity and potency make it a valuable tool for research in neuropharmacology and behavioral studies. -
5-HT Receptor
LEK 8841 methanesulfonate is a selective antagonist of the 5-HT2 receptor, demonstrating notable gastrointestinal calming properties. It exhibits strong competitive antagonism towards 5-HT and norepinephrine, with pA2 values of 7.93 and 6.45, respectively. LEK 8841's superior selectivity compared to other antagonists makes it a valuable reference compound in receptor research. Additionally, studies on structural modifications indicate that LEK 8841 possesses a high affinity for 5-HT2 receptors while exhibiting minimal activity at alpha-adrenergic receptors, enhancing its potential for therapeutic applications in psychopharmacology. -
5-HT Receptor Antagonist
SB-224289 is a selective antagonist of the 5-HT1B receptor, primarily involved in the modulation of serotonin signaling pathways. Its antagonistic properties contribute to its anxiolytic effects, making it relevant in research focused on anxiety disorders and neuropharmacology. This compound serves as a valuable tool for studying serotonin-related pathways and the development of potential therapeutic interventions. -
5-HT6R Antagonist
AVN-322 free base is a selective antagonist of the 5-HT6 receptor, primarily involved in the modulation of neurotransmission in the central nervous system. This compound exhibits potential therapeutic effects in various neuropsychiatric disorders, making it a valuable tool for research in CNS disease mechanisms and drug development. Its oral activity enhances its versatility in experimental applications. -
5-HT6 Receptor Antagonist
GSK215083 is a potent antagonist of the 5-HT6 receptor, exhibiting high affinity for this target. This compound holds potential as a radioligand candidate for imaging studies when labeled with carbon-11 through methylation. Its application in neuropharmacological research may further elucidate the role of 5-HT6 in cognitive processes and related disorders. -
5-HT3 Receptor Antagonist
KB R6933 is a potent and selective antagonist of the 5-HT3 receptor, known for its oral bioactivity. This compound effectively inhibits serotonin-induced diarrhea but does not affect diarrhea triggered by castor oil or prostaglandin E2. Additionally, KB R6933 has been shown to mitigate bradycardia induced by serotonin, making it a valuable tool for research in gastrointestinal pharmacology and cardiovascular studies. -
5-HT2A Agonist
ECPLA is a highly potent 5-HT2A agonist, exhibiting an EC50 value of 14.6 nM for Gq-mediated calcium signaling. As an analog of lysergic acid diethylamide (LSD), it demonstrates significant affinity for various serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors. ECPLA is valuable for research applications focused on neuropharmacology, receptor signaling pathways, and the exploration of serotonin-related mechanisms. -
Human 5HT2A Receptor
Altanserin hydrochloride is a selective radioligand for the human 5-hydroxytryptamine receptor 2A (5-HT2A). This compound serves as a valuable tool for investigating the biochemical and cellular pathways associated with serotonergic signaling and its impact on neurochemical processes. Research applications include understanding the modulation of extracellular serotonin levels and studying the neurobiological mechanisms underlying various psychiatric disorders. -
5-HT Agonist
Paynantheine is an alkaloid primarily recognized for its agonistic activity at the 5-HT1A and 5-HT2B receptors. This compound exhibits notable antinociceptive properties, demonstrated by its ability to induce lower lip retraction in rodent models. Its mechanism of action makes Paynantheine a valuable tool for research into analgesic pathways and the modulation of serotonin receptors in pain studies. -
5-HT2A Antagonist
5-HT2A Antagonist 3 is a selective antagonist and inverse agonist of the 5-HT2A receptor with a pIC50 of 8.7 and a pKi of 9. This compound exhibits significant biological activity relevant to neurological research, providing insights into 5-HT2A receptor-mediated pathways and their implications in various neuropsychiatric disorders. It serves as a valuable tool in the study of serotonin receptor interactions and the development of therapeutic agents targeting these pathways. -
5-HT2A Agonist
4-Hydroxy DiPT hydrochloride is a selective 5-HT2A agonist, known for its ability to elicit the head-twitch response (HTR) in murine models, a key indicator of psychoactive effects. This compound is valuable for research applications focused on the serotonergic system and the investigation of psychotropic drug mechanisms. Its specific activity at the 5-HT2A receptor makes it a useful tool for studying neuropharmacology and related behavioral effects. -
5-HT2A Receptor Antagonist
Pruvanserin hydrochloride is a selective antagonist of the serotonin 5-HT2A receptor, exhibiting IC50 values of 0.35 nM and 1 nM for human and rat receptors, respectively. This compound is primarily utilized in scientific research focused on schizophrenia, aiding in the exploration of therapeutic strategies targeting serotonergic pathways. Its high selectivity and potency make it a valuable tool in the study of neuropsychiatric disorders associated with serotonin dysregulation. -
5-HT2A/2C Agonist
5-HT2A&5-HT2C agonist-1 selectively targets the serotonin receptors 5-HT2A and 5-HT2C, exhibiting IC50 values of 196 nM and 0.9 nM, respectively. This compound demonstrates significant agonistic activity, making it a valuable tool for investigating various neuropsychiatric conditions. Its applications extend to research on depression, addiction (including alcohol, tobacco, and cocaine), inflammation, cluster headaches, PTSD, seizure disorders, and other central nervous system disorders. -
5-HT Receptor Inhibitor
Citalopram hydrochloride is an orally active inhibitor of the 5-HT receptor, primarily functioning as a selective serotonin reuptake inhibitor (SSRI). This compound exhibits significant antidepressant activity and is widely utilized in research focused on depression and related mood disorders. Its mechanism aids in increasing serotonin levels in the synaptic cleft, making it a valuable tool for studying serotonin-related pathways and therapeutic interventions in psychiatric conditions. -
5-HT2c Receptor Antagonist
SB-247853 is a highly selective antagonist of the 5-HT2c receptor, which plays a crucial role in various physiological processes, including cardiovascular regulation. Research has demonstrated that SB-247853 can induce orthostatic intolerance during head-up tilting, highlighting its potential impact on cardiovascular responses. This compound is valuable for studying mechanisms underlying cardiovascular diseases and the role of serotonin receptor modulation in these conditions. -
5-HT2C Agonist
5-HT2C agonist-6 is a potent agonist of the 5-HT2C receptor, exhibiting an EC50 of 13.8 nM. This tricyclic compound functions as a psychedelic psychoplastogen, showing potential in the modulation of neuroplasticity. Its efficacy makes it a valuable tool for research into neurological disorders and related therapeutic applications.
