Catalog No.
Product Name
Application
Product Information
Citations
-
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. -
Antihypertensive Agent
Pelanserin is an orally active antihypertensive agent that primarily functions as a potent 5-HT2 receptor antagonist. It effectively inhibits α-adrenergic receptor activity, showcasing an ED50 value of 0.03 μg/mL. Additionally, Pelanserin demonstrates vasodilatory properties with an ED100 of 5 μg. This compound is valuable for research applications focused on hypertension, proving effective in hypertensive rodent models and renal hypertensive dog breeds. -
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. -
Antipsychotic Agent
Melperone hydrochloride is a butyrophenone that functions primarily as an atypical antipsychotic agent. It acts as a multireceptor antagonist, demonstrating binding affinities with Kd values of 102 nM for 5-HT2A, 180 nM for dopamine D2, 180 nM for α1-adrenergic, and 150 nM for α2-adrenergic receptors. While exhibiting weaker interactions with additional receptors, Melperone hydrochloride shows potential as a CYP2D6 inhibitor. This compound is utilized in research for investigating schizophrenia and managing agitation in elderly populations. -
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. -
Mixed Agonist/Antagonist
2-(2-Methoxyphenoxy)ethylamine hydrochloride acts as a mixed agonist and antagonist, primarily targeting the 5-HT1A receptor as a partial agonist and the α1-adrenergic receptor as an antagonist. This reagent exhibits significant potential in studying neurological disorders, particularly in relation to anxiety, depression, and psychosis. Its dual mechanism of action makes it valuable for exploring therapeutic avenues in mental health research. -
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. -
5-HT2C Receptor Agonist
ASP-2205 is a potent agonist of the 5-HT2C receptor, with an EC50 of 0.85 nM for the human receptor and 2.5 nM for the rat receptor. This compound enhances the pudendal nerve-mediated urethral closure reflex, making it a valuable tool for research into therapies for urinary incontinence. ASP-2205 may be instrumental in studying the physiological roles of the 5-HT2C receptor in urogenital function and related disorders. -
α1/5-HT2 Receptor Antagonist
SGB-1534 hydrochloride is a selective and competitive antagonist of the alpha 1-adrenoceptor and the 5-HT2 receptor. This compound demonstrates the ability to inhibit vasoconstriction, resulting in lowered blood pressure, making it a valuable tool in cardiovascular research. SGB-1534 hydrochloride is particularly relevant for investigating conditions such as hypertension and other related cardiovascular diseases. -
5-HT7 Antagonist
SB 258741 is a selective antagonist of the 5-HT7 receptor, exhibiting a high affinity with a pKi of 8. This compound has demonstrated significant potential in studying serotonin-related pathways, making it valuable for research focused on mood disorders and other neuropsychiatric conditions. Its specificity for the 5-HT7 receptor allows for targeted investigations into receptor signaling and therapeutic applications. -
5-HT1A Partial Agonist
BMS-442606 is an orally active 5-HT1A partial agonist that exhibits significant affinity for the serotonin receptor. Its biological activity positions it as a valuable tool for research focused on generalized anxiety disorder (GAD). BMS-442606 is instrumental in exploring the therapeutic potential of 5-HT1A modulation in anxiety-related conditions. -
5-HT6/5-HT2A Receptor Antagonist
5-HT6/5-HT2A receptor ligand-2 is a potent dual antagonist of the 5-HT6 and 5-HT2A receptors, demonstrating Ki values of 25 nM and 32 nM, respectively. This compound exhibits pro-cognitive properties, making it a valuable tool for research in neuroscience and psychiatric disorders. Its ability to penetrate the blood-brain barrier enhances its potential applications in studying cognitive function and related therapeutics. -
5-HT Receptor Agonist
PRX933 is a selective agonist of the 5-HT2C receptor. It exhibits significant biological activity related to appetite regulation and may provide insights into the pathophysiology of obesity and glaucoma. This compound is valuable for research aimed at elucidating the role of serotonin receptors in metabolic disorders and ocular health. -
D2 Receptor/5-HT Receptor Anagonist
Flumezapine is a potent antagonist of the dopamine D2 receptor and the 5-hydroxytryptamine (5-HT) receptor. This compound has demonstrated the ability to inhibit conditioned avoidance responses in rodent models while maintaining a low risk of extrapyramidal side effects. Flumezapine is valuable in antipsychotic research, particularly in studies exploring the modulation of dopaminergic and serotonergic pathways without altering cortisol levels induced by κ-opioid receptor agonists. -
5-HT1D/1B Agonist
5-Benzyloxytryptamine is a selective partial agonist of the 5-hydroxytryptamine 1D/1B (5-HT1D/1B) receptors, exhibiting an IC50 of 40 nM for bovine caudate 5-HT1D, with significantly lower affinity for 5-HT2 receptors (IC50 > 470 nM). This compound effectively inhibits adenylate cyclase, leading to a decrease in neurotransmitter release and downregulation of cAMP signaling. 5-Benzyloxytryptamine is valuable for the study of neurotransmitter imbalance-related disorders, particularly in research related to migraines. -
D2 Receptor Agonist
(Rac)-Rotigotine serves as a dopamine D2 receptor agonist, exhibiting a multifaceted mechanism of action. It is recognized as a full agonist at dopamine receptors and a partial agonist at the 5-HT1A receptor, while also functioning as an antagonist of the α2B-adrenergic receptor, demonstrating Ki values of 0.71 nM for dopamine D3 and 4-15 nM for D2, D5, D4, and dopamine D1 receptors. This compound is primarily utilized in research focused on neurological disorders, particularly in the context of Parkinson's disease and other dopamine-related pathologies. -
5-HT6R Antagonist
5-HT6R antagonist 5 is a potent competitive antagonist of the 5-HT6 receptor, exhibiting an IC50 value of 4.19 nM. This compound is instrumental in the exploration of central nervous system disorders, as well as in studies related to cognitive and neurodegenerative diseases. Its ability to modulate 5-HT6R signaling makes it a valuable tool for investigating therapeutic strategies in these challenging conditions. -
5-HT1A Receptor Partial Agonist
Adatanserin is a selective partial agonist of the 5-HT1A receptor, exhibiting a high affinity with a Ki value of 1 nM. Additionally, it acts as a moderate-affinity antagonist at the 5-HT2 receptor with a Ki of 73 nM. This compound demonstrates pronounced anxiolytic and antidepressant effects in preclinical animal models, making it a valuable tool for research in anxiety and mood disorders. -
5-HT1A Agonist and D2/3 Antagonist
Adoprazine hydrochloride functions as a full agonist at the 5-HT1A receptor, demonstrating a high affinity with a pEC50 of 9 in cloned human receptors. Additionally, it acts as a full antagonist at D2 and D3 receptors, with pA2 values of 9.3 and 8.9, respectively. This compound showcases properties characteristic of atypical antipsychotics, making it relevant for research in neuropharmacology and the treatment of psychiatric disorders. -
5-HT3 receptor antagonist
Indisetron dihydrochloride is a selective antagonist of the 5-HT3 receptor, primarily known for its anti-emetic properties. This compound effectively mitigates nausea and vomiting by blocking the action of serotonin at these receptors. It is widely utilized in research settings to study the mechanisms of nausea and to develop therapies for emesis-related conditions. -
5-HT2A Agonist
Jimscaline is a potent 5-HT2A receptor agonist and a structural analog of mescaline. It is primarily employed in neurological research to investigate the role of serotonin receptors in various neurophysiological processes. Its ability to modulate 5-HT2A activity makes it a valuable tool for studying psychiatric disorders and related pathways. -
Stable Isotope
(Rac)-Rotigotine-d3 hydrochloride is a deuterium-labeled analog of (Rac)-Rotigotine, primarily acting as a full agonist at dopamine receptors. It also serves as a partial agonist of the 5-HT1A receptor and acts as an antagonist at the α2B-adrenergic receptor, showcasing Ki values of 0.71 nM, 4-15 nM, and 83 nM for the respective targets. This stable isotope is vital for pharmacokinetic studies, isotope labeling experiments, and research related to neuropharmacology. -
5-HT4 Agonist
Prucalopride hydrochloride is a selective and specific agonist for the 5-HT4 receptor, with high affinity identified by pKis of 8.6 and 8.1 for the human 5-HT4a and 4b subtypes, respectively. This compound enhances intestinal motility by facilitating the regeneration of the intestinal nervous system, as demonstrated in rodent models. Additionally, Prucalopride hydrochloride exhibits anticancer properties through the inhibition of the PI3K/AKT/mTOR signaling pathway. Its applications are relevant in research focused on chronic constipation, pseudo-intestinal obstruction, and cancer. -
5-HT Receptor Ligand
5-HT1A modulator 4 is a potent ligand for the 5-HT receptors, specifically targeting the 5-HT1A subtype with a Ki value of 2.18 μM. Additionally, it demonstrates activity at the 5-HT2A receptor with a Ki value of 19.7 μM. This compound is valuable for research applications related to neuropharmacology, particularly in studying the role of serotonin receptors in mood regulation and various neurological disorders.
