Catalog No.
Product Name
Application
Product Information
Citations
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5-HT1A Receptor Agonist
(R)-LY-41 is a selective agonist of the 5-HT1A receptor. It is known to effectively reduce the accumulation of 5-hydroxytryptophan in the rat brain induced by decarboxylase inhibitors, thereby influencing serotonin synthesis. This compound can also lower body temperature in rats and inhibit escape responses, contributing to the induction of the 5-HT behavioral syndrome, albeit with less potency compared to its S-enantiomer. (R)-LY-41 is an important reagent for research into neurological disorders, particularly depression and anxiety. -
5-HT2 Agonist
5-HT2 Agonist-1 is a potent agonist of the 5-HT2A, 5-HT2B, and 5-HT2C serotonin receptors, exhibiting IC50 values of 10 nM, 8.3 nM, and 1.6 nM, respectively. This compound is valuable for investigating a range of biological activities associated with central nervous system disorders, including depression, substance use disorders such as alcoholism and cocaine addiction, inflammation, cluster headaches, PTSD, and seizure disorders. Researchers can employ 5-HT2 Agonist-1 to deepen their understanding of the serotonergic system and its implications in various neuropsychiatric conditions. -
5-HT Receptor
Azasetron, a 5-HT3 receptor antagonist, is an effective antiemetic agent. It is primarily utilized to prevent postoperative nausea and vomiting as well as nausea induced by chemotherapy. Importantly, Azasetron does not interfere with neutrophil chemotaxis or phagocytosis, nor does it scavenge superoxide anions or hydrogen peroxide produced by cell-free systems, making it a valuable tool in various research applications related to antiemetic efficacy. -
5-HT Agonist
LY334370 fumarate is a selective agonist for the 5-HT1F receptor, exhibiting a Ki value of 1.6 nM. This compound is utilized in research to investigate its role in modulating serotonin signaling pathways and assessing potential therapeutic applications in neurological disorders. Its specific action on the 5-HT1F receptor makes it a valuable tool for studies focused on migraine treatment and other serotonin-related conditions. -
5-HT2A Inverse Agonist
5-HT2A inverse agonist-1 is a potent inverse agonist of the 5-HT2A receptor, exhibiting an IC50 of 5.5 nM. This compound demonstrates minimal inhibition of hERG channels, making it a valuable tool in pharmacological research. Its application spans the investigation of neurological diseases, including Parkinson’s disease, facilitating the study of receptor signaling pathways and potential therapeutic interventions. -
5-HT1A Agonist
U92016A hydrochloride is a selective agonist of the 5-HT1A receptor, demonstrating high intrinsic activity. It exhibits strong binding affinity to human 5-HT1A receptors, with a Ki of 0.2 nM when expressed in Chinese hamster ovary cells. This compound is suited for research applications investigating serotonin signaling pathways and has potential implications in the study of anxiety and depression-related disorders. -
5-HT Receptor Antagonist
LY-426965 hydrochloride is a selective antagonist of the serotonin 1A receptor. This arylpiperazine compound exhibits potent antagonistic properties, distinguishing itself with no partial agonist activity. Preclinical studies indicate its potential application in addressing disorders linked to serotonin dysregulation, including smoking cessation and depression-related conditions. -
5-HT6 Receptor Antagonist
SUVN-507 is a selective antagonist of the 5-HT6 receptor, known for its role in modulating cognitive functions. This compound has demonstrated potential to reverse cognitive impairments and enhance excitatory neural transmission, while reducing inhibitory signaling. SUVN-507 is a valuable tool for research into neurological disorders, particularly in the context of Alzheimer's disease and other cognitive dysfunctions. -
5-HT Receptor Antagonist
Methiothepin (Metitepine; Ro 8-6837) is a potent, non-selective antagonist of the 5-HT receptors, primarily targeting 5-HT2A, 5-HT2B, and 5-HT2C. It exhibits high affinity with pKi values of 8.50, 8.68, and 8.35 for these receptors, respectively. Methiothepin's antagonistic properties make it valuable for research in neuropharmacology, particularly in studies exploring serotonin signaling pathways and their implications in various mood disorders and psychotic conditions. -
5-HT2 Agonist
ALEPH hydrochloride is a partial agonist of the 5-HT2A and 5-HT2B receptors, exhibiting EC50 values of 10.3 nM and 19.2 nM, respectively. This compound induces a head twitch response in mice, with an ED50 of 0.80 mg/kg. ALEPH hydrochloride is suitable for research applications investigating serotonin receptor functions and their roles in neuropharmacology. -
5-HT3 Serotonin Receptor Agonist
Amanozine is a potent agonist of the 5-HT3 serotonin receptor, playing a critical role in mediating serotonin signaling within the nervous system. This compound exhibits potential therapeutic applications in the study of various neurological disorders, making it a valuable tool for research in psychopharmacology and neuropharmacology. Its ability to influence serotonin receptor activity could provide insights into the mechanisms underlying mood regulation and anxiety. -
5-HT4 Receptor Antagonist
GR125487 sulfamate is a selective antagonist of the 5-HT4 receptor, which plays a significant role in various cognitive and gastrointestinal functions. This compound effectively inhibits cognitive enhancement, making it valuable for researching memory disorders, mood disorders, gastrointestinal dysfunctions, and urinary tract issues. Its oral bioactivity allows for convenient administration in preclinical studies. -
5-HT(1B/1D) Receptor Agonist
Naratriptan-d3 hydrochloride is a selective agonist of the 5-HT1B/1D receptors. This deuterium-labeled derivative exhibits effective vasoconstrictive properties on cranial arteries through activation of these receptors, with an EC50 value of 0.11 μM observed in dog basilar arteries. Additionally, it is known to inhibit trigeminal nerve-mediated dural neurogenic plasma extravasation and mitigate sterile inflammation. Naratriptan-d3 hydrochloride is primarily utilized in research focusing on acute migraine, particularly related to cranial vascular dynamics and neuroinflammatory responses. -
5-HT2A/D2 Antagonist
Blonanserin dihydrochloride is a potent antagonist of the 5-HT2A and dopamine D2 receptors, exhibiting Ki values of 0.812 nM and 0.142 nM, respectively. This compound is primarily utilized as an atypical antipsychotic agent and is relevant for research focused on extrapyramidal symptoms, sedation levels, and hypotensive effects. Its pharmacological profile makes it a valuable tool in the study of neuropsychiatric disorders and related therapeutic interventions. -
5-HT2 Receptor Agonist
CYB210010 is a long-acting agonist of the serotonin 5-HT2 receptors, specifically targeting the 5-HT2A and 5-HT2C subtypes (EC50: 4.1 nM and 7.3 nM, respectively). This compound is orally bioavailable and capable of penetrating the central nervous system, leading to a notable head twitch response (HTR) without the development of behavioral tolerance following chronic administration. Its selectivity and consistent biological activity make CYB210010 a valuable tool for research into the roles of serotonin receptors in various neuropsychiatric conditions. -
5-HT1F Receptor Agonist
LY334370 hydrochloride is a highly selective agonist of the 5-HT1F receptor, demonstrating a binding affinity with a Kd value of 0.446 nM. This compound exhibits noteworthy anti-migraine activity, making it valuable for research in migraine pathophysiology and treatment exploration. Its mechanism of action highlights the therapeutic potential of targeting the serotonergic system in neurological disorders. -
5-HT Deamination Inhibitor
RS 2232 is a competitive inhibitor of 5-hydroxytryptamine (5-HT) deamination, demonstrating a Ki of 0.054 μM. This compound selectively and reversibly inhibits type A monoamine oxidase, making it a valuable tool in neurological research. RS 2232 is utilized to gain insights into the role of serotonin metabolism in various brain functions and disorders. -
5-HT6 Receptor Agonist
ST1936 is a selective agonist of the 5-HT6 receptor, exhibiting nanomolar affinity with a Ki value of 13 nM for human 5-HT6 receptors. It also demonstrates notable selectivity across related serotonin receptors, with Ki values of 168 nM for 5-HT7 and 245 nM for 5-HT2B. Additionally, ST1936 has moderate affinity for human and rat α2 adrenergic receptors, with a Ki of 300 nM. This compound is valuable for neuroscience research, particularly in studies related to cognitive function and mood disorders. -
5-HT2 Antagonist
Spiramide is a potent and selective antagonist of the 5-HT2 receptor and dopamine D2 receptor, demonstrating Ki values of 2 nM and 3 nM, respectively. It exhibits over 2000-fold selectivity for the 5-HT2 receptor compared to the 5-HT1C receptor (Ki = 4300 nM). Due to its pharmacological properties, Spiramide is valuable for research applications in the fields of neuropharmacology and the study of antipsychotic mechanisms. -
5-HT2 Receptor Antagonist
(S)-Mirtazapine is a stereoselective antagonist of the 5-HT2 receptor, showing significant pronociceptive effects in animal models of acute thermal nociception. This S(+)-enantiomer exhibits distinct pharmacological properties, contributing to its potential applications in pain research and neuropharmacology. Additionally, (S)-Mirtazapine is metabolized by CYP2D6 and CYP1A2, which may influence its therapeutic efficacy and safety profile. -
5-HT6/5-HT2A Antagonist
Landipirdine is a potent antagonist of the 5-HT6 and 5-HT2A receptors. This orally active compound is primarily investigated for its potential therapeutic effects in the context of Parkinson's disease. Its mechanism of action provides a valuable tool for researchers exploring receptor interactions and neuropharmacology related to neurodegenerative conditions. -
5HT4 Receptor Agonist
Renzapride is a full agonist of the 5-HT4 receptor, exhibiting a Ki value of 115 nM. Additionally, it acts as an antagonist at both the 5-HT2b and 5-HT3 receptors. This compound is primarily utilized in research focusing on constipation-predominant irritable bowel syndrome (C-IBS), making it valuable for exploring therapeutic interventions in gastrointestinal disorders. -
5-HT1A Receptor Agonist
Lauroscholtzine, also known as N-Methyllaurotetanine, acts as an agonist of the 5-HT1A receptor. This natural alkaloid is known for its modulatory effects on serotonergic signaling, making it a valuable tool for studying the role of serotonin in various physiological processes. Its biological activity is relevant for research into neuropharmacology, particularly in the context of anxiety and depression-related disorders. -
5-HT Receptor Antagonist
Seganserin is a potent orally active antagonist of the 5-HT receptor, exhibiting a plasma half-life of 26.1 ± 12.9 hours. This compound plays a crucial role in neurological research, offering insights into serotonin-mediated pathways and their implications in various neuropsychiatric conditions. Its selectivity for the 5-HT receptor makes it a valuable tool for exploring serotonin receptor signaling and pharmacology. -
5-HT Receptor Antagonist
Dolasetron Mesylate hydrate is a serotonin 5-HT3 receptor antagonist that primarily functions by blocking the action of serotonin at these receptors. This compound is widely utilized in research focused on understanding and mitigating chemotherapy-induced nausea and vomiting. Its efficacy in targeting the 5-HT3 receptor makes it a valuable tool in pharmacological studies related to antiemetic therapy. -
5-HT Receptor Control
2C-B-FLY hydrochloride is a selective 5-HT receptor agonist, functioning primarily on the serotonin receptor system. This compound exhibits significant hallucinogenic properties, making it valuable for research into psychoactive mechanisms and the modulation of serotonergic pathways. Its unique structure as a dihydrodifuran analog of 4-bromo-2,5-dimethoxyphenethylamine (2C-B) enhances its potential applications in behavioral and neuropharmacological studies. -
5-HT2 Receptor Antagonist
Cyproheptadine is a selective antagonist of the 5-HT2A receptor, exhibiting both antidepressant and antiserotonergic properties. In addition to its central nervous system effects, Cyproheptadine demonstrates antiplatelet and thromboprotective activities. This compound is valuable for research applications focused on thromboembolic disorders, contributing to the understanding of related vascular conditions. -
5-HT2/D1/D2 Antagonist
Olanzapine-d3 is a deuterated form of olanzapine, targeting multiple receptors, including serotonin receptors 5-HT2A, 5-HT2C, and dopamine receptors D1 to D4. This selective and orally active monoaminergic antagonist exhibits high affinity binding with Ki values ranging from 4 to 57 nM for relevant targets. It is primarily utilized in research related to psychopharmacology and the treatment of schizophrenia and bipolar disorder, enabling detailed pharmacokinetic studies and investigation of receptor interactions. -
5-HT2/D1/D2 Antagonist
Olanzapine hydrochloride is a selective antagonist of serotonin receptors (5-HT2A/2C, 5-HT3) and dopamine receptors (D1, D2). It exhibits high affinity binding to various targets, including H1, muscarinic M1-5, and adrenergic α1 receptors, contributing to its pharmacological profile. This atypical antipsychotic is primarily used in research focusing on neuropharmacology, the treatment of schizophrenia, and mood disorders, providing valuable insights into the modulation of neurotransmitter systems. -
5-HT Receptor Modulator
1-(1-Naphthyl)piperazine hydrochloride is a potent modulator of the 5-HT receptor system, functioning as an agonist at the 5-HT1A receptor while antagonizing the 5-HT2A receptor. This compound has demonstrated significant biological activity by inducing apoptosis in various cell types. Additionally, it exhibits potential in combatting immunosuppression and preventing photocarcinogenesis, making it a valuable tool for research in neuroscience and cancer studies. -
5-HT Receptor Modulator
1-(1-Naphthyl)piperazine is a modulator of the 5-HT receptors, functioning as an antagonist at the 5-HT2A receptor and an agonist at the 5-HT1A receptor. It demonstrates a binding affinity for the human 5-HT6 receptor with a Ki value of 120 nM. Additionally, 1-(1-Naphthyl)piperazine has been shown to inhibit forskolin-stimulated adenylate cyclase activity in calf substantia nigra, and it mitigates UV-induced immunosuppression. This compound induces S-phase cell cycle delay and apoptosis while elevating ROS levels, ultimately leading to the inhibition of MNT-1 cell proliferation, making it a valuable tool for melanoma research. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine mesylate is an orally active tricyclic antihistamine and anti-5-HT agent that exhibits significant activity against decerebrate rigidity, demonstrating minimal sedative and soporific effects. This compound effectively reduces or eliminates the influence of both static and dynamic fusimotor activity on muscle spindles in decerebrate models. Dimethothiazine mesylate is relevant for research applications related to hemicrania and spasticity. -
5-HT Receptor Agonist
8 Hydroxy PIPAT oxalate is a selective agonist of the 5-HT1A receptor. This compound activates serotonergic signaling pathways, promoting the degranulation of enteric mast cells and enhancing spontaneous histamine release in both guinea pig and human intestinal preparations. Its ability to modulate histamine release suggests potential applications in understanding and addressing functional gastrointestinal disorders, including irritable bowel syndrome. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine is a tricyclic antihistamine and anti-5-HT agent primarily targeting histamine receptors and serotonin pathways. It exhibits significant activity against decerebrate rigidity with minimal sedative and soporific effects. This compound effectively modulates fusimotor activity on muscle spindles in decerebrate models, making it a valuable reagent for studying conditions such as hemicrania and spasticity. -
5-HT Receptor Antagonist
AVN-101 is a potent 5-HT7 receptor antagonist with a Ki of 153 pM, demonstrating significant brain penetration and oral bioavailability. It also interacts with 5-HT6, 5-HT2A, and 5-HT2C receptors, exhibiting Ki values of 2.04 nM, 1.56 nM, and 1.17 nM, respectively. Additionally, AVN-101 has a high affinity for histamine H1 and adrenergic α2A, α2B, and α2C receptors, with Ki values ranging from 0.41 to 3.6 nM. This compound is suitable for research related to general anxiety disorders, depression, schizophrenia, Alzheimer’s disease, and multiple sclerosis. -
5-HT2A/ Histamine H1 Receptor Antagonist
LY2624803 is a potent antagonist of the 5-HT2A and histamine H1 receptors. This compound exhibits significant biological activity in modulating serotonergic and histaminergic signaling pathways, making it valuable for research in neuropharmacology. LY2624803 is particularly relevant for studies investigating mood disorders, anxiety, and other conditions associated with dysregulated serotonin and histamine receptor activity. -
Antihistamine/Anti-5-HT Agent
Dimethothiazine hydrochloride is an orally active tricyclic antihistamine and anti-5-HT agent. It exhibits notable efficacy against decerebrate rigidity, demonstrating minimal sedative and soporific effects. This compound has been shown to diminish or eliminate the influence of fusimotor activity on the muscle spindle in decerebrate cats. Dimethothiazine hydrochloride is valuable for research on hemicrania and spasticity. -
5-HT Receptor Antagonist
Asenapine citrate is a 5-HT receptor antagonist that exhibits potent activity against serotonin receptors (pKi: 8.4-10.5), adrenoceptors (pKi: 8.9-9.5), dopamine receptors (pKi: 8.9-9.4), and histamine receptors (pKi: 8.2-9.0). This atypical antipsychotic compound is primarily utilized in research focusing on schizophrenia and bipolar disorder, helping to elucidate the mechanisms of these neuropsychiatric conditions. -
H2 Histamine Receptors/ α2-AR/5-HT2(B,C) Serotonin Receptors Ligand
Platelet aggregation-IN-3 is a ligand for H2 histamine receptors, α2-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. This compound effectively inhibits platelet aggregation induced by ADP and collagen and modulates tumor cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 shows potential for applications in antiplatelet therapy for cardiovascular diseases and in the prevention of cancer-related thrombosis and tumor metastasis. -
5-HT Receptor Inhibitor
Proxibarbal is a barbiturate derivative that acts as a selective inhibitor of the 5-HT receptor. It demonstrates notable anti-anxiety properties and is utilized in research focused on migraine headache mechanisms. This compound serves as a valuable tool for understanding serotonergic pathways and their implications in anxiety and migraine disorders. -
5-HT6R Antagonist
PUC-10 is a potent antagonist of the 5-HT6 receptor, exhibiting a Ki value of 14.6 nM and an IC50 of 32 nM. Computational studies indicate that PUC-10 is orally bioactive and capable of penetrating the blood-brain barrier. This compound effectively induces autophagy in SH-SY5Y neuronal cells by inhibiting the mTOR signaling pathway. PUC-10 is ideally suited for studies focused on neurological disorders and related therapeutic strategies. -
5-HT Reuptake Inhibitor
Mesembrine, also known as (+)-Mesembrine, is a potent inhibitor of the 5-HT transporter with a Ki value of 1.4 nM. This alkaloid, characterized by its aryloctahydroindole structure, also inhibits phosphodiesterase 4B (PDE4B) with an IC50 of 7.8 μM. Due to its selective targeting of serotonin reuptake, Mesembrine is valuable for studies related to mood regulation and various neuropsychiatric disorders, as well as investigations into PDE4B's role in inflammatory processes. -
CGRP Receptor Antagonist/5-HT1F Receptor Agonist
PCC0105005 is a potent CGRP receptor antagonist, exhibiting an IC50 of 1.01 nM, coupled with partial agonist activity at the 5-HT1F receptor, with an EC50 of 77.91 nM. This compound demonstrates significant efficacy in preclinical migraine models, effectively reducing the expression levels of CGRP and c-Fos proteins and inhibiting ERK and CREB phosphorylation. PCC0105005 is suitable for research focused on migraine pathophysiology and potential therapeutic interventions. -
5-HT2A Regulator
2-Bromo-LSD D-Tartrate is a selective 5-HT2A receptor partial agonist and competitive antagonist. It exhibits significant biological activity, displaying an EC50 of 0.81 nM for Gq dissociation and a KB of 0.18 nM, making it a valuable tool for studying serotonergic signaling pathways. Additionally, it promotes dendritogenesis and spinogenesis while effectively reversing the behavioral impacts of chronic stress in animal models, enhancing active coping behaviors. This compound is suitable for research involving neurological and behavioral studies related to serotonin modulation. -
5-HT2A/5-HT2C Receptor Agonist
DOI hydrochloride is a potent agonist of the serotonin 5-HT2A and 5-HT2C receptors, exhibiting Ki values of 0.7 nM and 2.4 nM, respectively, while also targeting the 5-HT2B receptor with a Ki of 20 nM. This compound effectively crosses the blood-brain barrier, making it valuable for neurological research. DOI hydrochloride has been shown to induce head twitches in murine models, providing insight into its psychotropic effects and facilitating the study of serotonergic signaling pathways. -
5-HT2B Agonist
BW-723C86 is a selective agonist of the 5-HT2B receptor, demonstrating significant anxiolytic-like effects. In animal models, it has been shown to induce hyperphagia and decrease grooming behavior in rats. Additionally, BW-723C86 exhibits the ability to dilate pulmonary arteries and inhibit gastric accommodation following liquid meal intake, making it a useful reagent for research into anxiety, appetite regulation, and gastrointestinal physiology. -
5-HT4 Receptor Antagonist
GR 113808 is a potent and highly selective antagonist of the 5-HT4 receptor, exhibiting a pKb of 8.8. It demonstrates substantial selectivity, being 300-fold more effective against the 5-HT4 receptor compared to 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2C, and 5-HT3 receptors. This compound is widely utilized in research applications focusing on gastrointestinal motility and cognitive function related to serotonin signaling pathways. -
5-HT2B Antagonist
SB 204741 is a selective high-affinity antagonist of the 5-HT2B receptor, exhibiting a pKi value of 7.1. This compound is utilized in research exploring the role of 5-HT2B in various physiological and pathological processes. Its antagonistic properties make it valuable for studies on cardiac function, pulmonary effects, and potential therapeutic interventions in diseases related to serotonergic dysregulation. -
5-HT Biosynthesis Inhibitor
4-Chloro-L-phenylalanine is a potent inhibitor of serotonin (5-HT) biosynthesis, acting as a nonspecific antagonist of the tryptophan hydroxylase isoforms TPH1 and TPH2. This compound is valuable for studying serotonin-related pathways and their implications in psychiatric and neurological disorders. It serves as an important tool for researchers investigating the regulation of serotonin levels and the biochemical basis of 5-HT modulation. -
5-HT2C Receptor Agonist
Bexicaserin is a selective agonist of the 5-HT2C receptor, primarily involved in the regulation of appetite and mood. This compound demonstrates potential therapeutic applications in the study of obesity and psychiatric disorders, such as epilepsy. Its unique mechanism of action makes it a valuable tool for researchers investigating the role of serotonin receptors in these conditions.
