Catalog No.
Product Name
Application
Product Information
Citations
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5-HT2C Receptor Antagonist
RS-102221 is a selective antagonist of the 5-HT2C receptor, exhibiting a Ki value of 10 nM. This compound demonstrates significant selectivity, being nearly 100-fold more effective against the 5-HT2C receptor compared to the 5-HT2A and 5-HT2B receptors. RS-102221 has been shown to promote the differentiation of new nerve cells and is associated with increased food intake and weight gain in rat models, making it a valuable tool for research in neurobiology and metabolic studies. -
5-HT Receptor Antagonist
SB-656104 is a potent antagonist of the 5-HT7 receptor, exhibiting a pKi of 8.70. It effectively inhibits 5-carboxamidotryptamine (5-CT)-stimulated adenylyl cyclase activity, thereby modulating serotonergic signaling pathways. This compound is valuable for research investigations into the role of 5-HT7 receptors in neuropsychiatric disorders and related pharmacological studies. -
Antidepressant Agent
Etoperidone hydrochloride is an orally active antagonist of serotonin and norepinephrine reuptake, primarily functioning as an antidepressant agent. It exhibits Kd values of 36 nM for the 5-HT2 receptor, 38 nM for the α1-adrenergic receptor, 85 nM for the 5-HT1A receptor, and 570 nM for the α2-adrenergic receptor. This compound is utilized in research focused on mood disorders and the neurochemical pathways related to depression. -
5-HT2C Agonist
VER-3323 is an oral-active agonist of the 5-HT2C receptor, classified as an indoline analog. It effectively reduces food intake in rat models by inducing swallowing dysfunction, while demonstrating no significant alteration in energy expenditure due to thermogenesis or physical activity. This compound is valuable for research focused on obesity and appetite regulation. -
5-HT1B Antagonist
Isamoltan hydrochloride is a selective antagonist of the 5-HT1B receptor, exhibiting an IC50 value of 39 nM for the inhibition of [125I]ICYP binding to 5-HT1B recognition sites in rat brain membranes. Additionally, it acts as a β-adrenoceptor ligand with an IC50 of 8.4 nM. This compound demonstrates anxiolytic activity and is valuable in research exploring anxiety-related disorders and serotonergic signaling pathways. -
5-HT1A Agonist
R-137696 is an orally active agonist of the serotonin-1A (5-HT1A) receptor, known for its ability to induce relaxation in the proximal stomach. This compound is a valuable tool for research focusing on functional dyspepsia and related gastrointestinal disorders, facilitating the exploration of therapeutic strategies targeting serotonin pathways. -
CB1 Antagonist
LY320135 is a potent and selective antagonist of the cannabinoid receptor type 1 (CB1) with a Ki of 141 nM. It also exhibits binding affinity for 5-HT2 and muscarinic receptors, with Kis of 6.4 μM and 2.1 μM, respectively. This compound demonstrates neuroprotective effects and is useful in studies related to neurodegeneration and cannabinoid signaling pathways. -
5HT6R Antagonist
AVN-211 is a selective and orally bioavailable antagonist of the 5HT6 receptor, demonstrating an IC50 of 2.34 nM and a Ki of 1.09 nM. This compound exhibits a remarkable 5K-fold selectivity for the 5HT6 receptor over a range of 65 other receptors, enzymes, and ion channels. AVN-211 has been shown to significantly enhance cognitive functions and reduce anxiety-related behaviors in various animal models of Alzheimer's disease, making it a valuable tool for research into Alzheimer's dementia. -
5-HT Receptor Agonist/Dopamine Receptor Antagonist
SDZ 208-912 is a dual-action compound functioning as a 5-HT1A/2 receptor agonist and a dopamine D1 receptor antagonist. It demonstrates partial dopamine agonism along with atypical neurosedative effects in rodent models. This reagent is valuable for investigating neurological disorders, particularly in the context of schizophrenia research. -
α/β-Adrenergic Receptor Blocker
Arotinolol hydrochloride is a nonselective α/β-adrenergic receptor blocker that also functions as a vasodilating β-blocker. This compound exhibits significant potency in inhibiting the binding of the radioligand 125I-ICYP to 5HT1B serotonergic receptor sites. Arotinolol hydrochloride is primarily utilized as an antihypertensive agent in the management of various cardiovascular conditions, in addition to being studied for potential applications in non-cardiovascular diseases. -
5-HT Receptor Agonist
Osemozotan is a selective agonist of the 5-HT(1A) receptor, known for its role in modulating serotonergic signaling. This compound exhibits potential biological activity linked to anxiety and depression treatment, as well as influencing neurogenesis and synaptic plasticity. Research applications include investigations into the mechanisms of mood disorders and the development of novel therapeutic strategies targeting serotonin receptors. -
5-HT6 Antagonist
Ro4368554 is a selective antagonist of the 5-HT6 receptor, demonstrating the ability to penetrate the blood-brain barrier. This compound has shown efficacy in reversing memory deficits induced by scopolamine and tryptophan depletion. Ro4368554 serves as a valuable tool for investigating mechanisms underlying cognitive impairment and potential therapeutic strategies for memory-related disorders. -
5-HT2A Receptor Partial Agonist
(+)-OSU6162 is a partial agonist of the 5-HT2A receptor, acting as a stabilizer of dopaminergic and serotonergic signaling in the brain. This compound exhibits significant biological activity in modulating serotonin neurotransmission, making it a valuable tool for neurological research. Its ability to influence serotonin receptor activity positions it for use in studies related to mood disorders, cognitive function, and various neuropsychiatric conditions. -
D2 receptor/5-HT2A receptor Antagonist
S18327 is a selective antagonist of the D2 and 5-HT2A receptors, primarily targeting multiple neurotransmitter systems in the brain. Its pharmacological profile suggests efficacy in countering excessive dopamine activity and addressing glutamate hypo-function. S18327 has been shown to reproduce discriminative stimuli similar to Clozapine and may improve cognitive filtering deficits associated with schizophrenia while also exhibiting anxiolytic effects. Additionally, its reduced affinity for histaminergic and muscarinic receptors minimizes the risk of side effects commonly associated with other antipsychotic medications. -
Antipsychotic Agent
PD 158771 is an antipsychotic agent that acts as a partial agonist at D2 and D3 dopamine receptors (Ki = 42.0 nM and 13.7 nM, respectively) and as an agonist at 5-HT1A receptors (Ki = 2.6 nM). This dual activity allows PD 158771 to demonstrate potential in modulating dopaminergic and serotonergic signaling. It is primarily utilized in research focused on understanding the mechanisms underlying psychotic disorders and the development of novel antipsychotic therapies. -
5-HT Receptor Agonist
25I-NBF hydrochloride is a potent partial agonist of the 5-HT2A receptor, exhibiting a Ki value of 0.26 nM and an EC50 of 1.6 nM. This compound is primarily utilized in neuropharmacological research to investigate the role of 5-HT2A receptor modulation in various physiological and pathological processes. Its potency and selectivity make it a valuable tool for studying serotonergic signaling pathways and the development of related therapeutic agents. -
5-HT Receptor Agonist
E6801 is a selective 5-HT6 receptor agonist that enhances recognition memory through the modulation of cholinergic and glutamatergic neurotransmission pathways. This compound is essential for research into neuropsychiatric disorders, including dementia, depression, and obesity, as well as conditions such as epilepsy. E6801 serves as a valuable tool for investigating the therapeutic potential of targeting 5-HT6 receptors in cognitive enhancement and related fields. -
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. -
Stable Isotope
Paliperidone-d4 is the deuterated form of Paliperidone, a major active metabolite of Risperidone, acting as a dopamine D2 antagonist and 5-HT2A antagonist. This compound also exhibits antagonistic properties at alpha-1 and alpha-2 adrenergic receptors as well as H1-histaminergic receptors. Paliperidone's primary application is in the treatment of schizophrenia, making it valuable for pharmacological research and development of antipsychotic therapies. -
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. -
D2 Receptor Binder
Mosapramine is a D2 receptor binder that acts as an antipsychotic agent and is a metabolite of Clocapramine. It selectively binds to striatal dopamine D2 receptors and frontal lobe 5-HT2 receptors, exhibiting a D2/5-HT2 receptor occupancy ratio of 7.4. This compound induces characteristic neuropharmacological effects in rat models, including extrapyramidal symptoms, hyperprolactinemia, and increased salivation, while displaying a lower incidence of weight loss. Mosapramine is valuable for research applications related to schizophrenia and its underlying mechanisms. -
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. -
Serotonin/Dopamine Receptor Modulator
Brexpiprazole S-oxide is the primary metabolite of the atypical antipsychotic Brexpiprazole, functioning as a serotonin and dopamine receptor modulator. It exhibits partial agonism at the human 5-HT1A receptor and antagonism at the 5-HT2A receptor, with affinities (Ki) of 0.12 nM and 0.47 nM, respectively, and a potent partial agonist effect at the dopamine receptor (Ki = 0.3 nM). This compound is utilized in research focused on neuropharmacology, psychopharmacology, and the modulation of serotonergic and dopaminergic signaling pathways. -
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. -
Vasopressin Receptor Agonist
Argipressin acetate is a potent vasopressin receptor agonist, primarily targeting the V1, V2, and V3 receptors. It exhibits high affinity for the V1 receptor, with a dissociation constant (Kd) of 1.31 nM in A7r5 rat aortic smooth muscle cells. This compound is valuable for research applications exploring vascular physiology, fluid balance, and the modulation of blood pressure. -
Stable Isotope
Thioridazine-d3 hydrochloride is a deuterium-labeled derivative of Thioridazine, an antagonist of dopamine receptor D2 family proteins. It demonstrates significant anti-psychotic and anti-anxiety effects while also inhibiting the PI3K-Akt-mTOR signaling pathway, contributing to anti-angiogenic activity. Additionally, Thioridazine exhibits antiproliferative properties and induces apoptosis in various cancer cell types, with particular efficacy against cancer stem cells (CSCs). This stable isotope is valuable for pharmacokinetic studies and elucidating mechanisms of action in related research applications. -
ETA/ETB Antagonist
Macitentan-d4 is a deuterated analog of the dual ETA and ETB endothelin receptor antagonist, Macitentan. This compound exhibits significant biological activity by blocking the effects of endothelin-1, which is implicated in conditions such as pulmonary arterial hypertension (PAH) and idiopathic pulmonary fibrosis (IPF). Macitentan-d4 serves as a valuable tool for research into the underlying mechanisms of endothelin signaling and its role in cardiovascular and pulmonary disorders. -
Endocannabinoid
Arachidonoyl ethanolamide phosphate functions as an endogenous ligand for cannabinoid receptors, primarily targeting the CB1 subtype in the central nervous system and the CB2 subtype in peripheral immune cells. This compound is involved in modulating various physiological processes, including pain perception, mood regulation, and immune response. Its unique action profile makes it useful for research in neurobiology and immunology, particularly in studies focusing on the endocannabinoid system and its implications in various diseases.
