Catalog No.
Product Name
Application
Product Information
Citations
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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. -
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. -
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. -
5-HT6 Antagonist
Cerlapirdine hydrochloride is a selective and potent antagonist of the 5-hydroxytryptamine 6 (5-HT6) receptor. This compound is primarily employed in research related to neuropharmacology and has potential applications in the study of Alzheimer's disease. By modulating serotonergic signaling pathways, Cerlapirdine hydrochloride offers valuable insights into the mechanisms underlying cognitive disorders. -
5-HT2B Receptor Antagonist
SB-215505 is a selective antagonist of the 5-HT2B receptor, exhibiting a pKi of 8.3 for this target and lower affinities for 5-HT2A (pKi 6.77) and 5-HT2C (pKi 7.66). This compound has been shown to enhance wakefulness and motor activity in rodent models. SB-215505 is useful for studying the role of 5-HT2B receptors in various physiological and behavioral processes. -
D4/5-HT2A Antagonist
PNU-96415E is a selective antagonist of the dopamine D4 receptor and the 5-HT2A serotonin receptor. It demonstrates potential antipsychotic efficacy, making it a valuable tool in the study of neuropsychiatric disorders. Researchers can utilize PNU-96415E to explore its effects on dopaminergic and serotonergic signaling pathways in various preclinical models. -
5-HT1B/1D Receptor Agonist
Frovatriptan succinate is a selective agonist of the 5-HT1B and 5-HT1D receptors, exhibiting a pK50 of 8.2. This compound demonstrates greater than 10-fold selectivity for the targeted receptors compared to 5-HT1A, 5-HT1F, and 5-HT7, and over 1000-fold selectivity against various other receptors, including dopamine, histamine H1, and α1-adrenoceptors. Frovatriptan succinate is primarily utilized in migraine research, providing valuable insights into the mechanisms underlying migraine pathophysiology and potential therapeutic interventions. -
5-HT1A Receptor Agonist
(S)-LY-41 is a potent and selective agonist of the 5-HT1A receptor. This compound significantly reduces accumulations of 5-hydroxytryptophan in the rat brain, induced by decarboxylase inhibitors, and has been shown to lower body temperature and inhibit escape responses in animal models. Additionally, (S)-LY-41 can induce the 5-HT behavioral syndrome, making it a valuable tool for investigating neurological disorders such as depression and anxiety. -
5-HT Agonist
Frovatriptan is a selective agonist of the 5-HT1B and 5-HT1D serotonin receptors, exhibiting the highest potency for 5-HT1B among the triptan class. It demonstrates cerebroselectivity, making it particularly effective in targeting migraine pathophysiology. Frovatriptan is effective in alleviating migraine attacks, including those occurring during the headache phase with aura, highlighting its relevance in migraine research and therapeutic applications. -
5-HT1A Receptor Agonist
BP 554 is a selective agonist of the 5-HT1A receptor, classified as a Piperazine derivative. This compound has been shown to induce hypothermia, making it valuable for studies investigating the role of the 5-HT1A receptor in thermoregulation and related physiological processes. Its specific action on the 5-HT1A receptor positions BP 554 as a useful tool for research into serotonergic signaling pathways. -
DA/5-HT Releaser
5-Chloro-α-methyltryptamine is a potent and selective dual dopamine (DA) and serotonin (5-HT) releaser, as well as a 5-HT2A agonist. It effectively releases DA and 5-HT, with EC50 values of 54.3 nM and 16.2 nM, respectively. This compound is valuable for research in neurotransmitter dynamics and the exploration of related neuropharmacological pathways. -
5-HT6 Receptor Antagonist
MS 245 oxalate is a potent 5-HT6 receptor antagonist, exhibiting an inhibition constant (Ki) of 2 nM. This compound is valuable for research into neuropsychiatric disorders and cognitive function, particularly in studies exploring the modulation of serotonergic signaling. Its high affinity for the 5-HT6 receptor positions it as a significant tool for investigating potential therapeutic interventions. -
5-HT2C Agonist
5-HT2C agonist-12 is a selective and orally active agonist targeting the 5-HT2C receptor. It demonstrates potent inhibition of inositol trisphosphate (IP3) accumulation with an IC50 value of 4.5 nM. This compound has been shown to promote satiety, reduce eating duration, and lower caloric intake, making it a valuable tool in obesity research. -
5-HT Reuptake Inhibitor
Ifoxetine is a selective inhibitor of the serotonin (5-HT) reuptake process, primarily targeting the central nervous system while sparing peripheral uptake in blood platelets. This compound effectively inhibits the uptake of radiolabeled 5-HT in rat brain synaptosomes, both in vitro and ex vivo. Due to its mechanism of action, Ifoxetine demonstrates potential antidepressant properties and can be utilized in research related to mood disorders and serotonin signaling. -
5-HT1A/1B Agonist
RU 24969 hemisuccinate is a selective agonist for the serotonin receptors 5-HT1A and 5-HT1B, with a Ki of 0.38 nM for 5-HT1B and 2.5 nM for 5-HT1A. This compound exhibits low affinity for other brain receptor sites. Research indicates that RU 24969 hemisuccinate may decrease fluid consumption and enhance forward locomotion, supporting its use in studies related to serotonergic modulation and behavior. -
5HT1B/1D Receptor Agonist
GR-4991W93 is an orally active partial agonist of the 5HT1B and 5HT1D receptors, showing pIC50 values of 6.95 and 7.80, respectively. This compound exhibits significant inhibition of electrically evoked plasma extravasation in guinea pig models, demonstrating its pharmacological potential in modulating neurogenic inflammation. GR-4991W93 is suitable for use in migraine research, offering insights into the mechanisms underlying this condition. -
5-HT2C Agonist
5-HT2C agonist-3 free base is a selective agonist of the 5-HT2C receptor, exhibiting an EC50 of 24 nM and a Ki of 78 nM. This compound demonstrates antipsychotic-like activity and effectively inhibits amphetamine-induced hyperactivity. It serves as a valuable research tool for investigating the role of 5-HT2C receptor modulation in neurological disorders and potential therapeutic applications. -
5-HT1B Receptor Agonist
Anpirtoline is a potent agonist of the 5-HT1B receptor, exhibiting a Ki of 28 nM for this target, alongside 150 nM for 5-HT1A and 1.49 μM for 5-HT2 receptors. This compound demonstrates notable serotonergic activity and has been linked to antinociceptive and antidepressant-like effects. Anpirtoline is primarily utilized in research to explore its potential therapeutic applications in mood disorders and pain management. -
5-HT2R Antagonist
DV-7028 hydrochloride is a selective antagonist of the 5-hydroxytryptamine 2 (5-HT2) receptor. This compound exhibits significant inhibitory activity against 5-HT2 receptor-mediated signaling pathways, making it valuable for studying serotonin-related biological processes. Research applications include investigating the roles of 5-HT2 receptors in neurobiology, psychiatry, and pharmacology. -
5-HT4 Partial Agonist
PF-03382792 is a potent partial agonist of the 5-HT4 receptor, exhibiting a Ki value of 2.7 nM and an EC50 of 0.9 nM for the 5-HT4d subtype. This compound demonstrates the ability to penetrate the blood-brain barrier and has been shown to elicit moderate increases in cortical acetylcholine levels in the rat prefrontal cortex. PF-03382792 is a valuable tool for research investigating cognitive processes and potential therapeutic strategies for neurological disorders. -
SERT Inhibitor/5-HT₂A receptor Antagonist
LY 367265 is a potent inhibitor of the serotonin transporter (SERT) with an IC₅₀ value of 3.1 nM and also serves as a selective antagonist for the 5-HT₂A receptor (Kᵢ = 0.81 nM). It displays minimal activity on the norepinephrine transporter (NET) and low affinity for other serotonin receptor subtypes, reinforcing its selectivity. LY 367265 enhances the efflux of [³H]5-HT in a concentration-dependent manner (EC₅₀ = 250 nM) and can counteract the contraction induced by Sumatriptan, indicating its antagonistic effects on 5-HT₁D-like receptors. This compound is valuable for research into neurological disorders, including anxiety and post-traumatic stress disorder. -
5-HT₁A Receptor Agonist
U 93385 is a selective agonist of the 5-HT₁A receptor, primarily involved in neurotransmission modulation. This compound does not exhibit significant activity at α₂ adrenergic or D₂ dopamine receptors, making it suitable for specific studies targeting the 5-HT₁A pathway. U 93385 has been shown to influence heart rate by stimulating the vagus nerve, leading to bradycardia. This makes it a valuable tool for investigating the mechanisms underlying 5-HT₁A receptor-mediated vagal nerve tolerance. -
5-HT1D Agonist
CP-135807 is a selective 5-HT1D agonist with an IC50 of 3.1 nM, exhibiting oral bioactivity. This compound demonstrates significant central psychoactive effects, making it a valuable tool in antidepressant research. Its targeted action on the serotonin receptor subtype enables investigation into mood regulation and related pharmacological applications. -
5-HT2A Receptor Activator
AL-LAD, or 6-Allyl-6-nor-LSD, is a potent activator of the 5-HT2A receptor, exhibiting a Ki value of 3.4-8.1 nM. Additionally, it demonstrates notable affinity for dopamine D1 and D2 receptors, with K0.5 values of 189 nM and 12.3 nM, respectively. AL-LAD's psychoactive properties have been investigated in mouse models, making it a valuable tool for research in neuropharmacology and the study of serotonergic and dopaminergic pathways. -
5-HT1A Receptor Modulator
Ipsapirone hydrochloride is a selective modulator of the 5-HT1A receptor, functioning primarily as a partial agonist. This compound demonstrates anxiolytic properties, making it relevant for research in anxiety disorders. At elevated concentrations, ipsapirone hydrochloride can also exhibit antagonistic effects on the 5-HT1A receptor and inhibit 5-HT2 and α1-adrenergic receptor activities, expanding its applicability in pharmacological studies of serotonergic and adrenergic signaling pathways. -
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. -
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. -
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. -
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. -
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.
