Catalog No.
Product Name
Application
Product Information
Citations
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dopamine D2/D3 receptor antagonist
Amisulpride hydrochloride is a dopamine D2/D3 receptor antagonist with Kis of 2.8 and 3.2 nM for human dopamine D2 and D3, respectively. -
D2R antagonist
Pridopidine, a dopamine (DA) stabilizer, acts as a low affinity dopamine D2 receptor (D2R) antagonist. -
analgesic agent
Tetrahydropalmatine hydrochloride (DL-Tetrahydropalmatine hydrochloride), an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats. - MIF-1 TFA (Melanostatin), an endogenous brain peptide, is a potent dopamine receptor allosteric modulator. MIF-1 TFA inhibits melanin formation. MIF-1 TFA blocks the effects of opioid receptor activation to modulate the analgesic effects. MIF-1 TFA accesses from the blood to the CNS by directly crossing the blood-brain barrier (BBB).
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analgesic agent
Tetrahydropalmatine, an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats. -
dopamine D1-like receptor antagonist
SCH-23390 maleate (R-(+)-SCH-23390 maleate) is a potent and selective dopamine D1-like receptor antagonist with Kis of 0.2 nM and 0.3 nM for the D1 and D5 receptor, respectively. -
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. -
Stable Isotope
Perphenazine-d4 is a deuterated derivative of Perphenazine, a typical antipsychotic agent primarily inhibiting the 5-HT2A receptor, alpha-1A adrenergic receptor, dopamine receptor D2/D3, D2L receptor, and histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively. This stable isotope is valuable for pharmacokinetic studies, allowing for the precise tracking of Perphenazine metabolism and distribution in biological systems. Perphenazine-d4 is essential for researchers focusing on neuropharmacology and drug interaction studies involving antipsychotic medications. -
Dopaminergic Neurotoxin
MPTP (1-Methyl-4-phenyl-1,2,3,6-tetrahydropyridine) is a potent dopaminergic neurotoxin that readily penetrates the blood-brain barrier. It is primarily utilized to create animal models of Parkinson’s Disease, enabling the study of neurodegenerative processes. MPTP acts by converting into MPP+, which induces apoptosis in dopaminergic neurons, serving as a valuable tool for investigating therapeutic strategies and the underlying mechanisms of neurodegeneration. -
5-HT5A Receptor Antagonist
SB-699551 free base is a selective antagonist of the 5-HT5A receptor, characterized by a pKi of 8.2 nM, which allows for effective brain penetration. It exhibits significant selectivity over various serotonin receptor subtypes, dopamine receptors, and the α1B adrenoceptor. This compound disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, influencing the phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. SB-699551 free base is valuable for research into anxiety, breast cancer, and Alzheimer's disease. -
5-HT5A Antagonist
SB-699551 is a selective 5-HT5A receptor antagonist with a pKi of 8.2 nM, demonstrating significant brain penetrance. This compound exhibits high selectivity over various 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptors. By disrupting Gαi/o-coupled signaling and the PI3K/AKT/mTOR pathways, SB-699551 influences phosphorylation of key proteins such as CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 in breast tumor cells. It serves as a valuable tool in the study of anxiety, breast cancer, and Alzheimer's disease. -
Dopamine β-hydroxylase Inhibitor
Fusaric acid is a potent dopamine β-hydroxylase inhibitor that reduces endogenous levels of norepinephrine and epinephrine in various tissues, including the brain, heart, spleen, and adrenal glands. By inducing oxidative stress and apoptosis, fusaric acid disrupts mitochondrial integrity and activates key apoptosis-related proteases such as Caspase-3/7, -8, and -9. Additionally, fusaric acid regulates pivotal apoptotic proteins, inhibits fibrosis-related signaling pathways including NF-κB and TGF-β1/SMADs, and mitigates collagen deposition. Its applications extend to myocardial fibrosis and cardiac hypertrophy research, as well as studies on esophageal and liver cancers. -
Dopamine D2/D3 Agonist
Piribedil is a potent and orally active agonist of dopamine D2 and D3 receptors, also exhibiting antagonistic activity at α2-adrenoceptors. Additionally, Piribedil inhibits MLL1 methyltransferase with an EC50 value of 0.18 μM. This compound is primarily utilized in research focused on Parkinson’s disease, circulatory disorders, and certain cancers, making it a valuable tool for exploring dopaminergic pathways and related therapeutic strategies. -
Anticholinergic Agent
Benztropine mesylate is a centrally acting anticholinergic agent that effectively crosses the blood-brain barrier. It primarily functions as a selective antagonist at human D2 dopamine receptors, exhibiting anti-histaminic properties and acting as a dopamine re-uptake inhibitor. This compound is particularly relevant for Parkinson's disease research, as well as in studies exploring its effects on cancer stem cells (CSCs). Researchers can utilize Benztropine mesylate to examine its potential therapeutic benefits in neurodegenerative and cancer treatment contexts. -
Dopamine Receptor Antagonist
Levosulpiride is a selective antagonist of dopamine D2 receptors, classified as an atypical antipsychotic agent within the benzamide family. This compound is primarily used in the investigation of its effects on psychotic disorders and gastrointestinal conditions due to its ability to modulate dopaminergic activity. Researchers utilize Levosulpiride to study its therapeutic potential in conditions such as schizophrenia and to explore its impact on gastrointestinal motility. -
5-HT Receptor Modulator
Lurasidone Hydrochloride is a potent antagonist of both dopamine D2 and 5-HT7 receptors, exhibiting IC50 values of 1.68 nM and 0.495 nM, respectively. Additionally, it acts as a partial agonist at the 5-HT1A receptor with an IC50 of 6.75 nM. This compound is utilized in research focused on neuropharmacology and the treatment of psychiatric disorders, such as schizophrenia and bipolar disorder. Its selective modulation of serotonin and dopamine receptors makes it a valuable tool for investigating neurochemical pathways and therapeutic interventions. -
Dopamine Receptors Blocker
Trifluoperazine dihydrochloride is a dopamine receptor antagonist, primarily used in the study of schizophrenia. This compound demonstrates significant activity as an α1-adrenergic receptor blocker and acts as a potent inhibitor of NUPR1, exhibiting anticancer properties. Additionally, it functions as a calmodulin inhibitor and has been shown to inhibit P-glycoprotein, impacting multidrug resistance. Trifluoperazine dihydrochloride is also recognized for its reversible inhibition of influenza virus morphogenesis, making it valuable for various research applications in neuropharmacology and virology. -
5-HT1/D2 Agonist
Sarizotan dihydrochloride is a potent agonist of the serotonin 5-HT1A receptor and dopamine receptors. It demonstrates strong activity with IC50 values of 6.5 nM for rat 5-HT1A, 0.1 nM for human 5-HT1A, 15.1 nM for rat D2, 17 nM for human D2, 6.8 nM for human D3, and 2.4 nM for human D4.2. Sarizotan dihydrochloride is utilized in research to explore neuropharmacology, behavior, and potential therapeutic effects on psychiatric disorders. -
Stable Isotope
Loxapine-d8 hydrochloride is a deuterated derivative of Loxapine, primarily acting as a D2 and D4 dopamine receptor inhibitor. This stable isotope is utilized in research to study pharmacokinetics and metabolic pathways of Loxapine. Its serotonergic receptor antagonism further facilitates investigations into the neuropharmacological effects associated with dibenzoxazepine anti-psychotic agents. -
D3 Receptor Ligand
Dopamine D3 Receptor Ligand-5 is a selective ligand for the dopamine D3 receptor, exhibiting a Ki value of 0.14 nM, indicating high affinity. Additionally, it also demonstrates significant interaction with the D2 receptor, possessing a Ki value of 2.85 nM. This compound is primarily utilized in neurological research to investigate dopamine signaling pathways and their implications in neuropsychiatric disorders. Its specificity for the D3 receptor makes it a valuable tool for studies on receptor pharmacology and therapeutic development. -
5-HT2A Receptor Activator
ETH-LAD (N-Ethyl-nor-LSD) is a selective activator of the 5-HT2A receptor, exhibiting a binding affinity with a Ki value of 5.1 nM. Additionally, it demonstrates affinity for dopamine receptors D1 and D2, with Ki values of 22.1 nM and 4.4 nM, respectively. ETH-LAD is utilized in research exploring psychoactive effects and receptor pharmacology in various models, including rat studies. -
Asenapine Metabolite
N-Desmethyl asenapine is a primary metabolite of Asenapine, an atypical antipsychotic agent. This compound functions as an antagonist at multiple receptor sites, including serotonin, adrenoceptors, dopamine receptors, and histamine receptors. N-Desmethyl asenapine is valuable for research into psychopharmacology and the pharmacokinetics of antipsychotic drugs. Its role in studying the therapeutic and side effects associated with Asenapine makes it a significant reagent in the field. -
Stable Isotope
Quetiapine-d8 fumarate is a deuterated derivative of Quetiapine, primarily functioning as a stable isotope for enhanced analytical studies. This compound acts as a 5-HT receptor agonist, exhibiting a pEC50 of 4.77 for the human 5-HT1A receptor, while also serving as a dopamine receptor antagonist with a pIC50 of 6.33 for the human D2 receptor. Quetiapine-d8 fumarate demonstrates moderate to high affinity for multiple receptors, including human D2, 5-HT1A, 5-HT2A, and 5-HT2C, with respective pKis of 7.25, 5.74, 7.54, and 5.55, making it valuable for research into antidepressant and anxiolytic pharmacology. -
D2 Receptor/5HT2A Receptor Antagonist
5-HT2A Antagonist 4 Methanesulfonate is a selective antagonist of both dopamine D2 receptors and serotonin 5HT2A receptors. This compound is primarily utilized in research concerning central nervous system disorders, facilitating the exploration of neuropharmacology and the modulation of neurotransmitter activity. Its dual receptor targeting makes it a valuable tool for studying the pathophysiology and treatment strategies for various neuropsychiatric conditions. -
D2/5-HT2 Antagonist
Iloperidone hydrochloride is a dual D2 and 5-HT2 receptor antagonist. It is classified as an atypical antipsychotic and is primarily utilized in the treatment of schizophrenia symptoms. This compound is valuable for research focused on neuropharmacology and the elucidation of antipsychotic mechanisms. -
Antipsychotic agent
Rilapine is an atypical antipsychotic agent that primarily targets serotonin and dopamine receptors in the brain. It demonstrates significant efficacy in managing symptoms of schizophrenia and bipolar disorder. This compound is valuable for research into neuropsychiatric disorders and the development of novel therapeutic strategies in psychiatry. -
Serotonin/Norepinephrine/Dopamine Reuptake Inhibitor
Bicifadine is a serotonin/norepinephrine/dopamine reuptake inhibitor that demonstrates oral bioavailability. It exhibits significant antinociceptive properties across various models of acute, persistent, and chronic pain. Bicifadine is primarily utilized in research related to pain mechanisms and therapeutic interventions for pain management. -
Antidepressant Agent
Captodiame, a 5-HT2c receptor antagonist, exhibits significant antidepressant activity by modulating serotonin signaling. In addition, it acts as an agonist at sigma-1 and D3 dopamine receptors, enhancing its therapeutic potential. This compound is of interest for researchers focused on neuropharmacology and the development of novel antidepressant therapies. -
5-HT2A/dopamine D2 Antagonist
Abaperidone hydrochloride is a potent antagonist of the 5-HT2A receptor and dopamine D2 receptor, exhibiting IC50 values of 6.2 nM and 17 nM, respectively. This compound demonstrates significant affinity in modulating serotonergic and dopaminergic signaling pathways, making it a valuable tool for studying neuropharmacology and the treatment of psychiatric disorders. Research applications include investigations into schizophrenia, anxiety, and mood disorders. -
D3 Receptor Antagonist
RGH-1756 is a selective antagonist of the human D3 dopamine receptor, exhibiting pronounced effects in modulating dopaminergic pathways. This compound demonstrates lesser antagonistic activity on the human D2L and 5HT1A receptors. RGH-1756 is primarily utilized in research focusing on neuropharmacology and the mechanism of antipsychotic treatments, particularly in understanding conditions related to dopamine dysregulation. -
5-HT/DA Receptor Antagonist
Ziprasidone mesylate is a potent antagonist of the 5-HT and dopamine receptors, specifically targeting the Rat D2 receptor (Ki=4.8 nM), the 5-HT2A receptor (Ki=0.42 nM), and the 5-HT1A receptor (Ki=3.4 nM). This compound demonstrates significant activity in modulating serotonergic and dopaminergic pathways, making it valuable for research in psychiatric disorders, such as schizophrenia and mood disorders. Its unique pharmacological profile allows for a better understanding of the interplay between these neurotransmitter systems in various biological contexts. -
D2R/D3R/5-HT1AR Agonist
D2R/D3R/5-HT1AR agonist 1 is an orally active compound that selectively targets dopamine receptors D2R and D3R, as well as the serotonin receptor 5-HT1AR, exhibiting EC50 values of 1.29 nM, 1.05 nM, and 153.5 nM, respectively. This compound has demonstrated efficacy in alleviating behavioral disorders induced by MPTP and possesses anti-depressant properties. D2R/D3R/5-HT1AR agonist 1 is valuable for research in the fields of Parkinson's disease and depression, aiding in the exploration of potential therapeutic interventions. -
Quetiapine Metabolite
Quetiapine sulfone is a primary metabolite of Quetiapine, acting predominantly as a serotonin (5-HT) receptor agonist and a dopamine receptor antagonist. This compound is essential for studying the pharmacokinetics and efficacy of Quetiapine in various neurological disorders, including schizophrenia and bipolar disorder. Its role in modulating neurotransmitter systems makes it a valuable reagent for researchers exploring antipsychotic mechanisms and drug metabolism. -
D2/5-HT2A Receptors Antagonist
Clocapramine dihydrochloride hydrate is a potent antagonist of the D2 and 5-HT2A receptors. It demonstrates significant biological activity by inhibiting the signaling pathways associated with these receptors, making it valuable for pharmacological research. This compound is particularly useful in studies related to neuropharmacology, psychopharmacology, and the development of therapeutic agents targeting psychiatric disorders. -
5-HT/Dopamine Antagonist
BGC20-761 is a selective antagonist of the 5-HT6 and dopamine receptors, exhibiting human receptor Ki values of 20 nM for 5-HT6, 69 nM for 5-HT2A, and 140 nM for D2. It has demonstrated the ability to enhance long-term memory, suggesting its potential utility in cognitive enhancement therapies. Additionally, BGC20-761 may serve as a promising candidate for the development of antipsychotic agents, supporting research in neuropharmacology and mental health disorders. -
D2 Antagonist
Clozapine dihydrochloride is an antipsychotic compound that primarily functions as a dopamine D2 receptor antagonist, exhibiting a Ki of 75 nM. It demonstrates significant affinity for muscarinic M1 and serotonin 5HT2A receptors, with Kis of 9.5 nM and 4 nM, respectively. Additionally, Clozapine acts as a potent and selective agonist at the muscarinic M4 receptor, with an EC50 of 11 nM. This compound is crucial for research into schizophrenia and related neuropsychiatric disorders. -
5-HT6 Receptor Antagonist
SB-773812 is a high-affinity antagonist of the serotonin 5-HT6 receptor, exhibiting a pKi of 8.1. Additionally, it demonstrates moderate to high affinity for dopamine receptors 2 and 3, with pKi values of 7.4 and 8.5, respectively. This compound is primarily used in research investigating central nervous system disorders, particularly those involving serotonin and dopamine signaling pathways. Its profile suggests potential applications in studying neuropharmacology and related therapeutic areas. -
Stable Isotope
Deulumateperone is a deuterated derivative of Lumateperone, serving as a stable isotope for research applications. Lumateperone acts as a selective antagonist of the 5-HT2A receptor (Ki = 0.54 nM) and modulates dopamine receptors, demonstrating significant antipsychotic and antineoplastic properties. This reagent is valuable for studies involving receptor interactions, pharmacokinetics, and metabolic profiling in various biological systems. -
Dopamine/5-HT Receptor Inhibitor
Loxapine hydrochloride is an orally active inhibitor of dopamine receptors and an antagonist of 5-HT receptors. This dibenzoxazepine compound exhibits significant antipsychotic properties, making it valuable for research into psychotropic effects and therapeutic interventions for schizophrenia and other psychiatric disorders. Its dual receptor activity contributes to its efficacy in modulating dopaminergic and serotonergic pathways. -
D2/5-HT1A Agonist
Bifeprunox is a potent partial agonist for the dopamine D2 receptor and the 5-HT1A receptor, exhibiting a pKi of 7.19 for cortex 5-HT1A and 8.83 for striatum D2. It demonstrates a pEC50 of 6.37 for hippocampus 5-HT1A. This compound is utilized in research related to antipsychotic mechanisms and is particularly relevant for studies focusing on schizophrenia. -
5-HT1E/1F Agonist
BRL 54443 maleate is a potent agonist of the 5-HT1E and 5-HT1F receptors, exhibiting Ki values of 1.1 nM and 0.7 nM, respectively. This compound demonstrates over 30-fold selectivity against other serotonin and dopamine receptors, making it a valuable tool in the study of serotonergic signaling pathways. BRL 54443 maleate is primarily used in research applications focused on anxiety, depression, and other neuropsychiatric disorders where 5-HT receptor modulation is implicated. -
Stable Isotope
Quetiapine-d4-1 fumarate is a deuterated analogue of Quetiapine, specifically designed to enhance analytical precision in research applications. As a serotonin (5-HT) receptor agonist, it exhibits a pEC50 of 4.77 at the human 5-HT1A receptor and acts as a dopamine receptor antagonist with a pIC50 of 6.33 for the human D2 receptor. Quetiapine-d4-1 fumarate demonstrates moderate to high affinity for several key receptors, including D2, 5-HT1A, 5-HT2A, and 5-HT2C, making it suitable for studies in neuropharmacology, particularly in exploring antidepressant and anxiolytic effects. -
5-HT1/D2 Agonist
Sarizotan hydrochloride is a potent agonist of the serotonin 5-HT1A receptor and dopamine receptors D2, D3, and D4. It demonstrates high affinity with IC50 values of 0.1 nM for human 5-HT1A, 15.1 nM for rat D2, and 2.4 nM for human D4.2, among others. This compound is primarily utilized in neurological research and pharmacological studies, particularly in the exploration of psychopharmacological interventions and the modulation of serotonergic and dopaminergic pathways. -
Antipsychotic Agent
PZ-1190 is a multitarget ligand that primarily interacts with serotonin and dopamine receptors, exhibiting potential antipsychotic activity. This compound has been studied in rodent models to explore its effects on psychotic behaviors. Its unique mechanism of action positions it as a valuable tool for research into psychiatric disorders and the underlying neurotransmitter systems. -
Dopamine Receptor Antagonist
Zicronapine fumarate is a potent dopamine receptor antagonist primarily targeting D1 and D2 receptors, as well as serotonin 5-HT2A receptors. It exhibits significant pro-cognitive effects in preclinical models, positioning it as a promising candidate for the treatment of various neurological and psychiatric disorders. Research applications include the exploration of its therapeutic potential in conditions such as schizophrenia and mood disorders. -
5-HT2A Receptor Inhibitor
Belaperidone is a selective 5-HT2A receptor inhibitor, demonstrating significant antidopaminergic and antiserotonergic properties. This compound is primarily employed in research related to neuropsychiatric disorders and may provide insight into therapeutic strategies for conditions such as schizophrenia and depression. Its mechanism of action makes Belaperidone a valuable tool in studying serotonin and dopamine receptor interactions within the central nervous system. -
5-HT4/Dopamine D2 Receptor Agonist
Lirexapride is an agonist of the 5-HT4 and Dopamine D2 receptors. It is primarily known for its stimulatory effects on gastrointestinal motility, making it a valuable tool for researching digestive system disorders. This compound facilitates the study of gastroenterological conditions and the mechanisms underlying gut health and function. -
Antipsychotic Agent
Thiothixene hydrochloride functions as an antipsychotic agent by antagonizing dopamine receptors in the central nervous system. This compound is particularly relevant for research in psychiatric disorders, including borderline personality disorder and schizotypal disorder, facilitating the study of their underlying mechanisms and potential therapeutic strategies. Its application in preclinical and clinical studies underscores its importance in understanding the efficacy and safety of antipsychotic treatments. -
Dopamine Receptor Antagonist
Zicronapine is a potent dopamine receptor antagonist targeting both D1 and D2 subtypes, as well as serotonin receptor 5-HT2A. This compound demonstrates notable pro-cognitive effects in animal models, suggesting its potential utility in the treatment of various neurological and psychiatric disorders. Zicronapine's pharmacological profile makes it a valuable tool for research into psychotropic drug mechanisms and cognitive enhancement strategies.
