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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. -
5-HT7 Receptor Antagonist
Aramisulpride hydrochloride is a potent 5-HT7 receptor antagonist with a Ki value of 22 nM, demonstrating significant affinity for the D2 and D3 dopamine receptors as well, with Ki values of 140 nM and 13.9 nM, respectively. This compound is primarily utilized in psychiatric research to investigate the roles of serotonin and dopamine pathways in mental health disorders. Its unique pharmacological profile makes it a valuable tool for exploring therapeutic interventions and understanding neurobiological mechanisms. -
5-HT2A Agonist
ECPLA is a highly potent 5-HT2A agonist, exhibiting an EC50 value of 14.6 nM for Gq-mediated calcium signaling. As an analog of lysergic acid diethylamide (LSD), it demonstrates significant affinity for various serotonin receptors, α2-adrenoceptors, and D2-like dopamine receptors. ECPLA is valuable for research applications focused on neuropharmacology, receptor signaling pathways, and the exploration of serotonin-related mechanisms. -
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. -
D2 Receptor Agonist
(Rac)-Rotigotine serves as a dopamine D2 receptor agonist, exhibiting a multifaceted mechanism of action. It is recognized as a full agonist at dopamine receptors and a partial agonist at the 5-HT1A receptor, while also functioning as an antagonist of the α2B-adrenergic receptor, demonstrating Ki values of 0.71 nM for dopamine D3 and 4-15 nM for D2, D5, D4, and dopamine D1 receptors. This compound is primarily utilized in research focused on neurological disorders, particularly in the context of Parkinson's disease and other dopamine-related pathologies. -
5-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. -
Stable Isotope
(Rac)-Rotigotine-d3 hydrochloride is a deuterium-labeled analog of (Rac)-Rotigotine, primarily acting as a full agonist at dopamine receptors. It also serves as a partial agonist of the 5-HT1A receptor and acts as an antagonist at the α2B-adrenergic receptor, showcasing Ki values of 0.71 nM, 4-15 nM, and 83 nM for the respective targets. This stable isotope is vital for pharmacokinetic studies, isotope labeling experiments, and research related to neuropharmacology. -
Dopamine Stabilizer
(-)-OSU6162 hydrochloride is a dopamine stabilizer that functions as a partial agonist at the 5-HT2A receptor while acting as a dopamine D2 antagonist. This compound exhibits significant effects on modulating dopaminergic activity and is relevant for studies exploring aggression and irritability. Its unique mechanism makes it a valuable tool in research investigating neuropsychiatric disorders and dopaminergic regulation. -
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-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. -
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-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. -
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. -
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. -
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. -
Dopamine Receptor Antagonist
Flupentixol dihydrochloride is a potent antagonist of D1 and D2 dopamine receptors, demonstrating significant inhibition of PI3Kα with an IC50 of 127 nM. This compound exhibits anti-proliferative effects on cancer cells and promotes apoptosis, making it a valuable tool in oncology research. Additionally, Flupentixol has applications in studies related to schizophrenia, anxiety, and depression, contributing to the understanding of these complex neuropsychiatric disorders. -
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. -
D2/H1 Antagonist
Thiethylperazine is a potent antagonist of dopamine D2 and histamine H1 receptors. This phenothiazine derivative exhibits notable anti-emetic, antipsychotic, and antimicrobial properties, making it valuable in various therapeutic contexts. Additionally, it acts as a selective ABCC1 activator, contributing to the reduction of amyloid-β (Aβ) load in murine models, thus highlighting its potential relevance in neurodegenerative research. -
Anticholinergic Agent
Benztropine is an orally active anticholinergic agent that effectively crosses the blood-brain barrier. It serves as a dopamine re-uptake inhibitor and a human D2 dopamine receptor allosteric antagonist, making it relevant in Parkinson's disease research. Additionally, Benztropine demonstrates potential anti-cancer stem cell activity, enhancing its applicability in oncology studies. -
Antipsychotic Agent
Levomepromazine maleate is an N-substituted phenylthiazine compound that acts as an antipsychotic agent primarily targeting dopamine receptors. This compound exhibits significant sedative properties and is also a potent inhibitor of CYP2D6, making it a valuable tool for investigating the pharmacological mechanisms underlying schizophrenia. Its multifaceted receptor-blocking activity contributes to its role in research applications related to neuropsychiatric disorders. -
Dopamine Receptor Antagonist
Perphenazine dihydrochloride is a potent antagonist of dopamine receptors, primarily targeting D2 and D3 subtypes, with Ki values of 0.56 nM and 0.43 nM, respectively. Additionally, it exhibits activity against 5-HT2A and α1A adrenergic receptors. This compound demonstrates significant biological activity by inhibiting cancer cell proliferation and inducing apoptosis. Perphenazine dihydrochloride is particularly useful in research focused on mental disorders, oncology, and inflammatory processes. -
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. -
Dopamine D4 Receptor Antagonist
L 741742 is a highly selective antagonist of the dopamine D4 receptor, exhibiting a Ki of 3.5 nM for this target and demonstrating significantly lower affinity for the D2 and D3 receptors. This compound effectively suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, disrupts lysosomal function, and impairs autophagic flux. L 741742 induces G0/G1 cell-cycle arrest and apoptosis, enhances neuronal differentiation in human neural stem cells, and selectively targets the growth of glioblastoma neural stem cells. Its potential therapeutic applications include research in schizophrenia and glioblastoma, with demonstrated synergy when combined with Temozolomide in vitro. -
Dopamine Receptor Antagonist
Flupentixol is an orally active antagonist of D1 and D2 dopamine receptors. This compound exhibits anti-proliferative effects on cancer cells, promoting apoptosis, and has potential applications in the study of schizophrenia, anxiety, and depression. Additionally, Flupentixol has been identified as a new inhibitor of PI3Kα, with an IC50 value of 127 nM, making it a valuable reagent for research in neuropsychiatric disorders and cancer biology.

