Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Dopamine D2/D3 Agonist
Piribedil maleate is a potent agonist of dopamine D2 and D3 receptors, with additional activity as an α2-adrenoceptor antagonist. It has been shown to inhibit MLL1 methyltransferase activity with an EC50 of 0.18 μM. Piribedil maleate is of interest for research applications related to Parkinson’s disease, circulatory disorders, and various cancers. -
Dopamine D2/D3 Agonist
Piribedil hydrochloride is a potent agonist of dopamine D2 and D3 receptors, serving as a valuable tool for investigating dopaminergic signaling pathways. In addition to its agonistic activity, it acts as an antagonist at α2-adrenoceptors and inhibits MLL1 methyltransferase with an EC50 of 0.18 μM. This compound is primarily utilized in research related to Parkinson's disease, circulatory disorders, and certain types of cancer, making it an important reagent for studies focused on neurodegeneration and tumor biology. -
Dopamine D2/D3 Agonist
Piribedil dihydrochloride is a potent dopamine D2 and D3 agonist, also functioning as an antagonist at α2-adrenoceptors. This compound exhibits inhibitory activity on MLL1 methyltransferase with an EC50 of 0.18 μM. It is primarily utilized in research focused on Parkinson's disease, circulatory disorders, and various types of cancers. -
Stable Isotope
Dopamine-d5 hydrochloride is a deuterium-labeled analogue of dopamine, a catecholamine neurotransmitter primarily synthesized in the substantia nigra, ventral tegmental area, and hypothalamus. This compound retains the essential biological functions of dopamine, including its interaction with D2 dopamine receptors, which mediates the endocytosis of VEGFR2, a key process in angiogenesis. Dopamine-d5 hydrochloride is valuable for research applications involving neurotransmitter dynamics, neuropharmacology, and angiogenic pathways. -
Antipsychotic Agent
Penfluridol is a potent, long-acting antipsychotic agent that primarily targets D2-like dopamine receptors. It exhibits significant anti-inflammatory properties by inhibiting TNFα-induced NF-κB activation and demonstrates efficacy in models of arthritis and colitis. Additionally, Penfluridol acts as a Ca2+-calmodulin inhibitor, inducing apoptosis and autophagy in various cellular contexts. This compound is utilized in research focusing on chronic schizophrenia, acute psychosis, Tourette syndrome, autoimmune diseases, and it also shows antibacterial activity against E. faecalis with a minimum inhibitory concentration of 7.81 μg/ml. -
Dopamine Receptor Antagonist
Perphenazine is a potent dopamine receptor antagonist, specifically targeting D2 and D3 receptors with Ki values of 0.56 nM and 0.43 nM, respectively, while also interacting with the 5-HT2A receptor and the Alpha-1A adrenergic receptor. This compound demonstrates inhibitory effects on cancer cell proliferation and promotes apoptosis. Perphenazine is valuable for research into psychiatric disorders, cancer biology, and inflammatory processes. -
Dopamine Receptor Antagonist
Spiperone is a potent antagonist of dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A receptors. With its capability to enhance intracellular calcium levels and inhibit the Wnt signaling pathway, Spiperone serves as a valuable tool in the study of neurological disorders. Its role as a labeled ligand for neuroleptic receptors further underscores its utility in receptor binding studies and neurotransmitter research. This compound is particularly relevant for investigating the mechanisms underlying various neuropsychiatric conditions. -
Dopamine D1/D5 Receptor Antagonist
SKF-83566 is a selective antagonist of the D1-like dopamine receptors, specifically targeting the dopamine D1 and D5 receptors. This compound exhibits potent inhibition of the dopamine transporter (DAT) with an IC50 of 5.7 μM, and shows competitive antagonism at the vascular 5-HT2 receptor. In addition, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it relevant for research into neurological disorders such as Parkinson's disease and studies focused on alleviating nicotine cravings. -
D2R Agonist
UNC9994 hydrochloride is a functionally selective agonist of the dopamine D2 receptor (D2R), exhibiting β-arrestin–biased signaling and selectively activating β-arrestin recruitment. With a binding affinity of Ki 79 nM for D2R, it functions as an antagonist of Gi-mediated cAMP production and a partial agonist for D2R/β-arrestin-2 interactions. This compound demonstrates antipsychotic-like effects, making it a valuable tool for research in neuropharmacology and the study of dopamine receptor signaling pathways. -
Dopamine D3 Receptor Antagonist
SB-277011 hydrochloride is a selective antagonist of the dopamine D3 receptor (D3R), demonstrating potent inhibition with Ki values of 10.7 nM in rodents and 11.2 nM in humans. This compound exhibits significant selectivity, with an 80- to 100-fold preference for D3R over other dopamine receptors, including D2, 5-HT1B, and 5-HT1D. Due to its ability to penetrate the brain and oral bioavailability, SB-277011 hydrochloride is valuable in research investigating the role of D3R in various neurological and psychiatric disorders. -
Dopamine/5-HT2A Antagonist
Paliperidone palmitate is a competitive antagonist of dopamine D2 and 5-hydroxytryptamine 2A (5-HT2A) receptors with the capability to cross the blood-brain barrier. By binding to these receptors, it modulates the activity of dopamine and serotonin, thereby exerting antipsychotic effects. This compound is primarily utilized in research related to schizophrenia and other neuropsychiatric disorders, contributing to the understanding of antipsychotic mechanisms and therapeutic strategies. -
Dopamine Receptor Antagonist
2-Bromo-LSD (BOL-148; Bromolysergide) is a potent dopamine receptor antagonist specifically targeting dopamine neurons in the substantia nigra and neostriatum. It enhances the hydroxylation of tyrosine within the striatum and mitigates the reduction of Apomorphine-induced DOPA accumulation. Additionally, 2-Bromo-LSD inhibits 5-HT receptor-mediated DOPA formation, making it valuable for research on neurotransmitter regulation and potential therapeutic applications in neuropharmacology. -
Dopamine D2/5-HT2A Receptor Antagonist
Spiperone hydrochloride is a potent antagonist of dopamine D2 and 5-HT2A receptors, exhibiting Ki values of 0.06 nM and 1 nM, respectively. In addition, it selectively antagonizes the α1B-adrenoceptor and activates calcium-activated chloride channels (CaCC). This compound has demonstrated significant antipsychotic and anti-inflammatory properties, making it a valuable tool for research in neuropharmacology and inflammation studies. -
D2 Receptor Inhibitor, D3 Receptor Inhibitor, 5-HT1A Receptor Inhibitor, 5-HT2B Receptor Inhibitor
Desmethyl cariprazine is a potent inhibitor of the D2 and D3 dopamine receptors, as well as the 5-HT1A and 5-HT2B serotonin receptors. It demonstrates a pEC50 of 8.90 at D2 receptors, 8.09 at D3 receptors, and 6.28 at 5-HT1A receptors, significantly inhibiting forskolin-induced cAMP production and serotonin-induced Ca2+ release. This compound is valuable for research focused on psychiatric disorders such as schizophrenia and bipolar disorder type I. -
5-HT1/D2 Agonist
Sarizotan is a potent agonist of the serotonin 5-HT1A receptor and dopamine D2 receptor. 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. Its biological activity makes it suitable for research applications involving neuropharmacology and psychiatric disorders, contributing to the understanding of serotonergic and dopaminergic functions. -
Dopamine/5-HT Modulator
Brilaroxazine is a potent multimodal modulator targeting dopamine (DA) and serotonin (5-HT) receptors. It acts as a partial agonist at DA D2, D3, and D4 receptors, and 5-HT1A (Ki=1.5 nM) and 5-HT2A (Ki=2.5 nM) receptors, while exhibiting antagonist properties at 5-HT2B (Ki=0.19 nM) and 5-HT7 (Ki=2.7 nM) receptors. As an atypical antipsychotic, Brilaroxazine demonstrates promise in enhancing cognitive function in various neuropsychiatric and neurological conditions in vivo. -
Metabolite Of Cariprazine
Didesmethyl cariprazine is a metabolite of Cariprazine that acts as a partial agonist at D2 and D3 dopamine receptors while serving as a full agonist at the 5-HT1A receptor and an antagonist at the 5-HT2B receptor. With Ki values of 1.41 nM, 0.056 nM, 1.7 nM, and 0.52 nM for human D2L, human D3, human 5-HT1A, and human 5-HT2B, respectively, Didesmethyl cariprazine demonstrates significant interactions with these targets. This compound has been shown to dose-dependently inhibit the spontaneous activity of rat midbrain dopaminergic neurons, making it valuable for research in neuropharmacology and behavioral studies. -
Dopamine Receptor Antagonist
Nemonapride is a highly potent antagonist of the dopamine D2 receptor, exhibiting a Ki of 0.06 nM. Additionally, it activates the 5-HT1A receptor with an IC50 of 34 nM. This compound functions as an antipsychotic and efficiently crosses the blood-brain barrier, demonstrating significant neuroleptic effects in animal models. It is valuable for research focused on neuropharmacology and the mechanisms underlying psychiatric disorders. -
Stable Isotope
Chlorpromazine-d6 hydrochloride is a deuterated derivative of Chlorpromazine, primarily functioning as a dopamine receptor antagonist. This stable isotope is utilized in biochemical and pharmacological research to explore the interactions and mechanisms of action of antipsychotic agents. Its ability to inhibit serotonin receptors, potassium channels, and sodium channels makes it valuable for studying neuropharmacology and drug metabolism. -
Dopamine Receptor Antagonist
LE 300 is a potent and selective antagonist of the dopamine D1-like receptors, demonstrating inhibition constants (Kis) of 1.9 nM and 7.5 nM for human dopamine D1 and D5 receptors, respectively. Additionally, LE 300 acts as an antagonist of the 5-HT2A receptor, with a pA2 value of 8.32 in rat tail artery assays. This compound is valuable for research into dopamine receptor signaling pathways and neuropharmacology. -
Antipsychotic Agent
Cariprazine-d6 is a deuterium-labeled derivative of the antipsychotic agent, Cariprazine. It functions primarily as a potent antagonist at the D3 (Ki of 0.085 nM) and D2 (Ki of 0.49 nM) dopamine receptors, while also exhibiting moderate affinity for the 5-HT1A receptor (Ki of 2.6 nM). This compound is valuable for research into the mechanisms of antipsychotic action and the pharmacokinetics of labeled compounds. -
5-HT Agonist/D2 Antagonist
Quetiapine-d4 hemifumarate is a deuterated form of Quetiapine, functioning as a 5-HT receptor agonist and a D2 dopamine receptor antagonist. This compound exhibits notable antidepressant and anxiolytic properties, making it valuable for research into mood disorders and anxiety treatment. Its unique isotopic labeling allows for advanced studies in pharmacokinetics and metabolic pathways of Quetiapine. -
D2/5-HT1A Agonist
Aripiprazole monohydrate is a potent partial agonist of the dopamine D2 receptor and an inverse agonist at the 5-HT2B and 5-HT2A receptors. Additionally, it exhibits partial agonist functionality at 5-HT1A, 5-HT2C, D3, and D4 receptors. This compound is primarily utilized in research focused on schizophrenia and has also been explored for potential applications in treating COVID-19. -
Dopamine Receptor Agonist
TDHL (Tergurid) is a potent dopamine receptor agonist, exhibiting a Kd of 0.39 nM for the D2 receptor, and functions as an orally bioavailable 5-HT2 receptor antagonist. Its dual mechanism of action allows for comprehensive exploration in neuropharmacology studies. TDHL is suitable for investigating the role of dopamine signaling in various neurological and psychiatric disorders. -
Stable Isotope
Brexpiprazole S-oxide-d8 is a deuterium-labeled analog of Brexpiprazole S-oxide, the primary metabolite of the atypical antipsychotic Brexpiprazole. This compound acts as a partial agonist at human 5-HT1A and dopamine receptors, with inhibition constants (Kis) of 0.12 nM and 0.3 nM, respectively. Additionally, it functions as an antagonist at the 5-HT2A receptor, exhibiting a Ki of 0.47 nM. Brexpiprazole S-oxide-d8 is valuable for pharmacokinetic studies and metabolic profiling in research applications focused on psychiatric disorders. -
Dopamine D2/D3 Receptor Antagonist
Esamisulpride is a potent antagonist of the dopamine D2 and D3 receptors, exhibiting Ki values of 4.43 nM for D2R and 0.72 nM for D3R. Additionally, it functions as a 5-HT7 receptor antagonist with a Ki of 900 nM. This compound is primarily employed in research related to schizophrenia and depression, providing valuable insights into dopaminergic and serotonergic system modulation. -
5-HT/dopamine receptor Antagonist
Ziprasidone amino acid is a known impurity of Ziprasidone, functioning primarily as a 5-HT (serotonin) and dopamine receptor antagonist. This compound demonstrates significant antipsychotic activity, making it valuable in the study of neurological disorders. Its unique properties can aid researchers in investigating the mechanisms of antipsychotic effectiveness and receptor interactions in related drug development. -
5-HT Agonist/D2 Antagonist
Quetiapine-d4 fumarate is a deuterium-labeled derivative of Quetiapine fumarate, primarily acting as a 5-HT receptor agonist and D2 dopamine receptor antagonist. This compound exhibits significant antidepressant and anxiolytic effects, making it valuable for research into mood disorders and anxiety-related conditions. Quetiapine-d4 fumarate is useful in pharmacokinetic studies and drug metabolism research, providing insights into the bioavailability and therapeutic potential of the parent compound. -
Dopamine receptor Agonist, 20S proteasome Activator
Apomorphine hydrochloride is a potent dopamine receptor agonist and a known activator of the 20S proteasome. It enhances proteasomal and insulin-degrading enzyme activities, facilitating the degradation of intracellular amyloid-beta (Aβ), phosphorylated tau (p-tau), and p53, thereby reducing their levels in neuronal cells. This compound is particularly relevant for research focused on neurodegenerative disorders such as Alzheimer's disease and psychiatric conditions including schizophrenia. -
D1-like Dopamine-Receptor Antagonist
SKF-83566 hydrobromide is a selective antagonist of the D1-like dopamine receptors, exhibiting high blood-brain barrier permeability and oral bioavailability. This compound functions as a competitive inhibitor of the dopamine transporter (DAT), with an IC50 of 5.7 μM, and demonstrates a weaker antagonistic effect on the vascular 5-HT2 receptor (Ki=11 nM). Additionally, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it a valuable tool for studying Parkinson's disease and nicotine dependence. -
D3R/5-HT2AR Antagonist/5-HT1AR Agonist
D3/5-HT receptor modulator-1 is a selective antagonist for dopamine D3 receptors and 5-HT2A receptors, while also functioning as a partial agonist at 5-HT1A receptors. With measured Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the respective targets, this compound exhibits a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. Its unique pharmacological profile suggests potential applications in the development of atypical antipsychotic therapies and for studying dopaminergic and serotonergic signaling pathways. -
Ziprasidone Impurity
Keto Ziprasidone is a known impurity of the antipsychotic agent Ziprasidone, which functions primarily as a combined antagonist of serotonin (5-HT) and dopamine receptors. This compound is crucial for research applications focusing on drug metabolism and pharmacokinetics, particularly in understanding the potential effects of impurities on therapeutic efficacy and safety profiles. Its analysis can aid in the development of quality control measures in pharmaceutical formulations. -
5-HT(6/7/2A)/ Dopamin D2 Receptors Antagonist
5-HT6/7 Antagonist 1 is a potent antagonist of the 5-HT6, 5-HT7, and D2 receptors, exhibiting selectivity that spares M1 receptors and hERG channels. This compound's multifunctional activity makes it valuable for research into neuropharmacology and the modulation of serotonergic and dopaminergic systems. It provides a useful tool for studying disorders related to these receptor pathways, including anxiety, depression, and schizophrenia. -
Ziprasidone Impurity
Hydroxy ziprasidone is a known impurity of the antipsychotic agent ziprasidone, which functions primarily as a combined antagonist of both serotonin (5-HT) and dopamine receptors. This compound is useful for researchers studying the pharmacological properties and metabolic pathways of ziprasidone, as well as for quality control in the synthesis of pharmaceutical formulations. Its presence can provide insights into the drug's safety, efficacy, and potential side effects. -
Dopamine D2/D3/5-HT7 Receptor Inhibitor
LB-102 is an orally bioavailable inhibitor of dopamine D2, D3, and 5-HT7 receptors. It exhibits significant antagonistic activity, making it a valuable tool for investigating the neurochemical pathways involved in schizophrenia and other psychiatric disorders. This compound is useful for studies aimed at understanding the role of these receptors in various neuropsychiatric conditions. -
5-HT Receptor Antagonist
Clocapramine is a selective antagonist of the 5-HT2A receptor, with additional inhibitory effects on D2 dopamine receptors. This compound exhibits notable properties in modulating serotonin and dopamine signaling, making it relevant for neuropharmacological research. Clocapramine can be utilized in studies related to psychiatric disorders, including depression and schizophrenia, as well as the characterization of receptor interactions in neural pathways.
