Catalog No.
Product Name
Application
Product Information
Citations
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dopamine re-uptake inhibitor
Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI.- Alexander D H Kingdon, .et al. , J Antibiot (Tokyo), 2025, Jan;78(1):54-63 PMID: 39402358
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DAT and SLC6A2 inhibitor
GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.- Alexander D H Kingdon, .et al. , J Antibiot (Tokyo), 2025, Jan;78(1):54-63 PMID: 39402358
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dopamine D2 receptor agonist
UNC 9994 hydrochloride, unique, beta-arrestin-biased functionally selective dopamine D2 receptor (D2R) agonist (Ki value 30 nM; EC50 value 50 nM in ??-arrestin-2 recruitment assay) that exhibits antipsychotic activity in vivo. UNC9994 markedly inhibited PCP-induced hyperlocomotion in wild-type mice, which effect was completely abolished in ??-arrestin-2 knockout mice.- Anika Mann, .et al. , Sci Rep, 2021, Apr 15;11(1):8288 PMID: 33859231
- Reboxetine is an antidepressant compound that selectively inhibits norepinephrine uptake (IC50s = 8.2 and 1,070 nM for norepinephrine and serotonin transporters, respectively). It displays greater than 1,000-fold affinity for binding rat norepinephrine receptors compared to serotonin, histamine, acetylcholine, or dopamine receptors (Kis = 1.1, 129, 1,400, 3,900, and >10,000 nM, respectively).
- Antonia Donat, .et al. , iScience, 2023, Aug 29;26(10):107761 PMID: 37720081
- Domperidone blocks the action of dopamine. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which, among others, regulates nausea and vomiting (area postrema on the floor of the fourth ventricle and rhomboid fossa).
- Claudia Alvarez Baron, .et al. , Sci Rep, 2025, Aug 16;15(1):29995 PMID: 40819150
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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H1 antagonist
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.- Keisuke Obara, .et al. , Biol Pharm Bull, 2021, 44, 1140-1150 PMID: 34334499
- Clozapine displays a broad range of pharmacological actions; the antipsychotic effects are thought to be mediated principally by 5-HT2A/2C and dopamine receptor blockade.
- Majid Momeny, .et al. , EMBO Mol Med, 2024, Jun 17 PMID: 38886591
- Madeleine S A Tan, .et al. , Mol Pharm, 2022, Sep 23 PMID: 36149013
- Madeleine S. A. Tan, .et al. , Gels, 2022, Jan; 8(1): 38 PMID: 35049572
- Milan D Valyear, .et al. , Nat Commun, 2020, Jul 28;11(1):3764 PMID: 32724058
- Yutaro Kobayashi, .et al. , Transl Psychiatry, 2019, 9:181 PMID: 31371697
- M.D. Valyear, .et al. , bioRxiv, 2018, 2018
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dopamine receptor agonist
Nalmefene hydrochloride is an opioid receptor antagonist.- Mark G Papich, .et al. , Drug Deliv Transl Res, 2022, Feb;12(2):376-383 PMID: 34817831
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Dopamine Receptor agonist
Rotigotine hydrochloride is a dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.- Mattia Ferraiolo, .et al. , Neuropharmacology, 2022, 207: 108942 PMID: 35026287
- Mattia Ferraiolo, .et al. , Eur J Pharmacol, 2021, Nov 15;911:174557 PMID: 34626593
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Dopamine Receptor antagonist
Paliperidone(Invega) is an atypical antipsychotic.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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dopamine D2 receptor antagonist
Metoclopramide HCl is a selective dopamine D2 receptor antagonist.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- BP 897, is an antagonist at human dopamine D3 receptors and at rat somatodendritic dopamine D3 receptors
- Shaowen Qian, .et al. , Nat Commun, 2022, Jul 22;13(1):4229 PMID: 35869064
- Shaowen Qian, .et al. , Nature Portfolio Journal, 2021, Oct 1
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D2 dopamine receptor antagonist
L-741626 is a potent and selective antagonist for the dopamine receptor D2. It has good selectivity over the related D3 and D4 subtypes and other receptors.- Yoon-Jin Kim, .et al. , Sci Adv, 2021, Feb 19;7(8) PMID: 33608268
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Dopamine Receptors Blocker
Trifluoperazine dimaleate is a potent dopamine receptor blocker, primarily indicated for research into antipsychotic mechanisms. This compound exhibits significant α1-adrenergic receptor antagonism and serves as an inhibitor of NUPR1, highlighting its potential anticancer properties. Additionally, trifluoperazine dimaleate functions as a calmodulin inhibitor and inhibits P-glycoprotein activity. Its versatile applications extend to studying schizophrenia and the reversible inhibition of influenza virus morphogenesis. -
Stable Isotope
Trifluoperazine-d3 dihydrochloride is a deuterated derivative of Trifluoperazine, primarily targeting dopamine receptors to exert its antipsychotic effects. This compound is a potent α1-adrenergic receptor antagonist and an effective inhibitor of NUPR1, showcasing anticancer properties. Additionally, it functions as a calmodulin inhibitor and can interfere with P-glycoprotein activity. Trifluoperazine-d3 dihydrochloride is valuable for research applications related to schizophrenia and serves as a reversible inhibitor of influenza virus morphogenesis. -
Autophagy Inducer
Cabergoline diphosphate is an ergot alkaloid that acts as an agonist of dopamine D2-like receptors, demonstrating high affinity for D2, D3, and 5-HT2B receptors with Ki values of 0.7, 1.5, and 1.2, respectively. It serves as an autophagy inducer, making it a valuable tool for research focused on cellular processes related to autophagy and neurobiology. This compound is instrumental in studies investigating neurodegenerative diseases and metabolic regulation, providing insights into the role of dopamine receptors in cellular homeostasis. -
Stable Isotope
Cabergoline-d6 is a stable isotope-labeled form of Cabergoline, an ergot-derived dopamine D2-like receptor agonist. This compound exhibits high affinity for dopamine receptors D2 and D3, as well as 5-HT2B receptors, with Ki values of 0.7, 1.5, and 1.2 nM respectively. Cabergoline-d6 is utilized in pharmacokinetic studies and metabolic research to investigate the behavior of Cabergoline in biological systems. -
D4R Antagonist
Dopamine D4 receptor ligand 3 is a selective antagonist of the dopamine D4 receptor (D4R), exhibiting a pKi of 8.86. It demonstrates significant activity with pIC50 values of 5.78, 5.55, and 6.17 for Go, Gi, and βArr2 signaling pathways in HEK-293T cells, respectively. Additionally, this compound has been shown to inhibit cell viability in three human glioma cell lines—U87 MG, T98G, and U251 MG—while also inducing reactive oxygen species (ROS) production and mitochondrial dysfunction in these glioma cells. This makes it a valuable tool for studying the role of D4R antagonism in cancer biology and neuropharmacology. -
Dopamine Receptors Blocker
Trifluoperazine is an antipsychotic agent primarily acting as a blocker of central dopamine receptors. It exhibits significant activity as a potent α1-adrenergic receptor antagonist and a NUPR1 inhibitor, demonstrating anticancer properties. Additionally, Trifluoperazine functions as a calmodulin inhibitor and inhibits P-glycoprotein, contributing to its diverse biological effects. This compound is utilized in research on schizophrenia and shows potential as a reversible inhibitor of influenza virus morphogenesis. -
Dopamine-mimetic Probe
DAyne is a dopamine-mimetic probe that covalently interacts with proteins modified by dopamine oxidation products, such as dopaquinone, to create stable adducts. This compound is valuable for investigating the biochemical mechanisms underlying Parkinson’s disease, focusing on neurotoxicity and the modification of proteins. Its applications extend to exploring pathways affected by dopamine dysregulation, including endoplasmic reticulum stress and cytoskeletal instability. -
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.
