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Dopamine Receptor Antagonists

Cat.No. Product Name Information Product Use Citations Product Validations
S5749 Chlorpromazine (CPZ) Chlorpromazine (CPZ) is a low-potency typical antipsychotic agent that is used to treat psychotic disorders such as schizophrenia. Chlorpromazine (CPZ) inhibits 5-HT(2A) receptor and dopamine D2 in vitro. Chlorpromazine (CPZ) also inhibits sodium channel and blocks HERG potassium channels with IC50 of 21.6 μM.
EMBO J, 2025, 10.1038/s44318-025-00537-7
Mol Psychiatry, 2025, 10.1038/s41380-025-03374-6
J Thromb Haemost, 2025, 23(9):2926-2943
S4151 Penfluridol Penfluridol (TLP-607,R-16341) is a highly potent, first generation diphenylbutylpiperidine antipsychotic.
Signal Transduct Target Ther, 2025, 10(1):341
Transl Oncol, 2025, 62:102559
Acta Pharm Sin B, 2022, 12(3):1271-1287
S4631 Prochlorperazine dimaleate salt Prochlorperazine dimaleate salt is a dopamine (D2) receptor antagonist.
Cell Rep Med, 2025, 6(11):102421
Cancer Biol Ther, 2023, 24(1):2269637
Cancer Biol Ther, 2023, 10.1080/15384047.2023.2269637
S1763 Quetiapine (ICI-204636) fumarate Quetiapine Fumarate (ICI-204636) is an atypical antipsychotic used in the treatment of schizophrenia, bipolar I mania, bipolar II depression, bipolar I depression and shows affinity for various neurotransmitter receptors including serotonin, dopamine, histamine, and adrenergic receptors.
Front Microbiol, 2022, 13:979904
Clin Transl Sci, 2021, 10.1111/cts.13012
J Cancer Res Clin Oncol, 2019, 145(6):1495-1507
S4655 Sulpiride Sulpiride (Dolmatil, Dobren, Sulpyrid, Aiglonyl, Dogmatil) is a dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid.
Front Mol Biosci, 2024, 11:1423351
Sci Rep, 2024, 14(1):4820
Front Microbiol, 2022, 13:979904
S4358 Pimozide Pimozide (Orap, R6238) is an antagonist of Dopamine Receptors with Ki of 0.83 nM, 3.0 nM and 6600 nM for dopamine D3, D2 and D1 receptors, respectively. This compound also exhibits binding affinity at 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. It is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Mol Metab, 2025, 91:102069
Oncogenesis, 2025, 14(1):31
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
S5862 Metoclopramide Metoclopramide is a dopamine antagonist used for the treatment of nausea and vomiting.
J Control Release, 2025, 380:417-432
BMC Pharmacol Toxicol, 2024, 25(1):25
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
S1280 Amisulpride Amisulpride (DAN-2163) is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.
Front Biosci (Landmark Ed), 2025, 30(5):38875
Alzheimers Dement, 2023, 10.1002/alz.13090
Front Microbiol, 2022, 13:979904
S1724 Paliperidone Paliperidone, the main active metabolite of Risperidone, is a potent serotonin-2A and dopamine-2 receptor antagonist, used in the treatment of schizophrenia.
Front Pharmacol, 2025, 16:1539032
Front Microbiol, 2022, 13:979904
Anticancer Res, 2021, 41(2):687-697
S1920 Haloperidol Haloperidol (Haldol) is an antipsychotic and butyrophenone.
Front Microbiol, 2022, 13:979904
Sci Adv, 2022, 8(15):eabk2376
Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2
S4096 Droperidol Droperidol (NSC 169874,Dehydrobenzperidol) is a potent antagonist of dopamine subtype 2 receptors in the limbic system.
Eur J Pharmacol, 2024, 985:177058
Front Microbiol, 2022, 13:979904
Sci Rep, 2018, 8(1):15753
S2104 Levosulpiride Levosulpiride(RV-12309,S-(-)-Sulpiride) is a selective antagonist for D2 dopamine receptors used as an antipsychotic and prokinetic agent.
Mol Psychiatry, 2025, 10.1038/s41380-025-03374-6
Front Microbiol, 2022, 13:979904
Sci Rep, 2018, 8(1):15753
S5714 lurasidone Lurasidone (SM-13496) is a second-generation antipsychotic agent that exhibits full antagonism at dopamine D2 and serotonin 5-HT2A receptors with binding affinities Ki = 1 nM and Ki = 0.5 nM, respectively. This compound also has high affinity for serotonin 5-HT7 receptors (Ki = 0.5 nM), partial agonist activity at 5-HT1A receptors (Ki = 6.4 nM) and lacks affinity for histamine H1 and muscarinic M1 receptors.
Alzheimers Dement, 2023, 10.1002/alz.13090
Chem Biol Drug Des, 2022, 100(5):699-721
bioRxiv, 2021, 10.1101/2021.11.14.468520
S0476 SCH-23390 hydrochloride SCH-23390 hydrochloride (R-(+)-SCH-23390, SCH-23390) is a highly potent and selective dopamine D1-like receptor antagonist with Ki of 0.2 nM and 0.3 nM for the D1 and D5 dopamine receptor subtypes, respectively. This compound is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. It directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.
Behav Brain Funct, 2025, 21(1):22
Theranostics, 2023, 13(10):3149-3164
JCI Insight, 2023, 8(16)e170434
S4289 Metoclopramide HCl Metoclopramide HCl(Metoclopramide hydrochloride) is a selective dopamine D2 receptor antagonist, used for the treatment of nausea and vomiting.
Front Microbiol, 2022, 13:979904
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
Pharmazie, 2021, 76(4):172-174
S1771 Chlorprothixene Chlorprothixene(Minithixen,Truxal) has strong binding affinities to dopamine and histamine receptors, such as D1, D2, D3, D5, H1, 5-HT2, 5-HT6 and 5-HT7, with Ki of 18 nM, 2.96 nM, 4.56 nM, 9 nM, 3.75 nM, 9.4 nM, 3 nM and 5.6 nM, respectively.
Front Microbiol, 2022, 13:979904
Sci Rep, 2018, 8(1):15753
S5324 6-OHDA (Oxidopamine hydrobromide) 6-OHDA (Oxidopamine hydrobromide) is a neurotoxic synthetic organic compound that acts as an antagonist of the neurotransmitter dopamine with potential antineoplastic activity. 6-OHDA (Oxidopamine hydrobromide) can be used to induce animal models of Parkinson's Disease.Solutions are unstable and should be fresh-prepared.
PLoS One, 2024, 19(12):e0316179
Ther Adv Chronic Dis, 2021, 12:2040622321998139
S5949 Metoclopramide hydrochloride hydrate Metoclopramide hydrochloride (Clorpa, Gimoti, Maxolon, Reglan) hydrate is primarily a Dopamine receptor antagonist, with 5HT3 receptor antagonist and 5HT4 receptor agonist activity, and used as an antiemetic and gastroprokinetic.
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
Pharmazie, 2021, 76(4):172-174
S2437 Rotundine Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.
Mol Psychiatry, 2025, 10.1038/s41380-025-03374-6
J Med Virol, 2019, 91(8):1440-1447
S4219 Azaperone Azaperone (NSC 170976) crosses the blood-brain barrier and binds to both DI and D2 receptors, being an antagonist of Dopamine receptors with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
Front Microbiol, 2022, 13:979904
Mol Pharmacol, 2022, 101(4):236-245
S6853 ONC206 ONC206 is a selective antagonist of DRD2/3/4 with broad-spectrum anti-tumor activity.
Neoplasia, 2023, 39:100894
Pharmacol Res Perspect, 2022, 10(4):e00993
S4251 Phenothiazine Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.
Front Pharmacol, 2024, 15:1407335
S3044 Lurasidone HCl Lurasidone (SM-13496) is an atypical antipsychotic, inhibits Dopamine D2, 5-HT2A, 5-HT7, 5-HT1A and noradrenaline α2C with IC50 of 1.68 nM, 2.03 nM, 0.495 nM, 6.75 nM and 10.8 nM, respectively.
Alzheimers Dement, 2023, 10.1002/alz.13090
S5559 (+/-)-tetrahydropalmatine (+/-)-tetrahydropalmatine, a plant alkaloid used as an ingredient in dietary supplement products, is a potent and selective D1 receptor antagonist.
Mol Pain, 2021, 17:17448069211042117
S5565 Triflupromazine hydrochloride Triflupromazine hydrochloride (Fluopromazine) is an antipsychotic medication of the phenothiazine class.
bioRxiv, 2020, 2020/9/20.4.7.30734
S5481 Molindone hydrochloride Molindone hydrochloride is the hydrochloride salt form of molindone, a conventional antipsychotic used in the therapy of schizophrenia. It is a dopamine D2/D5 receptor antagonist.
Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433
S1789 Tetrabenazine (Xenazine) Tetrabenazine(Xenazine,Ro 1-9569) acts primarily as a reversible high-affinity inhibitor of mono-amine uptake into granular vesicles of presynaptic neurons by binding selectively to VMAT-2; Also blocks dopamine D2 receptors, but this affinity is 1,000-fold lower than its affinity for VMAT-2.
Front Microbiol, 2022, 13:979904
E0125 Raclopride Raclopride is a selective dopamine D2/D3 receptor antagonist that discriminates between dopamine-mediated motor functions. This compound binds to D2 and D3 receptors with dissociation constants of between 1.8 nM and 3.5 nM, but has a very low affinity for D4 receptors.
iScience, 2025, 28(9):113292
S5624 Paliperidone Palmitate Paliperidone Palmitate (9-hydroxyrisperidone palmitate) is a palmitate ester of paliperidone, which is a dopamine antagonist and 5-HT2A antagonist of the atypical antipsychotic class.
Anticancer Res, 2021, 41(2):687-697
S9509 Tiapride Hydrochloride Tiapride is a drug that selectively blocks D2 and D3 dopamine receptors in the brain and is used to treat a variety of neurological and psychiatric disorders.
Alzheimers Dement, 2023, 10.1002/alz.13090
S4731 Perphenazine Perphenazine (Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.
E7849 Haloperidol hydrochloride Haloperidol hydrochloride is an antagonist of dopamine receptors with selectivity for D2-like receptors. It is an antipsychotic used to treat the positive symptoms of schizophrenia caused by increased dopamine activity.
E1258 Pridopidine Pridopidine (ACR16, ASP2314, FR310826) , a dopamine (DA) stabilizer, acts as an antagonist against sigma 1 receptor (S1R) and dopamine D2 receptor (D2R).
S5399 Chlorprothixene hydrochloride Chlorprothixene HCl (Minithixen hydrochloride, Truxal hydrochloride, NSC 169899, NSC 56379, NSC 78193) is the hydrochloride salt form of chlorprothixene, a typical antipsychotic drug of the thioxanthene (tricyclic) class. It exerts strong blocking effects by blocking the 5-HT2 D1, D2, D3, histamine H1, muscarinic and alpha1 adrenergic receptors.
S9469 Haloperidol Decanoate Haloperidol decanoate (Halomonth) is a depot form of haloperidol with antipsychotic activity. It has potential to be used in the research of schizophrenia and schizoaffective disorder.
S4257 Alizapride HCl Alizapride HCl(Alizapride hydrochloride) is a dopamine receptor antagonist used for the theropy of nausea and vomiting.
S5034 Melitracen hydrochloride Melitracen hydrochloride (Thymeol) is a potential dopamine D1/2 receptor antagonist which has antidepressant properties.
E6049New Domperidone monomaleate Domperidone monomaleate (R33812 monomaleate) is a potent antagonist of dopamine D2 receptor that acts as an antiemetic and prokinetic agent by targeting the chemoreceptor trigger zone and motor function of the stomach and small intestine. It also inhibits cardiac Na⁺ channels such as Nav1.5, suggesting a potential molecular mechanism for cardiovascular side effects like malignant arrhythmias.
S6455 Clebopride malate Clebopride is a dopamine antagonist drug and is used to treat functional gastrointestinal disorder such as nausea or vomiting.
S5428 Promazine hydrochloride Promazine (Romtiazin, Sinophenin) is an antagonist at types 1, 2, and 4 dopamine receptors, 5-HT receptor types 2A and 2C, muscarinic receptors 1 through 5, alpha(1)-receptors, and histamine H1-receptors with antipsychotic effects.
S2493 Olanzapine Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Brain Behav Immun, 2025, 130:106111
Mol Psychiatry, 2025, 10.1038/s41380-025-03374-6
FASEB J, 2025, 39(3):e70355
Verified customer review of Olanzapine
S6887 Clozapine N-oxide (CNO chemical) CNO (Clozapine N-oxide) is a metabolite of Clozapine (GLXC-06516) and an agonist of human muscarinic designer receptors (Designer Receptors Exclusively Activated by Designer Drugs, DREADDs). Clozapine is a potent dopamine (DA) antagonist and a selective muscarinic M4 receptor agonist.Solutions are unstable and should be fresh-prepared.
Theranostics, 2025, 15(5):1822-1841
STAR Protoc, 2025, 6(1):103542
Theranostics, 2024, 14(7):2881-2896
S1444 Ziprasidone HCl Ziprasidone HCl (CP-88059) is a novel and potent dopamine and serotonin (5-HT) receptor antagonist, used in the treatment of schizophrenia and bipolar disorder.
UNIVERSITY OF PÉCS, 2023,
Anticancer Res, 2021, 41(2):687-697
Molecules, 2020, 25(18)E4206
Verified customer review of Ziprasidone HCl
S4086 Loxapine Succinate Loxapine Succinate(NSC 759578) is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Anticancer Res, 2021, 41(2):687-697
S4889 Perospirone hydrochloride Perospirone (SM-9018) is an atypical or second-generation antipsychotic of the azapirone family that antagonizes serotonin 5HT2A receptors and dopamine D2 receptors. It also displays affinity towards 5HT1A receptors as a partial agonist.
J Med Virol, 2023, 95(6):e28856
S5741 Quetiapine Quetiapine(ICI204636) is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder. This compound is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. It is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. This chemical has moderate to high affinity for the human D2, HT1A, 5-HT2A, 5-HT2C receptor with pKis of 7.23, 5.74, 7.54, 5.55.
S5153 Tetrahydroberberine Tetrahydroberberine (Canadine) is an isoquinoline alkaloid with micromolar affinity for dopamine D2 (antagonist, pKi = 6.08) and 5-HT1A (agonist, pKi = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors.
S5185 Perospirone Perospirone (SM-9018 free base) is an orally active antagonist of 5-hydroxytryptamine2 (5-HT2) receptor, dopamine2 (D2) receptor and 5-HT1A receptor with Ki of 0.6 nM, 1.4 nM and 2.9 nM, respectively.
E4840 Ziprasidone hydrochloride monohydrate Ziprasidone hydrochloride monohydrate is an antipsychotic drug, a combined antagonist of 5-HT (serotonin) and dopamine receptor. It exhibits binding affinities for D2, 5-HT2A, 5-HT1A with Ki values 4.8 nM, 0.42 nM, 3.4 nM respectively.
E0388 WQ 1 WQ 1 is a high affinity and selective σ1 receptor antagonist with pKi values of 10.85, 6.53 and 5.80 at σ1, σ2 receptors and dopamine transporter (DAT), displaying σ1/σ2 selectivity ratio of 20893.
S6410 Clemizole Clemizole, a first-generation histamine receptor (H1) antagonist, is a potent inhibitor of behavioural and electrographic seizure activity. It has a potential therapeutic effect on hepatitis C infection and also potently inhibits TRPC5 ion channels.
E4930 Asenapine Asenapine(Org 5222, HSDB8061) is a multi-target receptor antagonist. It acts as an antagonist of serotonin receptors with pKi values of 8.4-10.5, adrenoceptors with pKi values of 8.9-9.5, dopamine receptors with pKi values of 8.9-9.4 and histamine receptors with pKi values of 8.2-9.0.