Dopamine Receptor Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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.
Frontiers in Microbiology, November 01, 2022, 979904
Frontiers in Microbiology, November 01 2022, 979904
Frontiers in Pharmacology, April 08 2025, 1539032
S2529 Dopamine HCl Dopamine HCl(ASL279, NSC 173182) is a catecholamine neurotransmitter present in a wide variety of animals,And a dopamine D1-5 receptors agonist.
iScience, 2023, 26(3):106241
Cell Rep Methods, 2023, 3(10):100599
Front Microbiol, 2022, 13:979904
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.
BMC Pharmacology and Toxicology, 2024, 25
Frontiers in Microbiology, 2022, 979904
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
S2461 Domperidone Domperidone is an oral dopamine D2 receptor antagonist, used to treat nausea and vomiting. This compound acts by blocking dopamine receptors, which helps to reduce symptoms of gastrointestinal distress. It is often prescribed for its antiemetic effects.
Biomolecules, November 15, 2025, 1603
Cancer Research, March 01, 2021, 1398-1412
Biomolecules, 2025, 1603
S2451 Amantadine HCl Amantadine HCl has antiviral and anti-parkinsonian activities and is used to treat or prevent respiratory infections caused by certain viruses. It is also widely used in the treatment of Parkinson's disease.
Frontiers in Microbiology, November 01, 2022, 979904
J Immunother Cancer, 2024, 12(11)e009805
Frontiers in Microbiology, 2022, 979904
S2104 Levosulpiride Levosulpiride(RV-12309,S-(-)-Sulpiride) is a selective antagonist for D2 dopamine receptors used as an antipsychotic and prokinetic agent.
Molecular Psychiatry, 2025, 1-14
Mol Psychiatry, 2025, 10.1038/s41380-025-03374-6
Frontiers in Microbiology, 2022, 979904
S4569 Fluphenazine dihydrochloride Fluphenazine dihydrochloride (Prolixin) is a phenothiazine-class D1DR and D2DR inhibitor. It also inhibits Histamine H1 Receptor.
Frontiers in Microbiology, November 01, 2022, 979904
Nucleic Acid Therapeutics, 2023, 248-264
bioRxiv (Preprint), 2023, nan
S4618 Fenoldopam mesylate Fenoldopam (SKF 82526, Corlopam) is a selective dopamine-1 receptor (DA1) agonist with natriuretic/diuretic properties. It lowers blood pressure through arteriolar vasodilation.
J Immunother Cancer, 2024, 12(11)e009805
Journal for ImmunoTherapy of Cancer, 2024, e009805
iScience, 2024, 109587
S4151 Penfluridol Penfluridol (TLP-607,R-16341) is a highly potent, first generation diphenylbutylpiperidine antipsychotic.
Frontiers in Microbiology, November 2022, 979904
Acta Pharmaceutica Sinica B, March 2022, 1271-1287
Translational Oncology, December 2025, 102559
S4631 Prochlorperazine dimaleate salt Prochlorperazine dimaleate salt is a dopamine (D2) receptor antagonist.
Cancer Biology & Therapy, October 25, 2023, 2269637
Frontiers in Microbiology, November 01, 2022, 979904
EMBO Molecular Medicine, December 23, 2025, 433-461
S2011 Pramipexole 2HCl Monohydrate Pramipexole 2HCl Monohydrate is a novel non-ergoline dopamine (DA) agonist, used to treat Parkinson's disease.
British Journal of Pharmacology, 2024, 3336-3352
Front Microbiol, 2022, 13:979904
Autophagy, 2016, 12(12):2374-2385
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
Frontiers in Microbiology, 2022, 979904
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
Nature Biotechnology, 2024, 1515-1525
Molecular Pain, 2021, 17448069211042117
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
Scientific Reports, 2024, 4820
E4910 Cariprazine Cariprazine(RGH-188, MP-214) acts primarily as a partial agonist at dopamine receptors, with pKi values of 10.07 for D3, 9.16 for D2L, and 9.31 for D2S receptors. It also acts as an antagonist forserotonin receptors, with pKi of 9.24, 8.59, 7.73, and 6.87 for5-HT2B,5-HT1A, 5-HT2A, and 5-HT2C receptors, respectively.
ACS Pharmacology & Translational Science, October 25, 2022, 1086-1096
Journal of Developmental Biology, June 27, 2025, 22
Journal of Developmental Biology, 2025, 22
S8097 C-DIM12 C-DIM12 is a Nurr1 activator that stimulates this compound mediated apoptosis axis in bladder cancer cells and tumors and inhibits NF-κB–dependent gene expression in glial cells.
Frontiers in Molecular Neuroscience, 2020, 64
Frontiers in Molecular Neuroscience, 2020, 64
Front Mol Neurosci, 2020, 23724
S5842 Cabergoline Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor.
Neuro-Oncology, 2025, 727-742
iScience, 2024, 27(10):110862
Cells, 2022, 3344
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
S1920 Haloperidol Haloperidol (Haldol) is an antipsychotic and butyrophenone.
Clinical Cancer Research, August 15, 2023, 3172-3188
Front Microbiol, 2022, 13:979904
Sci Adv, 2022, 8(15):eabk2376
S2460 Pramipexole Pramipexole (SND 919,Mirapexin,Sifrol,Mirapex) is a partial/full D2S, D2L, D3, D4 receptor agonist with a Ki of 3.9, 2.2, 0.5 and 5.1 nM for D2S, D2L, D3, D4 receptor, respectively.
Metabolites, 2022 Jan 21, 101
Front Microbiol, 2022, 13:979904
Metabolites, 2022, 12(2)101
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.
Cancer Discovery, 2025, 202-226
PLoS One, 2024, 19(12):e0316179
Ther Adv Chronic Dis, 2021, 12:2040622321998139
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
S6853 ONC206 ONC206 is a selective antagonist of DRD2/3/4 with broad-spectrum anti-tumor activity.
bioRxiv, 2026 Feb 20, 2026.02.19.706776
Neoplasia, 2023, 39:100894
Pharmacology Research & Perspectives, 2022 Aug, e00993
S2089 Fenoldopam Fenoldopam (SKF 82526) is a selective dopamine-1 (DA1) receptor agonist with natriuretic/diuretic properties with EC50 of 55.5 nM in stimulating cAMP accumulation in LLC-PK1 cells, which is more potent than DA .
iScience, 2024, 27(4):109587
iScience, 2024, 109587
Oncogene, 2016, 3103–3113
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
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
Nature Chemical Biology, 2021, 659-670
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
Molecular Pain, 2021, 17448069211042117
S7993 SKF38393 HCl SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.
Sci Rep, 2024, 14(1):4820
JCI Insight, 2023, 8(16)e170434
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
Frontiers in Microbiology, 2022, 979904
Mol Pharmacol, 2022, 101(4):236-245
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
iScience, 2025, 113292
S4274 Rotigotine Rotigotine(N-0923) is a dopamine receptor agonist, used in the treatment of Parkinson's disease and restless legs syndrome.
Front Microbiol, 2022, 13:979904
Frontiers in Microbiology, 2022, 979904
Frontiers in Microbiology, 2022, 979904
S3189 Ropinirole HCl Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.
Frontiers in Microbiology, November 1, 2022, 979904
Frontiers in Microbiology, November 01, 2022, 979904
Front Microbiol, 2022, 13:979904
S3163 Benztropine mesylate Benztropine(Cogentin mesylate, Benztropine methanesulfonate) is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
Cell Death & Disease, October 2025, 16(1)
Cell Death & Disease, October 06 2025, 691
Frontiers in Microbiology, November 01, 2022, 979904
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
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
S3656 Piribedil Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. This compound also has α2-adrenergic (α2A/α2C) antagonist properties.
Cell Rep Methods, 2023, 3(1):100381
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
S2168 PD128907 HCl PD 128907 HCl is a potent and selective dopamine D3 receptor agonist, with EC50 of 0.64 nM, exhibits 53-fold selectivity over dopamine D2 receptor.
Brain Behav Immun, 2021, 101:165-179
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.
Nucleic Acid Therapeutics, 2023 Aug, 248-264
Nucleic Acid Therapeutics, 2023, 248-264
S4933 Lithium carbonate Lithium carbonate (Li2CO3) is an inorganic compound that is valuable and effective agent in the treatment and prophylaxis of mood disorders, particularly bipolar disorder (BD). This compound is able to alter D2 dopamine receptors response.
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.
Clinical Cancer Research, August 15, 2023, 3195-3211
Clinical Cancer Research, August 15 2023, 3172-3188
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.
Frontiers in Microbiology, 2022, 979904
S7236 Cariprazine hydrochloride Cariprazine hydrochloride(RGH188 hydrochloride) is a novel antipsychotic agent and is a highly selective partial agonist of dopamineD2 and D3 and 5HT1A receptors, with preferential binding to the D3 receptor. It exhibits high selectivity and affinity to dopamine D3 (Ki = 0.085 nM) and D2 (Ki = 0.49 nM) receptors and has moderate affinity for the 5-HT1A receptor (Ki = 2.6 nM).
ACS Pharmacology & Translational Science, October 25, 2022, 1086-1096
Journal of Developmental Biology, June 27, 2025, 22
Fundamental & Clinical Pharmacology, July 4, 2022, 976-984
E4856 Rotigotine Hydrochloride Rotigotine Hydrochloride (N-0923 Hydrochloride) is a potent Agonist of dopamine receptor, with Ki values of 0.71 nM for dopamine D3 receptor, 4-15 nM for D2, D5, D4 receptors, and 83 nM for dopamine D1 receptor. It also acts as a partial agonist of the 5-HT1A receptor, and as an antagonist of the α2B-adrenergic receptor.
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.
S0104 Pardoprunox (SLV-308) hydrochloride Pardoprunox hydrochloride (DU-126891, SME-308) is a potent but partial dopamine D2 receptor agonist with pEC50 of 8.0, and a partial agonist in the induction of [35S]GTPγS binding with pEC50 of 9.2 and a serotonin 5-HT1A receptor agonist, with pEC50 of 6.3, respectively.
S5707 Aripiprazole lauroxil Aripiprazole lauroxil(Aristada) is an extended-release prodrug of aripiprazole designed for intramuscular injection. It acts as a dopamine-serotonin system stabilizer, with a potent partial agonist for dopamine D2 and serotonin 5-HT1A receptors while an antagonist for serotonin 5-HT2A receptors.
S5796 Vanoxerine dihydrochloride Vanoxerine (GBR-12909) is a potent and selective inhibitor of the presynaptic dopamine uptake complex.
Cells, 2019, 1531
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.
S4309 Bromocriptine Mesylate Bromocriptine mesylate is a dopamine receptor agonist with a Ki of 12.2 nM for D3 receptor and D2 receptor and a Ki of 1659 nM, 59.7 nM, 1691 nM for D1 receptor, D4 receptor, and D5 receptor, respectively. Bromocriptine mesylate is used in the treatment of Parkinson's disease, hyperprolactinemia-associated dysfunctions, and acromegaly.
PLoS One, March 02, 2017, e0173240
E4885 Dopamine Dopamine is a catecholamine neurotransmitter in the mammalian brain. It plays role as a modulator of cardiovascular function, catecholamine release, hormone secretion, vascular tone, renal function, and gastrointestinal motility.
Science Signaling, 2025, eads6584
Cancer Communications, 2020, 694-710
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.
S5066 Pramipexole dihydrochloride Pramipexole dihydrochloride (SND919) is a dopamine agonist of the non-ergoline class indicated for treating Parkinson's disease (PD) and restless legs syndrome (RLS) with Ki values of 3.9 nM, 2.2 nM, 0.5 nM and 5.1 nM for D2S receptor, D2L receptor, D3 receptor and D4 receptor.
E7427 Dehydroaripiprazole Dehydroaripiprazole (OPC-14857, DM-14857) is the active metabolite of aripiprazole, primarily metabolized by CYP3A4 and CYP2D6. It inhibits glutamate release from rat prefrontocortical nerve terminals by activating dopamine D2 and 5-HT1A receptors, reducing nerve terminal excitability and VDCC activation through a PKA-mediated signaling cascade, potentially contributing to its neuroprotective effects in excitotoxic injury.
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
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
S2452 Amfebutamone (Bupropion) HCl Amfebutamone (Bupropion) HCl(Wellbutrin) is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively.
Cancer Res Commun, 2025, 10.1158/2767-9764.CRC-24-0433
Front Microbiol, 2020, 10:2936
G3 (Bethesda), 2014, 4(6):1081-9
S3821 Nuciferine Nuciferine (Sanjoinine E, (-)-Nuciferine, VLT 049) is a major active aporphine alkaloid from the leaves of N. nucifera Gaertn and possesses anti-hyperlipidemia, anti-hypotensive, anti-arrhythmic, and insulin secretagogue activities. This compound is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
Int J Neuropsychopharmacol, 2025, pyaf019
Antioxidants (Basel), 2024, 13(6)714
Br J Pharmacol, 2021, 178(5):1182-1199
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
J Immunother Cancer, 2024, 12(11)e009805
mBio, 2022, e02177-21
Scientific Reports, 2017, 8491
S4086 Loxapine Succinate Loxapine Succinate(NSC 759578) is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Anticancer Research, February 2021, 687-697
Anticancer Research, 2021, 687-697
Anticancer Res, 2021, 41(2):687-697
S6301 MPP+ iodide MPP+ iodide (N-Methyl-4-Phenylpyridinium Iodide), the metabolite of a neurotoxin MPTP, causes symptom of Parkinson's disease (PD) in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ induces autophagic cell death in SH-SY5Y cells. MPP+ induces dopamine transporter (DAT) externalization in dopaminergic (DA) neurons, but internalization of serotonin transporter (SERT) in serotonergic (5-HT) neurons.
NPJ Parkinsons Dis, 2025, 11(1):3
Front Immunol, 2023, 14:1193081
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
S3854 Tetrahydropalmatine hydrochloride Tetrahydropalmatine (THP, Gindarine, 1-Tetrahydropalmitine) is an isoquinoline alkaloid found in several different plant species, mainly in the Corydalis genus (Yan Hu Suo), but also in other plants such as Stephania rotunda. It is a potent muscle relaxant. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
Mol Pain, 2021, 17:17448069211042117
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.
S0318 Ansofaxine hydrochloride Ansofaxine hydrochloride (LY03005, LPM570065), a triple reuptake inhibitor, inhibits serotonin, dopamine and norepinephrine reuptake with IC50 values of 723, 491 and 763 nM, respectively.
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.
S3913 Pimethixene maleate Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, 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.
Brain, 2017, 669-683
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.