Dopamine Receptor

Choose Selective Dopamine Receptor Inhibitors

Dopamine Receptor Signaling Pathway Map

Dopamine Receptor Signaling Pathways

Dopamine Receptor Products

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  • Dopamine Receptor Inhibitors (12)
  • Dopamine Receptor Antagonists (46)
  • Dopamine Receptor Agonists (18)
  • Dopamine Receptor Modulators (2)
  • New Dopamine Receptor Products
Catalog No. Product Name Information Product Use Citations Product Validations
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
S2452 Amfebutamone (Bupropion) HCl Amfebutamone (Bupropion) HCl is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively.
Front Microbiol, 2020, 10:2936
G3 (Bethesda), 2014, 4(6):1081-9
Georgia State University, 2014, Chaquettea Felton
S2456 Chlorpromazine HCl Chlorpromazine HCl (Sonazine) is a dopamine and potassium channel inhibitor with IC50 of 6.1 and 16 μM for inward-rectifying K+ currents and time-independent outward currents.
Emerg Microbes Infect, 2022, 11(1):1135-1144
Viruses, 2022, 14(3)496
Virus Res, 2022, 315:198794
S2461 Domperidone Domperidone is an oral dopamine D2 receptor antagonist, used to treat nausea and vomiting.
S3163 Benztropine mesylate Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
S3189 Ropinirole HCl Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.
S3201 Trifluoperazine 2HCl Trifluoperazine (NSC-17474, RP-7623, SKF-5019) 2HCl is a dopamine D2 receptor inhibitor with IC50 of 1.1 nM. Trifluoperazine also inhibits calmodulin (CaM).
Toxicol Appl Pharmacol, 2021, 424:115595
Toxicol Lett, 2021, 348:10-17
Anticancer Res, 2021, 41(2):687-697
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
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.
S4569 Fluphenazine dihydrochloride Fluphenazine dihydrochloride (Prolixin) is a phenothiazine-class D1DR and D2DR inhibitor. It also inhibits Histamine H1 Receptor.
bioRxiv, 2020, 2020/9/20.4.7.30734
Methods Mol Biol, 2017, 1513:119-140
S5796 Vanoxerine dihydrochloride Vanoxerine (GBR-12909) is a potent and selective inhibitor of the presynaptic dopamine uptake complex.
S5856 Trifluoperazine Trifluoperazine (NSC-17474, RP-7623, SKF-5019) is an FDA-approved antipsychotic drug for schizophrenia. It is an inhibitor of calmodulin (CaM) and Dopamine D2 receptor with an IC50 value of 1.2 nM for D2 receptor.
Toxicol Appl Pharmacol, 2021, 424:115595
Toxicol Lett, 2021, 348:10-17
Biomed Chromatogr, 2021, e5205
E0125New Raclopride Raclopride is a selective dopamine D2/D3 receptor antagonist that discriminates between dopamine-mediated motor functions. Raclopride 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.
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. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.
S1280 Amisulpride Amisulpride (DAN-2163) is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.
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.
Anticancer Res, 2021, 41(2):687-697
Molecules, 2020, 25(18)E4206
Nature, 2018, 560(7718):372-376
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.
Anticancer Res, 2021, 41(2):687-697
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.
Clin Transl Sci, 2021, 10.1111/cts.13012
J Cancer Res Clin Oncol, 2019, 145(6):1495-1507
Toxicol Lett, 2019, 313:77-90
S1771 Chlorprothixene Chlorprothixene 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.
Sci Rep, 2018, 8(1):15753
S1789 Tetrabenazine (Xenazine) Tetrabenazine(Nitoman, Xenazine) 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.
S1920 Haloperidol Haloperidol (Haldol) is an antipsychotic and butyrophenone.
Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2
S2104 Levosulpiride Levosulpiride is a selective antagonist for D2 dopamine receptors used as an antipsychotic and prokinetic agent.
Sci Rep, 2018, 8(1):15753
S2437 Rotundine Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.
J Med Virol, 2019, 91(8):1440-1447
S2493 Olanzapine Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Nat Protoc, 2021, 10.1038/s41596-021-00624-z
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Pharmacol Res, 2021, 170:105714
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.
S4086 Loxapine Succinate Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Anticancer Res, 2021, 41(2):687-697
S4096 Droperidol Droperidol (NSC 169874) is a potent antagonist of dopamine subtype 2 receptors in the limbic system.
Sci Rep, 2018, 8(1):15753
S4151 Penfluridol Penfluridol (TLP-607) is a highly potent, first generation diphenylbutylpiperidine antipsychotic.
Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.09.007
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.
Mol Pharmacol, 2022, 101(4):236-245
S4251 Phenothiazine Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.
S4257 Alizapride HCl Alizapride HCl is a dopamine receptor antagonist used for the theropy of nausea and vomiting.
S4289 Metoclopramide HCl Metoclopramide HCl is a selective dopamine D2 receptor antagonist, used for the treatment of nausea and vomiting.
Pharmazie, 2021, 76(4):172-174
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. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S4631 Prochlorperazine dimaleate salt Prochlorperazine dimaleate (Prochlorperazin, Compazine, Capazine, Stemetil) is a dopamine (D2) receptor antagonist.
F1000Res, 2016, 5:150
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.
Nat Commun, 2020, 11(1):941
S4731 Perphenazine Perphenazine (Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.
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.
S5034 Melitracen hydrochloride Melitracen hydrochloride (Thymeol) is a potential dopamine D1/2 receptor antagonist which has antidepressant properties.
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.
S5197 Loxapine Loxapine (Adasuve), a typical neuroleptic, is a drug with D2/D3 receptor antagonist activity and a higher affinity for D3 than D2. Loxapine displays an extremely strong binding affinity for dopamine D4 and serotonin 5-HT2 receptors.
S5324 Oxidopamine hydrobromide Oxidopamine (6-hydroxydopamine, 6-OHDA, 2,4,5-trihydroxyphenethylamine) is a neurotoxic synthetic organic compound that acts as an antagonist of the neurotransmitter dopamine with potential antineoplastic activity. Solutions should be freshly prepared and protected from exposure to light.
Ther Adv Chronic Dis, 2021, 12:2040622321998139
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.
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.
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.
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
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
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. It 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.
S5741 Quetiapine Quetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine have 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.
S5749 Chlorpromazine 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.
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
Pharmaceuticals (Basel), 2022, 15(2)241
Viruses, 2022, 14(3)496
S5862 Metoclopramide Metoclopramide is a dopamine antagonist used for the treatment of nausea and vomiting.
Pharmazie, 2021, 76(4):172-174
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.
Pharmazie, 2021, 76(4):172-174
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.
S6455 Clebopride malate Clebopride is a dopamine antagonist drug and is used to treat functional gastrointestinal disorder such as nausea or vomiting.
S6853 ONC206 ONC206 is a selective antagonist of dopamine D2-like receptors (DRD2/3/4) with broad-spectrum anti-tumor activity.
S6887 Clozapine N-oxide Clozapine N-oxide (CNO) 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.
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.
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.
S1726 Levodopa Levodopa is the precursor to the neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine (adrenaline), used to treat Parkinson's symptoms.
PLoS One, 2017, 12(3):e0173240
S2011 Pramipexole 2HCl Monohydrate Pramipexole 2HCl Monohydrateis a novel non-ergoline dopamine (DA) agonist, used to treat Parkinson's disease.
Autophagy, 2016, 12(12):2374-2385
S2089New 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 .
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
S2451 Amantadine HCl Amantadine HCl (1-adamantanamine) is used to treat or prevent infections of the respiratory tract caused by a certain virus.
Ecotoxicol Environ Saf, 2021, 211:111900
Adv Ther (Weinh), 2020, 2000034
S2460 Pramipexole Pramipexole (SND 919) 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.
S2529 Dopamine HCl Dopamine HCl is a catecholamine neurotransmitter present in a wide variety of animals,And a dopamine D1-5 receptors agonist.
Cell, 2021, 184(4):943-956.e18
Cancer Commun (Lond), 2020, 10.1002/cac2.12103
Brain, 2019, 142(3):700-718
S3656 Piribedil Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties.
S3664 Flupentixol dihydrochloride Flupentixol (Flupenthixol) dihydrochloride, an antipsychotic neuroleptic drug, is a powerful antagonist of both D1 and D2 dopamine receptors and also an alpha-adrenergic receptor antagonist.
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. Nuciferine 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.
Br J Pharmacol, 2021, 178(5):1182-1199
Tohoku J Exp Med, 2021, 254(1):17-23
S4274 Rotigotine Rotigotine is a dopamine receptor agonist, used in the treatment of Parkinson's disease and restless legs syndrome.
Cell Death Dis, 2019, 10(9):649
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.
S4639 Brexpiprazole Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.
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.
S5842 Cabergoline Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor.
S5849 Cariprazine HCl Cariprazine (RGH-188), a novel second-generation antipsychotic, is a D3-preferring dopamine D2/D3 receptor partial agonist.
Eur J Pharmacol, 2021, 911:174557
S7993 SKF38393 HCl SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.
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). Lithium carbonate is able to alter D2 dopamine receptors response.
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.
S3188 (+,-)-Octopamine HCl Octopamine (OA), a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates.
S4732 MPTP hydrochloride MPTP hydrochloride is a dopaminergic neurotoxin and cause selective destruction of dopaminergic neurons in animal models of parkinsonism. MPTP hydrochloride induces apoptosis.
Free Radic Biol Med, 2022, 181:82-97
Front Pharmacol, 2022, 13:848813
Neurosci Lett, 2022, 782:136638
S8097 C-DIM12 C-DIM12 is Nurr1 activator that stimulates Nurr1 mediated apoptosis axis in bladder cancer cells and tumors and inhibits NF-κB–dependent gene expression in glial cells.
Front Mol Neurosci, 2020, 23724
Cell Death Dis, 2018, 9(3):411
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
S2452 Amfebutamone (Bupropion) HCl Amfebutamone (Bupropion) HCl is a selective norepinephrine-dopamine reuptake inhibitor with IC50 of 6.5 and 3.4 μM for the reuptake of dopamine and norepinephrine, respectively.
Front Microbiol, 2020, 10:2936
G3 (Bethesda), 2014, 4(6):1081-9
Georgia State University, 2014, Chaquettea Felton
S2456 Chlorpromazine HCl Chlorpromazine HCl (Sonazine) is a dopamine and potassium channel inhibitor with IC50 of 6.1 and 16 μM for inward-rectifying K+ currents and time-independent outward currents.
Emerg Microbes Infect, 2022, 11(1):1135-1144
Viruses, 2022, 14(3)496
Virus Res, 2022, 315:198794
S2461 Domperidone Domperidone is an oral dopamine D2 receptor antagonist, used to treat nausea and vomiting.
S3163 Benztropine mesylate Benztropine is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
S3189 Ropinirole HCl Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.
S3201 Trifluoperazine 2HCl Trifluoperazine (NSC-17474, RP-7623, SKF-5019) 2HCl is a dopamine D2 receptor inhibitor with IC50 of 1.1 nM. Trifluoperazine also inhibits calmodulin (CaM).
Toxicol Appl Pharmacol, 2021, 424:115595
Toxicol Lett, 2021, 348:10-17
Anticancer Res, 2021, 41(2):687-697
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
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.
S4569 Fluphenazine dihydrochloride Fluphenazine dihydrochloride (Prolixin) is a phenothiazine-class D1DR and D2DR inhibitor. It also inhibits Histamine H1 Receptor.
bioRxiv, 2020, 2020/9/20.4.7.30734
Methods Mol Biol, 2017, 1513:119-140
S5796 Vanoxerine dihydrochloride Vanoxerine (GBR-12909) is a potent and selective inhibitor of the presynaptic dopamine uptake complex.
S5856 Trifluoperazine Trifluoperazine (NSC-17474, RP-7623, SKF-5019) is an FDA-approved antipsychotic drug for schizophrenia. It is an inhibitor of calmodulin (CaM) and Dopamine D2 receptor with an IC50 value of 1.2 nM for D2 receptor.
Toxicol Appl Pharmacol, 2021, 424:115595
Toxicol Lett, 2021, 348:10-17
Biomed Chromatogr, 2021, e5205
E0125New Raclopride Raclopride is a selective dopamine D2/D3 receptor antagonist that discriminates between dopamine-mediated motor functions. Raclopride 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.
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. SCH-23390 hydrochloride is a potent and high efficacy agonist at h5-HT2C receptors with Ki of 9.3 nM. SCH-23390 hydrochloride directly inhibits G protein-coupled inwardly rectifying potassium (GIRK) channels with IC50 of 268 nM.
S1280 Amisulpride Amisulpride (DAN-2163) is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.
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.
Anticancer Res, 2021, 41(2):687-697
Molecules, 2020, 25(18)E4206
Nature, 2018, 560(7718):372-376
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.
Anticancer Res, 2021, 41(2):687-697
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.
Clin Transl Sci, 2021, 10.1111/cts.13012
J Cancer Res Clin Oncol, 2019, 145(6):1495-1507
Toxicol Lett, 2019, 313:77-90
S1771 Chlorprothixene Chlorprothixene 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.
Sci Rep, 2018, 8(1):15753
S1789 Tetrabenazine (Xenazine) Tetrabenazine(Nitoman, Xenazine) 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.
S1920 Haloperidol Haloperidol (Haldol) is an antipsychotic and butyrophenone.
Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2
S2104 Levosulpiride Levosulpiride is a selective antagonist for D2 dopamine receptors used as an antipsychotic and prokinetic agent.
Sci Rep, 2018, 8(1):15753
S2437 Rotundine Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.
J Med Virol, 2019, 91(8):1440-1447
S2493 Olanzapine Olanzapine (LY170053) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Nat Protoc, 2021, 10.1038/s41596-021-00624-z
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
Pharmacol Res, 2021, 170:105714
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.
S4086 Loxapine Succinate Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Anticancer Res, 2021, 41(2):687-697
S4096 Droperidol Droperidol (NSC 169874) is a potent antagonist of dopamine subtype 2 receptors in the limbic system.
Sci Rep, 2018, 8(1):15753
S4151 Penfluridol Penfluridol (TLP-607) is a highly potent, first generation diphenylbutylpiperidine antipsychotic.
Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.09.007
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.
Mol Pharmacol, 2022, 101(4):236-245
S4251 Phenothiazine Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.
S4257 Alizapride HCl Alizapride HCl is a dopamine receptor antagonist used for the theropy of nausea and vomiting.
S4289 Metoclopramide HCl Metoclopramide HCl is a selective dopamine D2 receptor antagonist, used for the treatment of nausea and vomiting.
Pharmazie, 2021, 76(4):172-174
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. Pimozide also exhibits binding affinity at α2-adrenoceptor and 5-HT1A with Ki of 360 nM and 310 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S4631 Prochlorperazine dimaleate salt Prochlorperazine dimaleate (Prochlorperazin, Compazine, Capazine, Stemetil) is a dopamine (D2) receptor antagonist.
F1000Res, 2016, 5:150
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.
Nat Commun, 2020, 11(1):941
S4731 Perphenazine Perphenazine (Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.
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.
S5034 Melitracen hydrochloride Melitracen hydrochloride (Thymeol) is a potential dopamine D1/2 receptor antagonist which has antidepressant properties.
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.
S5197 Loxapine Loxapine (Adasuve), a typical neuroleptic, is a drug with D2/D3 receptor antagonist activity and a higher affinity for D3 than D2. Loxapine displays an extremely strong binding affinity for dopamine D4 and serotonin 5-HT2 receptors.
S5324 Oxidopamine hydrobromide Oxidopamine (6-hydroxydopamine, 6-OHDA, 2,4,5-trihydroxyphenethylamine) is a neurotoxic synthetic organic compound that acts as an antagonist of the neurotransmitter dopamine with potential antineoplastic activity. Solutions should be freshly prepared and protected from exposure to light.
Ther Adv Chronic Dis, 2021, 12:2040622321998139
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.
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.
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.
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
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
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. It 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.
S5741 Quetiapine Quetiapine is an atypical antipsychotic used for the treatment of schizophrenia, bipolar disorder, and major depressive disorder.Quetiapine is a 5-HT receptors agonist with a pEC50 of 4.77 for human 5-HT1A receptor. Quetiapine is a dopamine receptor antagonist with a pIC50 of 6.33 for human D2 receptor. Quetiapine have 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.
S5749 Chlorpromazine 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.
ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
Pharmaceuticals (Basel), 2022, 15(2)241
Viruses, 2022, 14(3)496
S5862 Metoclopramide Metoclopramide is a dopamine antagonist used for the treatment of nausea and vomiting.
Pharmazie, 2021, 76(4):172-174
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.
Pharmazie, 2021, 76(4):172-174
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.
S6455 Clebopride malate Clebopride is a dopamine antagonist drug and is used to treat functional gastrointestinal disorder such as nausea or vomiting.
S6853 ONC206 ONC206 is a selective antagonist of dopamine D2-like receptors (DRD2/3/4) with broad-spectrum anti-tumor activity.
S6887 Clozapine N-oxide Clozapine N-oxide (CNO) 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.
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.
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.
S1726 Levodopa Levodopa is the precursor to the neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine (adrenaline), used to treat Parkinson's symptoms.
PLoS One, 2017, 12(3):e0173240
S2011 Pramipexole 2HCl Monohydrate Pramipexole 2HCl Monohydrateis a novel non-ergoline dopamine (DA) agonist, used to treat Parkinson's disease.
Autophagy, 2016, 12(12):2374-2385
S2089New 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 .
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
S2451 Amantadine HCl Amantadine HCl (1-adamantanamine) is used to treat or prevent infections of the respiratory tract caused by a certain virus.
Ecotoxicol Environ Saf, 2021, 211:111900
Adv Ther (Weinh), 2020, 2000034
S2460 Pramipexole Pramipexole (SND 919) 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.
S2529 Dopamine HCl Dopamine HCl is a catecholamine neurotransmitter present in a wide variety of animals,And a dopamine D1-5 receptors agonist.
Cell, 2021, 184(4):943-956.e18
Cancer Commun (Lond), 2020, 10.1002/cac2.12103
Brain, 2019, 142(3):700-718
S3656 Piribedil Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties.
S3664 Flupentixol dihydrochloride Flupentixol (Flupenthixol) dihydrochloride, an antipsychotic neuroleptic drug, is a powerful antagonist of both D1 and D2 dopamine receptors and also an alpha-adrenergic receptor antagonist.
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. Nuciferine 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.
Br J Pharmacol, 2021, 178(5):1182-1199
Tohoku J Exp Med, 2021, 254(1):17-23
S4274 Rotigotine Rotigotine is a dopamine receptor agonist, used in the treatment of Parkinson's disease and restless legs syndrome.
Cell Death Dis, 2019, 10(9):649
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.
S4639 Brexpiprazole Brexpiprazole (OPC-34712) is a novel D2 dopamine and serotonin 1A partial agonist, called serotonin-dopamine activity modulator (SDAM), and a potent antagonist of serotonin 2A receptors, noradrenergic alpha 1B and 2C receptors with Ki values of 0.3, 0.12, 0.47, 0.17 and 0.59 nM for D2L, 5-HT1A, 5-HT2A, α1B receptors and α2C receptors respectivey.
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.
S5842 Cabergoline Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor.
S5849 Cariprazine HCl Cariprazine (RGH-188), a novel second-generation antipsychotic, is a D3-preferring dopamine D2/D3 receptor partial agonist.
Eur J Pharmacol, 2021, 911:174557
S7993 SKF38393 HCl SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.
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). Lithium carbonate is able to alter D2 dopamine receptors response.
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.
E0125New Raclopride Raclopride is a selective dopamine D2/D3 receptor antagonist that discriminates between dopamine-mediated motor functions. Raclopride 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.
S2089New 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 .
Tags: Dopamine Receptor inhibitor|Dopamine Receptor agonist|Dopamine Receptor activator|Dopamine Receptor inducer|Dopamine Receptor antagonist|Dopamine Receptor signaling pathway|Dopamine Receptor assay kit