Dopamine Receptor

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Dopamine Receptorシグナル伝達経路

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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.
Nat Commun, 2024, 15(1):1669
Adv Sci (Weinh), 2023, 10(7):e2205566
Int J Nanomedicine, 2023, 18:4647-4662
S2456 Chlorpromazine HCl Chlorpromazine HCl 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.
Virus Res, 2024, 339:199258
Cell Mol Immunol, 2022, 19(8):925-943
Emerg Microbes Infect, 2022, 11(1):1135-1144
S2493 Olanzapine Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Nat Protoc, 2021, 10.1038/s41596-021-00624-z
Pharmacol Res, 2021, 170:105714
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
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.
Phytomedicine, 2024, 123:155230
Cell Death Discov, 2024, 10(1):52
Redox Biol, 2023, 62:102698
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, 2023, 466:116490
Cell Rep Methods, 2023, 3(10):100599
Toxicol Lett, 2022, 367:3-8
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).
Antiviral Res, 2024, 222:105817
Front Microbiol, 2022, 13:979904
Toxicol Lett, 2022, 367:3-8
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
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
S6887 CNO (Clozapine N-oxide) 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.
Nat Commun, 2023, 10.1038/s41467-023-42814-1
Nat Commun, 2023, 14(1):71
Nat Commun, 2023, 14(1):6923
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
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.
Front Microbiol, 2020, 10:2936
G3 (Bethesda), 2014, 4(6):1081-9
G3 (Bethesda), 2014, 10.1534/g3.114.010819
S4631 Prochlorperazine dimaleate salt Prochlorperazine dimaleate salt is a dopamine (D2) receptor antagonist.
Cancer Biol Ther, 2023, 24(1):2269637
Cancer Biol Ther, 2023, 10.1080/15384047.2023.2269637
Front Microbiol, 2022, 13:979904
S2451 Amantadine HCl Amantadine HCl (1-adamantanamine) is used to treat or prevent infections of the respiratory tract caused by a certain virus.
Front Microbiol, 2022, 13:979904
Ecotoxicol Environ Saf, 2021, 211:111900
Adv Ther (Weinh), 2020, 2000034
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
S4569 Fluphenazine dihydrochloride Fluphenazine dihydrochloride (Prolixin) is a phenothiazine-class D1DR and D2DR inhibitor. It also inhibits Histamine H1 Receptor.
Front Microbiol, 2022, 13:979904
bioRxiv, 2020, 2020/9/20.4.7.30734
Methods Mol Biol, 2017, 1513:119-140
S4151 Penfluridol Penfluridol (TLP-607,R-16341) is a highly potent, first generation diphenylbutylpiperidine antipsychotic.
Acta Pharm Sin B, 2022, 12(3):1271-1287
Front Microbiol, 2022, 13:979904
Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.09.007
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.
Theranostics, 2023, 13(10):3149-3164
JCI Insight, 2023, 8(16)e170434
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
S1726 Levodopa Levodopa(L-DOPA) is the precursor to the neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine (adrenaline), used to treat Parkinson's symptoms.
Front Pharmacol, 2022, 13:903235
PLoS One, 2017, 12(3):e0173240
S2461 Domperidone Domperidone is an oral dopamine D2 receptor antagonist, used to treat nausea and vomiting.
Front Microbiol, 2022, 13:979904
Sci Adv, 2022, 8(15):eabk2376
S1280 Amisulpride Amisulpride (DAN-2163) is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.
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 Microbiol, 2022, 13:979904
Anticancer Res, 2021, 41(2):687-697
S2011 Pramipexole 2HCl Monohydrate Pramipexole 2HCl Monohydrate is a novel non-ergoline dopamine (DA) agonist, used to treat Parkinson's disease.
Front Microbiol, 2022, 13:979904
Autophagy, 2016, 12(12):2374-2385
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
S4096 Droperidol Droperidol (NSC 169874,Dehydrobenzperidol) is a potent antagonist of dopamine subtype 2 receptors in the limbic system.
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.
Front Microbiol, 2022, 13:979904
Sci Rep, 2018, 8(1):15753
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.
Front Microbiol, 2022, 13:979904
Metabolites, 2022, 12(2)101
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.
Br J Pharmacol, 2021, 178(5):1182-1199
Tohoku J Exp Med, 2021, 254(1):17-23
S7993 SKF38393 HCl SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.
JCI Insight, 2023, 8(16)e170434
JCI Insight, 2023, 8(16)e170434
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
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 Microbiol, 2022, 13:979904
Nat Commun, 2020, 11(1):941
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.
Alzheimers Dement, 2023, 10.1002/alz.13090
Chem Biol Drug Des, 2022, 100(5):699-721
S4219 Azaperone Azaperone (NSC 170976,Ketamine) 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
S8097 C-DIM12 C-DIM12 is a 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
S6853 ONC206 ONC206 is a selective antagonist of dopamine D2-like receptors (DRD2/3/4) with broad-spectrum anti-tumor activity.
Neoplasia, 2023, 39:100894
Pharmacol Res Perspect, 2022, 10(4):e00993
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 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
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
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.
Front Immunol, 2023, 14:1193081
Front Immunol, 2023, 14:1193081
S5862 Metoclopramide Metoclopramide is a dopamine antagonist used for the treatment of nausea and vomiting.
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
Pharmazie, 2021, 76(4):172-174
S3163 Benztropine mesylate Benztropine(Cogentin mesylate, Benztropine methanesulfonate) is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
Front Microbiol, 2022, 13:979904
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
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
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
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. Solutions are unstable and should be fresh-prepared.
Ther Adv Chronic Dis, 2021, 12:2040622321998139
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
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.
Front Microbiol, 2022, 13:979904
S5565 Triflupromazine hydrochloride Triflupromazine hydrochloride (Fluopromazine) is an antipsychotic medication of the phenothiazine class.
bioRxiv, 2020, 2020/9/20.4.7.30734
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
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.
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
S5842 Cabergoline Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor.
Cells, 2022, 11(21)3344
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.
Mol Pain, 2021, 17:17448069211042117
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
S3189 Ropinirole HCl Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.
Front Microbiol, 2022, 13:979904
S4251 Phenothiazine Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.
S5741 Quetiapine Quetiapine(ICI204636) 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.
S4731 Perphenazine Perphenazine (Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties.
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.
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.
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.
S7236New 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).
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.
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.
S9469New 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.
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
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.
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.
S5796 Vanoxerine dihydrochloride Vanoxerine (GBR-12909) is a potent and selective inhibitor of the presynaptic dopamine uptake complex.
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.
S4309New 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.
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.
S6455 Clebopride malate Clebopride is a dopamine antagonist drug and is used to treat functional gastrointestinal disorder such as nausea or vomiting.
E0125 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.
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 .
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.
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
S2451 Amantadine HCl Amantadine HCl (1-adamantanamine) is used to treat or prevent infections of the respiratory tract caused by a certain virus.
Front Microbiol, 2022, 13:979904
Ecotoxicol Environ Saf, 2021, 211:111900
Adv Ther (Weinh), 2020, 2000034
S1726 Levodopa Levodopa(L-DOPA) is the precursor to the neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine (adrenaline), used to treat Parkinson's symptoms.
Front Pharmacol, 2022, 13:903235
PLoS One, 2017, 12(3):e0173240
S2011 Pramipexole 2HCl Monohydrate Pramipexole 2HCl Monohydrate is a novel non-ergoline dopamine (DA) agonist, used to treat Parkinson's disease.
Front Microbiol, 2022, 13:979904
Autophagy, 2016, 12(12):2374-2385
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.
Front Microbiol, 2022, 13:979904
Metabolites, 2022, 12(2)101
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.
Br J Pharmacol, 2021, 178(5):1182-1199
Tohoku J Exp Med, 2021, 254(1):17-23
S7993 SKF38393 HCl SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.
JCI Insight, 2023, 8(16)e170434
JCI Insight, 2023, 8(16)e170434
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
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.
Front Microbiol, 2022, 13:979904
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.
Cell Rep Methods, 2023, 3(1):100381
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
S5842 Cabergoline Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor.
Cells, 2022, 11(21)3344
S7236New 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).
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.
S4309New 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.
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 .
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.
S2456 Chlorpromazine HCl Chlorpromazine HCl 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.
Virus Res, 2024, 339:199258
Cell Mol Immunol, 2022, 19(8):925-943
Emerg Microbes Infect, 2022, 11(1):1135-1144
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, 2023, 466:116490
Cell Rep Methods, 2023, 3(10):100599
Toxicol Lett, 2022, 367:3-8
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).
Antiviral Res, 2024, 222:105817
Front Microbiol, 2022, 13:979904
Toxicol Lett, 2022, 367:3-8
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.
Front Microbiol, 2020, 10:2936
G3 (Bethesda), 2014, 4(6):1081-9
G3 (Bethesda), 2014, 10.1534/g3.114.010819
S4569 Fluphenazine dihydrochloride Fluphenazine dihydrochloride (Prolixin) is a phenothiazine-class D1DR and D2DR inhibitor. It also inhibits Histamine H1 Receptor.
Front Microbiol, 2022, 13:979904
bioRxiv, 2020, 2020/9/20.4.7.30734
Methods Mol Biol, 2017, 1513:119-140
S2461 Domperidone Domperidone is an oral dopamine D2 receptor antagonist, used to treat nausea and vomiting.
Front Microbiol, 2022, 13:979904
Sci Adv, 2022, 8(15):eabk2376
S3163 Benztropine mesylate Benztropine(Cogentin mesylate, Benztropine methanesulfonate) is a dopamine transporter (DAT) inhibitor with IC50 of 118 nM.
Front Microbiol, 2022, 13:979904
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.
Mol Pain, 2021, 17:17448069211042117
S3189 Ropinirole HCl Ropinirole (SKF-101468A) a selective dopamine D2 receptors agonist with Ki of 29 nM.
Front Microbiol, 2022, 13:979904
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.
S1642 Methyldopa Methyldopa (Aldomet) is a DOPA decarboxylase competitive inhibitor with an ED50 of 21.8 mg/kg.
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.
S5796 Vanoxerine dihydrochloride Vanoxerine (GBR-12909) is a potent and selective inhibitor of the presynaptic dopamine uptake complex.
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.
Nat Commun, 2024, 15(1):1669
Adv Sci (Weinh), 2023, 10(7):e2205566
Int J Nanomedicine, 2023, 18:4647-4662
S2493 Olanzapine Olanzapine (LY170053,Zyprexa, Zalasta, Zolafren, Olzapin, Oferta, Zypadhera) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Nat Protoc, 2021, 10.1038/s41596-021-00624-z
Pharmacol Res, 2021, 170:105714
Cell Mol Gastroenterol Hepatol, 2021, S2352-345X(21)00196-X
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
S6887 CNO (Clozapine N-oxide) 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.
Nat Commun, 2023, 10.1038/s41467-023-42814-1
Nat Commun, 2023, 14(1):71
Nat Commun, 2023, 14(1):6923
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
S4631 Prochlorperazine dimaleate salt Prochlorperazine dimaleate salt is a dopamine (D2) receptor antagonist.
Cancer Biol Ther, 2023, 24(1):2269637
Cancer Biol Ther, 2023, 10.1080/15384047.2023.2269637
Front Microbiol, 2022, 13:979904
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
S4151 Penfluridol Penfluridol (TLP-607,R-16341) is a highly potent, first generation diphenylbutylpiperidine antipsychotic.
Acta Pharm Sin B, 2022, 12(3):1271-1287
Front Microbiol, 2022, 13:979904
Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.09.007
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.
Theranostics, 2023, 13(10):3149-3164
JCI Insight, 2023, 8(16)e170434
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
S1280 Amisulpride Amisulpride (DAN-2163) is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.
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 Microbiol, 2022, 13:979904
Anticancer Res, 2021, 41(2):687-697
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
S4096 Droperidol Droperidol (NSC 169874,Dehydrobenzperidol) is a potent antagonist of dopamine subtype 2 receptors in the limbic system.
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.
Front Microbiol, 2022, 13:979904
Sci Rep, 2018, 8(1):15753
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
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 Microbiol, 2022, 13:979904
Nat Commun, 2020, 11(1):941
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.
Alzheimers Dement, 2023, 10.1002/alz.13090
Chem Biol Drug Des, 2022, 100(5):699-721
S4219 Azaperone Azaperone (NSC 170976,Ketamine) 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 dopamine D2-like receptors (DRD2/3/4) with broad-spectrum anti-tumor activity.
Neoplasia, 2023, 39:100894
Pharmacol Res Perspect, 2022, 10(4):e00993
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 5-HT1A and α1-adrenoceptor with Ki of 310 nM and 39 nM, respectively. Pimozide is an antipsychotic drug with anti-tumor activity and suppresses STAT3 and STAT5 activity.
Cell Rep Med, 2023, 10.1016/j.xcrm.2023.101286
Biol Pharm Bull, 2021, 10.1248/bpb.b21-00531
S5862 Metoclopramide Metoclopramide is a dopamine antagonist used for the treatment of nausea and vomiting.
Anticancer Drugs, 2022, 10.1097/CAD.0000000000001344
Pharmazie, 2021, 76(4):172-174
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
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
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
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. Solutions are unstable and should be fresh-prepared.
Ther Adv Chronic Dis, 2021, 12:2040622321998139
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
S5565 Triflupromazine hydrochloride Triflupromazine hydrochloride (Fluopromazine) is an antipsychotic medication of the phenothiazine class.
bioRxiv, 2020, 2020/9/20.4.7.30734
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
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
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
S4251 Phenothiazine Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain.
S5741 Quetiapine Quetiapine(ICI204636) 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.
S4731 Perphenazine Perphenazine (Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic 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.
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.
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.
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.
S9469New 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.
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.
S6455 Clebopride malate Clebopride is a dopamine antagonist drug and is used to treat functional gastrointestinal disorder such as nausea or vomiting.
E0125 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.
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.
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
S2451 Amantadine HCl Amantadine HCl (1-adamantanamine) is used to treat or prevent infections of the respiratory tract caused by a certain virus.
Front Microbiol, 2022, 13:979904
Ecotoxicol Environ Saf, 2021, 211:111900
Adv Ther (Weinh), 2020, 2000034
S1726 Levodopa Levodopa(L-DOPA) is the precursor to the neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine (adrenaline), used to treat Parkinson's symptoms.
Front Pharmacol, 2022, 13:903235
PLoS One, 2017, 12(3):e0173240
S2011 Pramipexole 2HCl Monohydrate Pramipexole 2HCl Monohydrate is a novel non-ergoline dopamine (DA) agonist, used to treat Parkinson's disease.
Front Microbiol, 2022, 13:979904
Autophagy, 2016, 12(12):2374-2385
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.
Front Microbiol, 2022, 13:979904
Metabolites, 2022, 12(2)101
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.
Br J Pharmacol, 2021, 178(5):1182-1199
Tohoku J Exp Med, 2021, 254(1):17-23
S7993 SKF38393 HCl SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.
JCI Insight, 2023, 8(16)e170434
JCI Insight, 2023, 8(16)e170434
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
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.
Front Microbiol, 2022, 13:979904
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.
Cell Rep Methods, 2023, 3(1):100381
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
S5842 Cabergoline Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor.
Cells, 2022, 11(21)3344
S7236New 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).
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.
S4309New 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.
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 .
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.
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.
Front Immunol, 2023, 14:1193081
Front Immunol, 2023, 14:1193081
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.
S7236New 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).
S9469New 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.
S4309New 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.
S7236New 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).
S4309New 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.

Dopamine Receptor阻害剤の選択性比較

Tags: Dopamine Receptor inhibitor|Dopamine Receptor agonist|Dopamine Receptor activator|Dopamine Receptor inducer|Dopamine Receptor antagonist|Dopamine Receptor signaling pathway|Dopamine Receptor assay kit