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
|
|
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
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S1771 |
Chlorprothixene
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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
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S1789 |
Tetrabenazine (Xenazine)
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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. |
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S1920 |
Haloperidol
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Haloperidol (Haldol) is an antipsychotic and butyrophenone. |
- Neuropsychopharmacology, 2021, 10.1038/s41386-021-00962-2
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S2104 |
Levosulpiride
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Levosulpiride is a selective antagonist for D2 dopamine receptors used as an antipsychotic and prokinetic agent. |
- Sci Rep, 2018, 8(1):15753
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S2437 |
Rotundine
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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
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S2493 |
Olanzapine
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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
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S3044 |
Lurasidone HCl
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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. |
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S4086 |
Loxapine Succinate
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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
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S4096 |
Droperidol
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Droperidol (NSC 169874) is a potent antagonist of dopamine subtype 2 receptors in the limbic system. |
- Sci Rep, 2018, 8(1):15753
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S4151 |
Penfluridol
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Penfluridol (TLP-607) is a highly potent, first generation diphenylbutylpiperidine antipsychotic. |
- Acta Pharmaceutica Sinica B, 2021, 10.1016/j.apsb.2021.09.007
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S4219 |
Azaperone
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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
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S4251 |
Phenothiazine
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Phenothiazine (ENT 38) is a dopamine-2 (D2) receptor antagonist therefore decreases the effect of dopamine in the brain. |
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S4257 |
Alizapride HCl
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Alizapride HCl is a dopamine receptor antagonist used for the theropy of nausea and vomiting. |
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S4289 |
Metoclopramide HCl
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Metoclopramide HCl is a selective dopamine D2 receptor antagonist, used for the treatment of nausea and vomiting.
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- Pharmazie, 2021, 76(4):172-174
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S4358 |
Pimozide
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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
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S4631 |
Prochlorperazine dimaleate salt
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Prochlorperazine dimaleate (Prochlorperazin, Compazine, Capazine, Stemetil) is a dopamine (D2) receptor antagonist. |
- F1000Res, 2016, 5:150
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S4655 |
Sulpiride
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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
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S4731 |
Perphenazine
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Perphenazine (Perphenazin, Trilafon, Etaperazine) is a phenothiazine derivative and a dopamine antagonist with antiemetic and antipsychotic properties. |
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S4889 |
Perospirone hydrochloride
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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. |
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S5034 |
Melitracen hydrochloride
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Melitracen hydrochloride (Thymeol) is a potential dopamine D1/2 receptor antagonist which has antidepressant properties. |
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S5153 |
Tetrahydroberberine
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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. |
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S5185 |
Perospirone
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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. |
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S5197 |
Loxapine
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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. |
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S5324 |
Oxidopamine hydrobromide
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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
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S5399 |
Chlorprothixene hydrochloride
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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. |
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S5428 |
Promazine hydrochloride
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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. |
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S5481 |
Molindone hydrochloride
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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. |
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S5559 |
Tetrahydropalmatine
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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
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S5565 |
Triflupromazine hydrochloride
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Triflupromazine hydrochloride (Fluopromazine) is an antipsychotic medication of the phenothiazine class. |
- bioRxiv, 2020, 2020/9/20.4.7.30734
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S5624 |
Paliperidone Palmitate
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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
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S5714 |
lurasidone
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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. |
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S5741 |
Quetiapine
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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. |
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S5749 |
Chlorpromazine
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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
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S5862 |
Metoclopramide
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Metoclopramide is a dopamine antagonist used for the treatment of nausea and vomiting. |
- Pharmazie, 2021, 76(4):172-174
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S5949 |
Metoclopramide hydrochloride hydrate
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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
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S6410 |
Clemizole
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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. |
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S6455 |
Clebopride malate
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Clebopride is a dopamine antagonist drug and is used to treat functional gastrointestinal disorder such as nausea or vomiting. |
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S6853 |
ONC206
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ONC206 is a selective antagonist of dopamine D2-like receptors (DRD2/3/4) with broad-spectrum anti-tumor activity. |
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S6887 |
Clozapine N-oxide
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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. |
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S9509 |
Tiapride Hydrochloride
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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. |
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S0104 |
Pardoprunox (SLV-308) hydrochloride
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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. |
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S1726 |
Levodopa
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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
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S2011 |
Pramipexole 2HCl Monohydrate
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Pramipexole 2HCl Monohydrateis a novel non-ergoline dopamine (DA) agonist, used to treat Parkinson's disease. |
- Autophagy, 2016, 12(12):2374-2385
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S2089New |
Fenoldopam
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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 . |
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S2168 |
PD128907 HCl
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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
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S2451 |
Amantadine HCl
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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
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S2460 |
Pramipexole
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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. |
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S2529 |
Dopamine HCl
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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
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S3656 |
Piribedil
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Piribedil (Trivastal, Trivastan) is a relatively selective dopamine (D2/D3) agonist with moderate antidepressant activity. It also has α2-adrenergic (α2A/α2C) antagonist properties. |
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S3664 |
Flupentixol dihydrochloride
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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. |
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S3821 |
Nuciferine
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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
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S4274 |
Rotigotine
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Rotigotine is a dopamine receptor agonist, used in the treatment of Parkinson's disease and restless legs syndrome.
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- Cell Death Dis, 2019, 10(9):649
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S4618 |
Fenoldopam mesylate
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Fenoldopam (SKF 82526, Corlopam) is a selective dopamine-1 receptor (DA1) agonist with natriuretic/diuretic properties. It lowers blood pressure through arteriolar vasodilation. |
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S4639 |
Brexpiprazole
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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. |
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S5066 |
Pramipexole dihydrochloride
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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. |
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S5842 |
Cabergoline
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Cabergoline (FCE-21336), an ergot derivative, is a long-acting dopamine agonist and prolactin inhibitor. |
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S5849 |
Cariprazine HCl
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Cariprazine (RGH-188), a novel second-generation antipsychotic, is a D3-preferring dopamine D2/D3 receptor partial agonist. |
- Eur J Pharmacol, 2021, 911:174557
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S7993 |
SKF38393 HCl
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SKF38393 HCl is a selective dopamine D1/D5 receptor agonist.
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