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- Amfebutamone (Bupropion) is an atypical antidepressant and smoking cessation aid.
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Dopamine Receptor antagonist
Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder. -
H1 antagonist
Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.- Keisuke Obara, .et al. , Biol Pharm Bull, 2021, 44, 1140-1150
- Chlorprothixene exerts strong antagonism at the following receptors: 5-HT2; D1, D2, D3; H1;mACh; α1-adrenergic.
- Clozapine displays a broad range of pharmacological actions; the antipsychotic effects are thought to be mediated principally by 5-HT2A/2C and dopamine receptor blockade.
- Madeleine S A Tan, .et al. , Mol Pharm, 2022, Sep 23 PMID: 36149013
- Madeleine S. A. Tan, .et al. , Gels, 2022, Jan; 8(1): 38 PMID: 35049572
- Milan D Valyear, .et al. , Nat Commun, 2020, Jul 28;11(1):3764 PMID: 32724058
- Yutaro Kobayashi, .et al. , Transl Psychiatry, 2019, 9:181 PMID: 31371697
- M.D. Valyear, .et al. , bioRxiv, 2018, 2018
- Domperidone blocks the action of dopamine. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which, among others, regulates nausea and vomiting (area postrema on the floor of the fourth ventricle and rhomboid fossa).
- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
- Dopamine (abbreviated as DA), a simple organic chemical in the catecholamine family, is a monoamine neurotransmitter - a chemical released by nerve cells to send signals to other nerve cells.
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CYP2D6 inhibitor
Haloperidol (Haldol) is an antipsychotic and butyrophenone. -
5-HT Receptors/D2 dopamine receptor antagonist
Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist. -
Dopamine Receptor antagonist
Paliperidone(Invega) is an atypical antipsychotic.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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dopamine re-uptake inhibitor
Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI. -
Dopamine Receptor Agonist
Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating early-stage Parkinson's disease (PD) and restless legs syndrome (RLS). - Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorder.
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5-HT (serotonin) and dopamine receptor antagonist
Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
Dopamine Receptor agonist
Rotigotine hydrochloride is a dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.- Mattia Ferraiolo, .et al. , Neuropharmacology, 2022, 207: 108942
- Mattia Ferraiolo, .et al. , Eur J Pharmacol, 2021, Nov 15;911:174557 PMID: 34626593
- Thioridazine is a dopamine receptor antagonist that displays antipsychotic activity. Recently thioridazine is also reported to successfully kill human cancer stem cells.
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Dopamine D2 inhibitor
Lurasidone is an atypical antipsychotic that alleviates positive symptoms (e.g., hallucinations, delusions) without inducing extrapyramidal side effects except for akathisia,despite its potent D2 antagonistic actions. -
D2 receptor agonist
B-HT 920 is a dopamine agonist that has been proposed as an antiparkinsonian agent. It also has α1-adrenergic and α2-adrenergic agonist activity. -
Dopamine agonist
Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively. - Fenoldopam is used as an antihypertensive agent postoperatively, and also intravenously (IV) to treat a hypertensive crisis.
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D2/5-HT2 receptor antagonist
Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic. - Pramipexole dihydrochloride is a dopamine receptor agonist exhibiting selectivity for the D3 receptor.
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D1/D5 receptor antagonist
SCH 23390 hydrochloride is a potent dopamine receptor antagonist (Ki values are 0.2 nM and 0.3 nM at D1 and D5 receptor sub-types, respectively). -
dopamine uptake inhibitor
GBR 12783 dihydrochloride is a very potent and selective inhibitor of dopamine uptake (IC50 for inhibition of [3H]-dopamine uptake in rat striatal synaptosomes is 1.8 nM). -
D2 receptor antagonist
Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms. -
D2 dopamine partial agonist
Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD). -
D2 dopamine receptor antagonist
L-741626 is a potent and selective antagonist for the dopamine receptor D2. It has good selectivity over the related D3 and D4 subtypes and other receptors.- Yoon-Jin Kim, .et al. , Sci Adv, 2021, Feb 19;7(8) PMID: 33608268
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dopamine D2 receptor agonist
Bromocriptine mesylate is a potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM).1,2 As a result, it has found applications in combination therapy for Parkinsonism. -
dopamine receptor agonist
Nalmefene hydrochloride is an opioid receptor antagonist.- Mark G Papich, .et al. , Drug Deliv Transl Res, 2022, Feb;12(2):376-383 PMID: 34817831
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dopaminergic agonist
Pergolide mesylate is a dopaminergic agonist that also decrease plasma prolactin concentrations. -
dopamine D2 receptor antagonist
Metoclopramide HCl is a selective dopamine D2 receptor antagonist.- Reiko Watanabe, .et al. , J Med Chem, 2021, Mar 11;64(5):2725-2738 PMID: 33619967
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Dopamine receptor agonist
(+)-PD 128907 hydrochloride is a potent D3DR (dopamine receptor) agonist (Ki = 2.3 nM). -
dopamine agonist
Dexpramipexole dihydrochloride is a neuroprotective agent and weak non-ergoline dopamine agonist. -
Dopamine Receptor antagonist
Metoclopramide is a dopamine D2 antagonist that is used as an antiemetic. -
D2 receptor agonist
rac-Rotigotine Hydrochloride is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM. -
5-HT/dopamine receptor antagonist
Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. -
dopamine (D2) receptor antagonist
Prochlorperazine is a dopamine (D2) receptor antagonist that belongs to the phenothiazine class of antipsychotic agents. -
Dopamine receptor antagonist
Alizapride HCl is a dopamine receptor antagonist used for the theropy of nausea and vomiting.
