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Dopamine receptor agonists and antagonists act on the five G protein-coupled receptors that respond to dopamine. The receptors form two groups, with D1 and D5 in the D1-like class and D2, D3 and D4 in the D2-like class. D1-like receptors stimulate adenylyl cyclase, whereas D2-like receptors inhibit it and lower cyclic adenosine monophosphate (cAMP) levels. Dopamine signaling controls movement, reward, motivation and hormone release, and is studied in Parkinson's disease and psychiatric research. Ligands here include the agonist rotigotine HCl, the D2 antagonists L-741626 and domperidone, and the D3-preferring ligand BP897.
BP 897, is an antagonist at human dopamine D3 receptors and at rat somatodendritic dopamine D3 receptors
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.
Synonyms: Invega; INVEGA Sustenna; 9-hydroxyrisperidone
Paliperidone(Invega) is an atypical antipsychotic.
Synonyms: L-741,626
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.
Nalmefene hydrochloride is an opioid receptor antagonist.
Metoclopramide HCl is a selective dopamine D2 receptor antagonist.
Synonyms: CCRIS-4248
Sulpiride is a dopamine D2-receptor antagonist. It has been used therapeutically as an antidepressant, antipsychotic, and as a digestive aid.
Synonyms: Solian
Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.
Synonyms: Zyprexa; Zalasta; Zolafren; Olzapin; Oferta; Zypadhera; LY170053
Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
Synonyms: CP 88059 (hydrochloride monohydrate); CP88059
Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
Thioridazine is a dopamine receptor antagonist that displays antipsychotic activity. Recently thioridazine is also reported to successfully kill human cancer stem cells.
Synonyms: SLV-313
Adoprazine is part of the Antidepressant Agent group
Synonyms: SB-277011-A
SB-277011 is a drug which acts as a potent and selective dopamine D3 receptor antagonist which is around 80-100x selective for D3 over D2 and lacks any partial agonist activity.
Synonyms: Lonasen; AD 5423
Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
Synonyms: Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate
Benztropine mesylate is a centrally acting anticholinergic agent that effectively crosses the blood-brain barrier. It primarily functions as a selective antagonist at human D2 dopamine receptors, exhibiting anti-histaminic properties and acting as a dopamine re-uptake inhibitor. This compound is particularly relevant for Parkinson's disease research, as well as in studies exploring its effects on cancer stem cells (CSCs). Researchers can utilize Benztropine mesylate to examine its potential therapeutic benefits in neurodegenerative and cancer treatment contexts.
Synonyms: RV-12309; S-(-)-Sulpiride
Levosulpiride is a selective antagonist of dopamine D2 receptors, classified as an atypical antipsychotic agent within the benzamide family. This compound is primarily used in the investigation of its effects on psychotic disorders and gastrointestinal conditions due to its ability to modulate dopaminergic activity. Researchers utilize Levosulpiride to study its therapeutic potential in conditions such as schizophrenia and to explore its impact on gastrointestinal motility.
Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.
Synonyms: R79598
Ocaperidone is an effective antipsychotic agent.
Synonyms: Flupentixol dihydrochloride
cis-(Z)-Flupentixol dihydrochloride is a dopamine receptor antagonist, antipsychotic, neuroleptic agent.
Synonyms: Floropipamide; McN-JR 3345; R 3345
Pipamperone (Floropipamide; McN-JR 3345; R 3345) is a high-affinity antagonist of 5-HT2A receptor (pKi=8.2) and D4 receptor (pKi=8.0) and a low-affinity antagonist of D2 receptor (pKi=6.7).
GR 103691 is an effective and selective receptor antagonist of the dopamine D3 receptor (D3DR).
Synonyms: (R)-(+)-SCH 23390 hydrochloride
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).
Synonyms: (+/-)-Veralipride; LIR166
Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms.
GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.
SB269652 is a new chemical probe that can differentiate D2R monomers from dimers or oligomers depending on the observed pharmacology.
