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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.
Synonyms: RGH-188 hydrochloride
Cariprazine hydrochloride is a novel antipsychotic drug candidate that exhibits high selectivity and affinity to dopamine D3(Ki=0.09 nM) and D2 (Ki=0.5 nM) receptors and moderate affinity to serotonin 5-HT(1A) receptors.
Metoclopramide is a dopamine D2 antagonist that is used as an antiemetic.
Synonyms: Geodon; CP 88059
Ziprasidone is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
Synonyms: Compazine; Capazine; Stemetil
Prochlorperazine is a dopamine (D2) receptor antagonist that belongs to the phenothiazine class of antipsychotic agents.
Alizapride HCl is a dopamine receptor antagonist used for the theropy of nausea and vomiting.
Synonyms: NSC 170976
Azaperone is a pyridinylpiperazine and butyrophenone neuroleptic drug with sedative and antiemetic effects, which is used mainly as a tranquilizer in veterinary medicine.
Synonyms: Dehydrobenzperidol
Droperidol is a butyrophenone compound primarily acting as a dopamine receptor antagonist. It inhibits the activation of GABA(A) and neuronal nicotinic acetylcholine receptors (nAChR), demonstrating IC50 values of 12.6 nM and 5.8 μM, respectively. This compound exhibits notable anesthetic and sedative properties, making it useful in research related to neuropharmacology and anesthesiology.
Fluphenazine dihydrochloride is a potent dopamine receptor antagonist primarily targeting dopamine D2 receptors in the mesolimbic, nigrostriatal, and tuberoinfundibular pathways. This phenothiazine derivative also exhibits the ability to inhibit neuronal voltage-gated sodium channels. Its key biological activities include the suppression of Methylphenidate-induced stereotyped behaviors and climbing in murine models. Fluphenazine dihydrochloride is widely utilized in research related to psychosis, diabetic peripheral neuropathy, and may also have implications for the inhibition of SARS-CoV-2.
Synonyms: SM-13496 Hydrochloride
Lurasidone Hydrochloride is a potent antagonist of both dopamine D2 and 5-HT7 receptors, exhibiting IC50 values of 1.68 nM and 0.495 nM, respectively. Additionally, it acts as a partial agonist at the 5-HT1A receptor with an IC50 of 6.75 nM. This compound is utilized in research focused on neuropharmacology and the treatment of psychiatric disorders, such as schizophrenia and bipolar disorder. Its selective modulation of serotonin and dopamine receptors makes it a valuable tool for investigating neurochemical pathways and therapeutic interventions.
Perphenazine is a potent dopamine receptor antagonist, specifically targeting D2 and D3 receptors with Ki values of 0.56 nM and 0.43 nM, respectively, while also interacting with the 5-HT2A receptor and the Alpha-1A adrenergic receptor. This compound demonstrates inhibitory effects on cancer cell proliferation and promotes apoptosis. Perphenazine is valuable for research into psychiatric disorders, cancer biology, and inflammatory processes.
Trifluoperazine dihydrochloride is a dopamine receptor antagonist, primarily used in the study of schizophrenia. This compound demonstrates significant activity as an α1-adrenergic receptor blocker and acts as a potent inhibitor of NUPR1, exhibiting anticancer properties. Additionally, it functions as a calmodulin inhibitor and has been shown to inhibit P-glycoprotein, impacting multidrug resistance. Trifluoperazine dihydrochloride is also recognized for its reversible inhibition of influenza virus morphogenesis, making it valuable for various research applications in neuropharmacology and virology.
Synonyms: CP-88059 hydrochloride
Ziprasidone Hcl(CP-88059 Hcl) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
Synonyms: R 6238; Orap; Opiran.
Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
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Synonyms: N 7001; Melitracen HCl
Melitracen HCl ia potential dopamine D1/2 receptor antagonist used to treat depression. It is often co-administered with flupenthixol as a treatment for trigeminal neuralgia. It does not effect cardiovascular function.
Synonyms: Molindone HCl; Molindone Hydrochloride salt; Molindone HCl salt; Moban
Molindone HCl is a D2 dopamine receptor antagonist. It also acts as a MAO inhibitor.
Tiapride hydrochloride is a selective antagonist of the D2 and D3 dopamine receptors, exhibiting IC50 values of 110-320 nM and 180 nM, respectively. This compound is recognized for its anti-dyskinetic and anxiolytic activities, making it valuable in neurological research. Tiapride hydrochloride is utilized as a neuroleptic agent, contributing to studies on movement disorders and anxiety-related conditions.
Synonyms: AHR-3070-C; Maxolon; Metoclopramide HCl; Metoclopramide hydrochloride; Metoclopramide monohydrochloride monohydrate; Metozolv; Reglan
Metoclopramide hydrochloride hydrate is a dopamine D2 antagonist that is used as an antiemetic.
Clebopride malate is an orally active antagonist of dopamine D2 receptors, exhibiting significant antiemetic and prokinetic properties. This compound is useful in research focused on functional gastrointestinal disorders, providing valuable insights into dopaminergic modulation in gastrointestinal motility and emesis. Clebopride malate may serve as an important tool for understanding the underlying mechanisms of these conditions.
Haloperidol hydrochloride is a potent dopamine D2 receptor antagonist, widely used as an antipsychotic.
Raclopride is a dopamine D2/D3 receptor antagonist, which binds to D2 and D3 receptors with dissociation constants (Kis) of 1.8 nM and 3.5 nM, respectively, but has a very low affinity for D1 and D4 receptors with Kis of 18000 nM and 2400 nM, respectively.
NRA-0160 is a selective dopamine D4 receptor antagonist, with a Ki value of 0.48 nM and with negligible affinity for dopamine D2 receptor (Ki: >10000 nM), D3 receptor (Ki: 39 nM), rat 5-HT2A receptor (Ki: 180 nM) and rat α1 adrenoceptor (Ki: 237 nM).
Abaperidone is a potent antagonist of 5-HT2A receptor and dopamine D2 receptor with IC50s of 6.2 and 17 nM.
CGP 25454A is a novel and selective presynaptic dopamine autoreceptor antagonist.
Synonyms: LIN-1418
Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor.
Deschloroclozapine is a dual dopamine and serotonin receptor antagonist with Kis of 200, 2500, 420, 39, 84, 40 nM for dopamine D1, D2,D4, and serotonin S2A, S2C, S3, respectively.
