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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: GBR12935
GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.
Synonyms: Haldol
Haloperidol (Haldol) is an antipsychotic and butyrophenone.
Synonyms: RS-25560-197; SYN-117
Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.
Synonyms: SM13496
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.
Ropinirole a selective dopamine D2 receptors inhibitor with IC5N/A of 29 nM.
Synonyms: CGS 10746
Pentiapine is a novel dopamine release inhibitor.
Synonyms: BIA 5-1058
Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects.
Synonyms: R-16341
Penfluridol is a potent, long-acting antipsychotic agent that primarily targets D2-like dopamine receptors. It exhibits significant anti-inflammatory properties by inhibiting TNFα-induced NF-κB activation and demonstrates efficacy in models of arthritis and colitis. Additionally, Penfluridol acts as a Ca2+-calmodulin inhibitor, inducing apoptosis and autophagy in various cellular contexts. This compound is utilized in research focusing on chronic schizophrenia, acute psychosis, Tourette syndrome, autoimmune diseases, and it also shows antibacterial activity against E. faecalis with a minimum inhibitory concentration of 7.81 μg/ml.
Synonyms: Loxapine succinate salt; Loxapac; Cloxazepin; Daxolin; Maleate; Loxipine; Oxilapine; Succinate; Loxapine
Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia.
Synonyms: Promazine Hcl; Starazin; Talofen; Promazine monohydrochloride; Hydrochloride; Promazine; Protactyl; Sinophenin; Sparine
Promazine Hydrochloride is a phenothiazine compound and D2DR inhibitor. Promazine Hydrochloride has been employed in studies investigating dopamine-stimulated glycosylation of brain proteins in vitro. It has actions similar to chlorpromazine but with less antipsychotic activity.
Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
Synonyms: Ro 8-4650 hydrochloride; Ro8-4650
Diclofensine hydrochloride (Ro-8-4650 hydrochloride) is a potent inhibitor of monoamine reuptake, blocking the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC50 values of 0.74, 2.3, and 3.7 nM, respectively.
Synonyms: EB-1020
Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
Synonyms: BIA 5-453
Etamicastat (BIA 5-453) is a potent and reversible peripheral dopamine-β-hydroxylase (DβH) inhibitor.
Synonyms: SEP-225289 hydrochloride; SEP225289
Dasotraline hydrochloride (SEP-225289 hydrochloride) is a triple reuptake inhibitor that blocks dopamine, norepinephrine, and serotonin transporters with IC50 values of 4, 6, and 11 nM, respectively.
Synonyms: DL-Tetrahydropalmatine hydrochloride
Tetrahydropalmatine hydrochloride (DL-Tetrahydropalmatine hydrochloride), an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
Synonyms: DL-Tetrahydropalmatine
Tetrahydropalmatine, an active component isolated from corydalis, possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats.
Fusaric acid is a potent dopamine β-hydroxylase inhibitor that reduces endogenous levels of norepinephrine and epinephrine in various tissues, including the brain, heart, spleen, and adrenal glands. By inducing oxidative stress and apoptosis, fusaric acid disrupts mitochondrial integrity and activates key apoptosis-related proteases such as Caspase-3/7, -8, and -9. Additionally, fusaric acid regulates pivotal apoptotic proteins, inhibits fibrosis-related signaling pathways including NF-κB and TGF-β1/SMADs, and mitigates collagen deposition. Its applications extend to myocardial fibrosis and cardiac hypertrophy research, as well as studies on esophageal and liver cancers.
Loxapine hydrochloride is an orally active inhibitor of dopamine receptors and an antagonist of 5-HT receptors. This dibenzoxazepine compound exhibits significant antipsychotic properties, making it valuable for research into psychotropic effects and therapeutic interventions for schizophrenia and other psychiatric disorders. Its dual receptor activity contributes to its efficacy in modulating dopaminergic and serotonergic pathways.
Synonyms: LU-111995
Belaperidone is a selective 5-HT2A receptor inhibitor, demonstrating significant antidopaminergic and antiserotonergic properties. This compound is primarily employed in research related to neuropsychiatric disorders and may provide insight into therapeutic strategies for conditions such as schizophrenia and depression. Its mechanism of action makes Belaperidone a valuable tool in studying serotonin and dopamine receptor interactions within the central nervous system.
Synonyms: Benzatropine; Benzotropine
Benztropine is an orally active anticholinergic agent that effectively crosses the blood-brain barrier. It serves as a dopamine re-uptake inhibitor and a human D2 dopamine receptor allosteric antagonist, making it relevant in Parkinson's disease research. Additionally, Benztropine demonstrates potential anti-cancer stem cell activity, enhancing its applicability in oncology studies.
Synonyms: Methotrimeprazine maleate
Levomepromazine maleate is an N-substituted phenylthiazine compound that acts as an antipsychotic agent primarily targeting dopamine receptors. This compound exhibits significant sedative properties and is also a potent inhibitor of CYP2D6, making it a valuable tool for investigating the pharmacological mechanisms underlying schizophrenia. Its multifaceted receptor-blocking activity contributes to its role in research applications related to neuropsychiatric disorders.
BL-1020 mesylate is a dopamine receptor inhibitor with high affinity for D2L, D2S, and 5-HT2A receptors, exhibiting Ki values of 0.066, 0.062, and 0.21 nM, respectively. This compound functions as an antipsychotic agent and also acts as an agonist at the GABAA receptor, enhancing GABA release with a Ki of 3.74 μM. Furthermore, BL-1020 mesylate interacts effectively with histamine receptors (Ki of 0.47 nM) and demonstrates the ability to diminish amphetamine-induced hyperactivity while minimizing catalepsy and sedation. It penetrates the blood-brain barrier, making it suitable for neurological research applications.
Metribuzin is a non-selective herbicide that acts as an inhibitor of the D1 protein at the QB site of photosystem II. By disrupting photosynthesis, Metribuzin effectively inhibits plant DNA synthesis, leading to reduced growth of target species. This compound is primarily utilized in agricultural research to study weed control, particularly against annual grass and broadleaf weeds.
Trifluoperazine is an antipsychotic agent primarily acting as a blocker of central dopamine receptors. It exhibits significant activity as a potent α1-adrenergic receptor antagonist and a NUPR1 inhibitor, demonstrating anticancer properties. Additionally, Trifluoperazine functions as a calmodulin inhibitor and inhibits P-glycoprotein, contributing to its diverse biological effects. This compound is utilized in research on schizophrenia and shows potential as a reversible inhibitor of influenza virus morphogenesis.
