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CYP2D6 inhibitor
Haloperidol (Haldol) is an antipsychotic and butyrophenone. -
dopamine beta-hydroxylase inhibitor
Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine. -
dopamine re-uptake inhibitor
Vanoxerine (GBR-12909) is a piperazine derivative which is a potent and selective DRI.- Alexander D H Kingdon, .et al. , J Antibiot (Tokyo), 2025, Jan;78(1):54-63 PMID: 39402358
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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. -
DAT and SLC6A2 inhibitor
GBR-12935 is a piperazine derivative which is a potent and selective dopamine reuptake inhibitor.- Alexander D H Kingdon, .et al. , J Antibiot (Tokyo), 2025, Jan;78(1):54-63 PMID: 39402358
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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). -
dopamine β-hydroxylase (DBH) inhibitor
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. -
Dopamine reuptake inhibitor
Phenylpiracetam is a phenylated derivative of the nootropic drug piracetam. It is used as a stimulant nootropic drug that can be up to 30-60 times more potent than piracetam. -
D2DR and D4DR inhibitor
Loxapine Succinate is a D2DR and D4DR inhibitor and serotonergic receptor antagonist. Loxapine succinate is an antipsychotic agent used in schizophrenia. -
D2DR inhibitor
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. -
MAO inhibitor
Molindone HCl is a D2 dopamine receptor antagonist. It also acts as a MAO inhibitor. -
monoamine reuptake inhibitor
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. -
dual NE/DA transporter inhibitor
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. -
triple reuptake inhibitor
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. -
dopamine reuptake inhibitor
Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). -
Dopamine β-hydroxylase Inhibitor
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. -
Serotonin/Norepinephrine/Dopamine Reuptake Inhibitor
Bicifadine is a serotonin/norepinephrine/dopamine reuptake inhibitor that demonstrates oral bioavailability. It exhibits significant antinociceptive properties across various models of acute, persistent, and chronic pain. Bicifadine is primarily utilized in research related to pain mechanisms and therapeutic interventions for pain management. -
Dopamine/5-HT Receptor Inhibitor
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. -
5-HT2A Receptor Inhibitor
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. -
Histamine Receptor Inhibitor
Perphenazine-d8 dihydrochloride is a deuterium-labeled derivative of Perphenazine, primarily functioning as a histamine receptor inhibitor. This compound exhibits potent antipsychotic properties by interacting with serotonin and dopamine receptors. It is valuable for research focused on neuropharmacology, chemical biology, and the study of receptor-ligand interactions in psychiatric disorders. -
Dopamine Receptor Inhibitor
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. -
D2 Receptor Inhibitor, D3 Receptor Inhibitor, 5-HT1A Receptor Inhibitor, 5-HT2B Receptor Inhibitor
Desmethyl cariprazine is a potent inhibitor of the D2 and D3 dopamine receptors, as well as the 5-HT1A and 5-HT2B serotonin receptors. It demonstrates a pEC50 of 8.90 at D2 receptors, 8.09 at D3 receptors, and 6.28 at 5-HT1A receptors, significantly inhibiting forskolin-induced cAMP production and serotonin-induced Ca2+ release. This compound is valuable for research focused on psychiatric disorders such as schizophrenia and bipolar disorder type I. -
Dopamine D2/D3/5-HT7 Receptor Inhibitor
LB-102 is an orally bioavailable inhibitor of dopamine D2, D3, and 5-HT7 receptors. It exhibits significant antagonistic activity, making it a valuable tool for investigating the neurochemical pathways involved in schizophrenia and other psychiatric disorders. This compound is useful for studies aimed at understanding the role of these receptors in various neuropsychiatric conditions. -
Dopamine β-hydroxylase Inhibitor
A32390A is a potent inhibitor of dopamine β-hydroxylase, functioning primarily to decrease norepinephrine synthesis. This reduction can lead to lowered blood pressure, making A32390A valuable in studies related to hypertension, particularly in models such as DOCA hypertensive rats. Additionally, the compound's properties as a copper chelator allow for exploration in the context of bacterial infections and metabolic disorders, providing versatile applications in chemical research. -
AChE/Dopamine 2 Inhibitor
Itopride is a potent dopamine D2 receptor antagonist and an acetylcholinesterase (AChE) inhibitor. Itopride enhances gastric motility through its dual mechanisms of action, promoting both antidopaminergic and anti-acetylcholinesterase effects. This compound is primarily utilized in research related to gastrointestinal disorders, particularly gastroesophageal reflux disease (GERD), offering insights into prokinetic therapies. -
Phospholipase D Inhibitor
Halopemide is a potent inhibitor of phospholipase D (PLD), exhibiting IC50 values of 220 nM for human PLD1 and 310 nM for PLD2. In addition to its enzymatic inhibition, Halopemide functions as a dopamine receptor antagonist and exhibits psychotropic properties. This reagent is valuable for research applications exploring PLD-mediated signaling pathways and dopamine receptor interactions in various biological contexts. -
Dopamine Receptor Inhibitor
Clopenthixol is a thiaquinoline compound that acts as an antagonist of D1 and D2 dopamine receptors. It exhibits inhibitory effects comparable to those of phenothiazine antipsychotics, making it valuable in the treatment of schizophrenia and other mental disorders. This compound is primarily utilized in research related to psychiatric conditions and the exploration of dopamine regulation in the central nervous system. -
SR-2A/D2DR Inhibitor
Octoclothepin maleate salt is a dual inhibitor of the SR-2A and D2 dopamine receptors. This compound exhibits significant central depressant activity, demonstrated in various observational and instrumental studies using rodent models. Its properties make it a valuable tool in neuropharmacological research, particularly in the study of neuroleptic effects and dopaminergic signaling pathways. -
Dopamine Receptor Inhibitor
7-Hydroxy-DPAT hydrobromide is a selective agonist for the D3 dopamine receptor, primarily impacting dopamine signaling pathways. This compound demonstrates significant biological activity in modulating locomotor behavior and influencing dopamine metabolism within the central nervous system. It serves as a valuable tool for research applications related to neuropharmacology and the study of dopamine-related disorders. -
Dopamine Receptor Inhibitor
GBR 12783 is a selective dopamine uptake inhibitor that targets dopamine receptors with high potency. It effectively inhibits [3H]dopamine uptake in striatal synaptosomes from rats and mice, exhibiting IC50 values of 1.8 nM and 1.2 nM, respectively. This compound has been shown to enhance memory performance and increase hippocampal acetylcholine release in rodent models, making it valuable for research in neuropharmacology and cognitive function studies. -
Dopamine Receptor Inhibitor
Cyclo(glycyl-L-leucyl) is a neuropeptide that specifically inhibits dopamine receptors, playing a crucial role in modulating dopaminergic signaling. This compound has been shown to down-regulate dopamine receptor activity and reduce dopaminergic supersensitivity, particularly in the context of morphine-induced analgesia in animal models. Cyclo(glycyl-L-leucyl) holds promise for potential therapeutic applications in preventing tardive dyskinesias and L-DOPA-induced dyskinesias, making it valuable for research in neuropharmacology and movement disorders. -
Dopamine Receptor Inhibitor
Fosopamine hydrochloride is a dopamine receptor D agonist, primarily targeting the dopamine receptor pathways. It has demonstrated significant utility in research related to hypertension, aiding in the exploration of cardiovascular mechanisms and blood pressure regulation. This compound may provide insights into both the physiological and pathological roles of dopamine signaling in hypertension-related studies. -
Dopamine Receptor Inhibitor
PD 128907 is a selective dopamine D3 receptor inhibitor that effectively modulates dopaminergic signaling. The active (+) enantiomer exhibits high affinity for rat D3 receptors and demonstrates significant inhibitory effects on neuronal firing in the ventral tegmental area and substantia nigra pars compacta, with EC50 values of 33 nM and 38 nM, respectively. Additionally, it inhibits dopamine release in the caudate putamen with an EC50 of 66 nM. While PD 128907 primarily targets D3 receptors, evidence suggests its actions may also involve D2 autoreceptors, making it a valuable tool for exploring dopamine receptor pharmacology and neurobehavioral research. -
Dopamine Receptor Inhibitor
ADTN is a dopamine receptor inhibitor that modulates dopamine neurotransmission. It demonstrates the ability to reduce dopamine-related signaling, which may help target conditions associated with excessive dopamine activity. ADTN is applicable in research focused on mental health disorders and cognitive function modulation, providing insights into therapeutic strategies for related pathologies. -
Dopamine Receptor Inhibitor
Metoclopramide dihydrochloride is a dopamine D2 receptor antagonist primarily used for its antiemetic effects. It demonstrates notable activity in managing nausea and vomiting, particularly in patients undergoing chemotherapy or surgery. This compound is also employed in research settings to explore the modulation of dopaminergic pathways and gastrointestinal motility. -
Dopamine Receptor Inhibitor
Bulbocapnine hydrochloride is a potent dopamine receptor inhibitor that plays a significant role in modulating dopaminergic activity. This aporphine alkaloid is known to inhibit dopamine synthesis and exhibits neuroleptic-like properties, alongside anticonvulsant and antinociceptive effects. Its pharmacological profile makes it a valuable tool in research related to neurological disorders and the exploration of dopamine-related pathways. -
Dopamine Receptor Inhibitor
Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia. -
Dopamine D1/D2 Receptor Inhibitor
(Z)-Flupenthixol decanoate is a potent antagonist of dopamine D1 and D2 receptors, functioning primarily to inhibit dopaminergic signaling. This compound exhibits significant antipsychotic activity, making it valuable in the study of psychiatric disorders and neuropharmacology. Research applications include investigations into the modulation of dopaminergic pathways and the evaluation of therapeutic strategies for schizophrenia and related conditions. -
Dopamine Receptor Inhibitor
Seproxetine hydrochloride is a dopamine receptor inhibitor known for its selective serotonin reuptake inhibitory activity. By specifically blocking the serotonin uptake transporter, it increases serotonin levels in the brain, while also exhibiting significant interactions with dopamine receptors. This compound is actively researched for its potential therapeutic applications in mood disorders and associated neurological conditions, showcasing enhanced biological activity and efficacy through its ability to form stable charge transfer complexes. -
Dopamine Receptor Inhibitor
TISCH is a potent and selective iodinated ligand that targets CNS D1 dopamine receptors, demonstrating a high affinity with a Kd value of 0.205 nM in rat striatal tissue. Its ability to cross the blood-brain barrier allows for effective distribution in regions with substantial D1 receptor density, making it a valuable pharmacological tool for characterizing these receptors. Additionally, TISCH, when labeled with I-123, has potential applications as an in vivo imaging agent for studying D1 dopamine receptor function in the central nervous system. -
Dopamine Receptor Inhibitor
Opromazine hydrochloride is a dopamine receptor inhibitor known for its sedative and antiemetic effects. It primarily reduces dopaminergic activity by blocking dopamine receptors in the brain, making it useful in the treatment of psychiatric disorders such as schizophrenia and psychosis. Additionally, studies have investigated its metabolites through various microsomal enzymes, highlighting differences in formation rates and the variability of drug-metabolizing enzymes in human liver and placenta microsomes, which is essential for understanding its pharmacokinetic profile. -
Dopamine Receptor Inhibitor
SV 293 is a selective antagonist that primarily targets dopamine D2 receptors with a binding affinity that is 100-fold greater than that of D3 and D4 receptor subtypes. This compound exhibits neutral antagonist activity and effectively blocks the effects of the full agonist quinpirole in forskolin-dependent adenylate cyclase inhibition assays and electrophysiological assays. SV 293 serves as a valuable pharmacological tool for investigating the role of D2-like receptor subtypes in dopamine-related pathways associated with neurological, neuropsychiatric, and movement disorders. -
Dopamine Uptake Inhibitor
GBR-12879 dihydrochloride is a potent dopamine uptake inhibitor that selectively targets the dopamine transporter. Its primary mechanism involves preventing the reabsorption of dopamine, thus enhancing dopaminergic signaling. This compound is widely utilized in research to investigate the role of dopamine in neurological disorders and to explore potential therapeutic strategies for conditions such as depression and schizophrenia. -
DAT/NET/SERT Inhibitor
Amitifadine is a serotonin-norepinephrine-dopamine reuptake inhibitor (SNDRI) that targets the dopamine transporter (DAT), norepinephrine transporter (NET), and serotonin transporter (SERT). It exhibits inhibitory concentrations of 12 nM for serotonin, 23 nM for norepinephrine, and 96 nM for dopamine in HEK 293 cells. This compound is pertinent for research applications exploring the modulation of monoaminergic systems and investigating potential therapeutic effects in mood disorders. -
Dopamine Receptor Inhibitor
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.

