Dopamine Receptors

Cat. No.

A45883

CAS No.

839712-15-1

Desmethyl cariprazine

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.

Cat. No.

A46106

CAS No.

2227154-23-4

LB-102

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.

Cat. No.

A49447

CAS No.

61241-59-6

A32390A

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.

Cat. No.

A49540

CAS No.

122898-67-3

Itopride

Synonyms: HSR803 free base

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.

Cat. No.

A59898

CAS No.

59831-65-1

Halopemide

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.

Cat. No.

A59915

CAS No.

4789-68-8

Octoclothepin maleate salt

Synonyms: Clorotepine maleate salt

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.

Cat. No.

A59954

CAS No.

67469-57-2

GBR 12783

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.

Cat. No.

A59968

CAS No.

5845-67-0

Cyclo(glycyl-L-leucyl)

Synonyms: Cyclo(leu-gly)

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.

Cat. No.

A59980

CAS No.

146725-34-0

MFZ 2-13

Synonyms: O-456

MFZ 2-13 is an N-demethylated intermediate and N-nor-analogue of MFD 2-12 that targets the human dopamine receptor. It functions as an inhibitor of dopamine uptake, exhibiting an IC50 of 1.4 nM. This compound is valuable for research in neuropharmacology and the study of psychoactive substances.

Cat. No.

A59998

CAS No.

123594-64-9

PD 128907

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.

Cat. No.

A60006

CAS No.

53463-78-8

ADTN

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.

Cat. No.

A60016

CAS No.

632-47-3

Bulbocapnine hydrochloride

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.

Cat. No.

A60041

CAS No.

1639208-51-7

Valbenazine dihydrochloride

Synonyms: NBI-98854 dihydrochloride

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.

Cat. No.

A60044

CAS No.

69079-98-7

(Z)-Flupenthixol decanoate

(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.

Cat. No.

A60055

CAS No.

127685-30-7

Seproxetine hydrochloride

Synonyms: S-Norfluoxetine hydrochloride; LY 215229 hydrochloride

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.

Cat. No.

A60117

CAS No.

316-07-4

Opromazine hydrochloride

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.

Cat. No.

A60192

CAS No.

410074-73-6

Amitifadine

Synonyms: DOV-21947; EB-1010

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.

Cat. No.

A68116

CAS No.

5169-78-8

Tipepidine

Tipepidine is an inhibitor of the dopamine D2 receptor-mediated G-protein coupled inwardly rectifying potassium (GIRK) currents, exhibiting a half-maximal inhibitory concentration (IC50) of 7.0 μM. By inhibiting these currents, Tipepidine activates ventral tegmental area (VTA) dopamine neurons, thereby influencing dopaminergic signaling. This compound has demonstrated potential antidepressant-like effects and is commonly studied in research related to neuropharmacology and respiratory conditions.

Cat. No.

A70055

CAS No.

95333-81-6

SKF-102698

SKF-102698 is an inhibitor of dopamine β-hydroxylase, a key enzyme in catecholamine biosynthesis. By inhibiting this enzyme, SKF-102698 effectively increases endogenous dopamine levels, providing valuable insights into dopaminergic signaling. This compound is particularly useful in hypertension research, allowing for the exploration of dopamine’s role in blood pressure regulation and cardiovascular health.

Cat. No.

A70056

CAS No.

14901-16-7

U-14624

U-14624 is a potent inhibitor of dopamine beta-hydroxylase, exhibiting strong oral bioavailability. This compound effectively suppresses the enzymatic activities of aminopyrine N-demethylase, aniline hydroxylase, and p-nitroanisole O-demethylase. U-14624 is valuable for research applications focusing on neuropharmacology and the regulation of dopamine levels.

Cat. No.

A70060

CAS No.

22632-06-0

Bupicomide

Bupicomide is a selective inhibitor of dopamine beta-monooxygenase, functioning through the mechanism analogous to fusaric acid. This compound has demonstrated utility in the study of hypertension, making it a valuable tool for research on neurochemical pathways related to blood pressure regulation and cardiovascular health.

Cat. No.

A70062

CAS No.

1446-24-8

3-Allylphenol

3-Allylphenol is a potent inhibitor of dopamine β-hydroxylase, demonstrating a Ki value of 12 mM. This compound is essential for studying the regulation of catecholamine synthesis and can be utilized in research applications aimed at understanding neurotransmitter dynamics and related physiological processes.

Cat. No.

A78910

CAS No.

1627576-64-0

JJC8-089

JJC8-089 is a selective dopamine transporter (DAT) inhibitor that enhances motivational behaviors and promotes engagement in goal-directed tasks. Research has demonstrated that JJC8-089 effectively counteracts the low-effort behavior induced by the VMAT-2 inhibitor Tetrabenazine in rat models, leading to a marked preference for high-effort tasks over free access to food. This compound serves as a valuable tool for investigating dopamine-related behavioral mechanisms and motivational dysfunction.