Dopamine Receptors

Cat. No.

A59938

CAS No.

131796-63-9

Odapipam

Synonyms: NNC 756

Odapipam (NNC 756) is a selective dopamine D1 receptor antagonist, exhibiting high affinity with a Kd of 0.18 nM. This compound serves as a valuable tool in neuroscience research, particularly for studying dopaminergic signaling pathways and related neuropsychiatric disorders. In addition, Odapipam functions as an effective radiotracer for positron emission tomography (PET) imaging, enhancing the investigation of receptor dynamics in vivo.

Cat. No.

A59944

CAS No.

1221408-42-9

YQA14

YQA14 is a high-affinity antagonist of the dopamine D3 receptor. It exhibits significant anti-opioid addiction activity, demonstrating the ability to inhibit morphine- and cocaine-induced conditioned place preference (CPP) in preclinical models. This compound is valuable for research into the mechanisms of addiction and the development of therapeutic strategies for substance use disorders.

Cat. No.

A59948

CAS No.

2562346-14-7

Mesdopetam hemitartrate

Synonyms: IRL790 hemitartrate

Mesdopetam hemitartrate is a selective antagonist of the dopamine D3 receptor, exhibiting a Ki value of 90 nM and an IC50 of 9.8 μM for human recombinant D3 receptors. This compound demonstrates psychomotor stabilizing effects, making it a valuable tool in the investigation of motor and psychiatric complications associated with Parkinson's disease. Its unique properties contribute to research aimed at understanding the underlying mechanisms of dopamine-related disorders.

Cat. No.

A59949

CAS No.

1403894-72-3

Mesdopetam

Synonyms: IRL790

Mesdopetam is a selective antagonist of the dopamine D3 receptor, displaying a Ki value of 90 nM and an IC50 of 9.8 μM for the human recombinant D3 receptor. This compound exhibits psychomotor stabilizing properties and is utilized in research focused on motor and psychiatric complications associated with Parkinson's disease. Its role in modulating dopamine signaling makes it valuable for studying therapeutic strategies in this context.

Cat. No.

A59950

CAS No.

1782532-06-2

PD 168568 dihydrochloride

PD 168568 dihydrochloride is a potent and orally active antagonist of the dopamine receptor D4 (DRD4). This compound exhibits selectivity for the D4 receptor, with Ki values of 8.8 nM for DRD4 compared to 1842 nM for DRD2 and 2682 nM for DRD3. PD 168568 dihydrochloride is applicable in glioblastoma (GBM) research, making it a valuable tool for investigating the role of DRD4 in cancer biology and potential therapeutic strategies.

Cat. No.

A59952

CAS No.

85378-82-1

AJ-76 hydrochloride

Synonyms: (+)-AJ 76 hydrochloride; (1S,2R)-AJ 76 hydrochloride

AJ-76 hydrochloride is a potent antagonist of dopamine autoreceptors, exhibiting pKi values of 6.95, 6.67, 6.37, 6.21, and 6.07 for human D3, D4, D2 short, D2 long, and rat D2 receptors, respectively. This compound is valuable for research focused on dopamine receptor modulation and its implications in neurological disorders. Its specific receptor affinity allows for investigations into the roles of dopamine signaling in various physiological and pathological processes.

Cat. No.

A59955

CAS No.

58045-23-1

Zuclopenthixol dihydrochloride

Synonyms: (Z)-Clopenthixol dihydrochloride

Zuclopenthixol dihydrochloride is a thioxanthene derivative that functions as a mixed antagonist of dopamine D1 and D2 receptors. This compound is primarily utilized in schizophrenia research, aiding in the investigation of neurochemical pathways associated with the disorder. Its ability to modulate dopaminergic signaling makes it a valuable tool for studying the efficacy of antipsychotic therapies.

Cat. No.

A59956

CAS No.

863766-31-8

(-)-GSK598809 hydrochloride

Synonyms: (1S,5R)-GSK598809 hydrochloride

(-)-GSK598809 hydrochloride is a potent and selective antagonist of the dopamine D3 receptor (DRD3). It exhibits high affinity for DRD3, making it a valuable tool for studying dopamine-related pathways and their implications in neuropsychiatric disorders. This compound is suitable for research applications focused on drug development, behavioral studies, and understanding the role of dopamine in various physiological processes.

Cat. No.

A59957

CAS No.

337972-47-1

FAUC 213

FAUC 213 is a potent antagonist of the dopamine D4 receptor, exhibiting a binding affinity (Ki) of 2.2 nM for the human D4.4 receptor. This compound demonstrates significantly lower activity towards D2 and D3 receptors, with Kis of 3.4 μM and 5.3 μM, respectively. FAUC 213 is capable of crossing the blood-brain barrier, suggesting its utility in the study of neurological conditions. Its distinct pharmacological profile supports research into atypical antipsychotic therapies.

Cat. No.

A59958

CAS No.

1076189-55-3

RG-15

RG-15 is a potent oral antagonist of the dopamine receptors, specifically targeting the human D2 and D3 receptors with pKi values of 8.23 and 10.49, respectively. It effectively inhibits dopamine-stimulated [35S]GTPγS binding, demonstrating an IC50 of 21.2 nM in rat striatal membranes, 36.7 nM in mouse A9 cells expressing human D2L receptors, and 7.2 nM in CHO cells expressing human D3 receptors. RG-15 also enhances dopamine turnover and biosynthesis in the mouse striatum and olfactory bulb, indicating potential antipsychotic properties. This compound is valuable for research into dopamine-related disorders and therapeutics.

Cat. No.

A59960

CAS No.

149649-22-9

Nafadotride

Nafadotride is a selective antagonist of the dopamine D3 receptor. By inhibiting dopamine D3 receptor activity, Nafadotride modulates dopamine signaling pathways that are critical for regulating emotion, motivation, reward, and motor functions. This compound is suitable for research into the role of dopamine D3 receptors in neuropsychiatric disorders and behavior-related studies, providing insights into potential therapeutic targets.

Cat. No.

A59963

CAS No.

234757-41-6

U-99194 maleate

Synonyms: U-99194A; PNU-99194A maleate; JPC-211 maleate

U-99194 maleate is a potent and selective antagonist of the dopamine D3 receptor, exhibiting a Ki value of 160 nM. This compound effectively inhibits both endogenously released dopamine and exogenous D3 agonist activation of the D3 receptor. In rat hippocampal slices, U-99194 maleate reverses the IPSC-suppressive effect induced by the D3 agonist PD 128907. Additionally, it demonstrates significant suppression of nicotine-induced tremors in mouse models, making it a valuable tool for investigating dopamine D3 receptor-mediated motor disorders, particularly in the context of kinetic tremors.

Cat. No.

A59967

CAS No.

33162-17-3

Dicarbine dihydrochloride

Dicarbine dihydrochloride is a dopamine receptor antagonist that modulates neurotransmission within multiple regions of the brain. By blocking dopamine receptors, it effectively mitigates the suppression of conditioned defense reflexes induced by stimulation of the mesencephalic reticular formation. This compound serves as a valuable tool in research addressing schizophrenia and alcoholic psychosis, facilitating insights into dopamine-related pathophysiology and therapeutic interventions.

Cat. No.

A59971

CAS No.

3568-24-9

Propionylpromazine

Propionylpromazine is a selective antagonist of the dopamine D2 receptor (DRD2), exhibiting potent tranquilizing effects. This compound is widely utilized in veterinary research to investigate its impact on behavioral modulation and neuropharmacological pathways. Its ability to influence dopamine signaling makes it a valuable tool for studying psychiatric disorders and the effects of antipsychotic agents.

Cat. No.

A59973

CAS No.

59338-93-1

Alizapride

Alizapride is a selective antagonist of the D2 dopamine receptor, primarily used for its potent antiemetic properties. It exhibits effectiveness in managing nausea and vomiting, and is also applicable in the treatment of various human digestive disorders. Research involving Alizapride contributes to the understanding of dopamine's role in gastrointestinal function and the development of therapeutic strategies for related conditions.

Cat. No.

A59979

CAS No.

1050-79-9

Moperone

Synonyms: Methylperidol; R 1658

Moperone is a potent antagonist of D2 and D3 dopamine receptors, with IC50 values of 1.0 nM for both targets. This compound exhibits significant biological activity in the modulation of dopaminergic signaling pathways, making it a valuable tool for research into psychiatric disorders and neurological conditions. Moperone is particularly useful in studies examining the role of dopamine receptors in behavior and cognition.

Cat. No.

A59981

CAS No.

220519-06-2

A-437203

Synonyms: Lu201640; A37203

A-437203 is a selective antagonist for the dopamine D3 receptor, exhibiting Ki values of 71 nM for D2, 1.6 nM for D3, and 6220 nM for D4 receptors. This compound is valuable for research into dopamine-related pathways and offers potential applications in studying neuropsychiatric disorders. Its specificity for the D3 receptor makes it a useful tool for exploring the role of this receptor in various biological processes and assessing new therapeutic strategies.

Cat. No.

A59989

CAS No.

1352993-39-5

Trazpiroben

Synonyms: TAK-906

Trazpiroben is a selective antagonist of the dopamine D2 and D3 receptors, primarily utilized for investigating the pathophysiology and treatment of moderate-to-severe gastroparesis. Its inhibition of these receptors plays a significant role in regulating gastrointestinal motility. Trazpiroben is a valuable tool for researchers exploring the therapeutic potential and underlying mechanisms of dopamine-related gastrointestinal disorders.

Cat. No.

A59993

CAS No.

200195-01-3

PD 172760

Synonyms: CI 1030

PD 172760 is a selective antagonist of the D4 receptor, playing a significant role in neurotransmission modulation. Its action may enhance understanding of psychosis and related neuropsychiatric disorders. This compound is valuable for researchers investigating the therapeutic potential of targeting D4 receptors in various neurological and psychiatric conditions.

Cat. No.

A59994

CAS No.

169451-33-6

YM-50001

YM-50001 is a potent and selective antagonist of the dopamine D4 receptor, exhibiting a Ki value of 5.62 nM. This compound is utilized in research related to neurological diseases, contributing to the understanding of dopamine-mediated pathways and their implications in various neuropsychiatric disorders.

Cat. No.

A59996

CAS No.

84226-12-0

Eticlopride

Synonyms: FLB-131

Eticlopride is a selective antagonist of the dopamine D2 receptor, demonstrating a high binding affinity for dopamine D2 as well as for α1-adrenergic, α2-adrenergic, 5HT1, and 5HT2 receptors, with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. This compound is primarily utilized in research related to antipsychotic drug development and elucidation of dopamine's role in neuropsychiatric disorders. Its pharmacological profile supports investigations into dopamine receptor modulation and its implications in various neurological conditions.

Cat. No.

A60001

CAS No.

179333-18-7

NGD 94-1 dimaleate

NGD 94-1 dimaleate is a selective antagonist targeting the dopamine D4 receptor, demonstrating a high affinity for the cloned human D4.2 receptor with a Ki value of 3.6 nM. This compound modulates cognitive functions within the frontostriatal system and effectively regulates dopaminergic transmission in models of Phencyclidine (PCP)-induced behavior. NGD 94-1 dimaleate is a valuable tool for research focused on neurological diseases and disorders involving dopaminergic signaling.

Cat. No.

A60002

CAS No.

474432-66-1

FAUC 365

FAUC 365 is a highly selective antagonist for the dopamine D3 receptor, exhibiting a Ki value of 0.5 nM. It demonstrates significantly lower binding affinities at D4.4, D2short, and D2Long receptors, with Ki values of 340 nM, 2600 nM, and 3600 nM, respectively. FAUC 365 is primarily utilized in research related to schizophrenia and Parkinson's disease, providing valuable insights into dopamine receptor interactions and potential therapeutic interventions.

Cat. No.

A60009

CAS No.

2576-84-3

Metoclopramide dihydrochloride

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.

Cat. No.

A60013

CAS No.

124842-93-9

Y-20024 hydrochloride

Y-20024 hydrochloride is a selective D2 receptor antagonist known for its ability to cross the blood-brain barrier. It effectively inhibits Apomorphine-induced symptoms associated with attention deficit hyperactivity disorder (ADHD) in murine models and also mitigates Apomorphine-induced vomiting in canine subjects. This compound demonstrates prolactin-promoting activity and is valuable for research into neurological disorders such as ADHD and emesis.