Dopamine Receptors

Cat. No.

A45918

CAS No.

112108-01-7

Ecopipam

Synonyms: SCH 39166

Ecopipam is a potent and selective antagonist of the dopamine D1 and D5 receptors, displaying inhibition constants (Kis) of 1.2 nM and 2.0 nM, respectively. It exhibits over 40-fold selectivity against D2, D4, 5-HT, and α2a receptors, with Kis of 0.98 μM, 5.52 μM, 0.08 μM, and 0.73 μM, respectively. Ecopipam is primarily utilized in research related to schizophrenia and obesity, offering insights into the modulation of dopaminergic signaling pathways.

Cat. No.

A45943

CAS No.

274694-98-3

LE 300

LE 300 is a potent and selective antagonist of the dopamine D1-like receptors, demonstrating inhibition constants (Kis) of 1.9 nM and 7.5 nM for human dopamine D1 and D5 receptors, respectively. Additionally, LE 300 acts as an antagonist of the 5-HT2A receptor, with a pA2 value of 8.32 in rat tail artery assays. This compound is valuable for research into dopamine receptor signaling pathways and neuropharmacology.

Cat. No.

A45968

CAS No.

54241-01-9

Clozapine hydrochloride

Synonyms: HF 1854 hydrochloride

Clozapine hydrochloride is an antipsychotic agent primarily targeting dopamine D2 receptors, where it acts as a potent antagonist with a Ki value of 75 nM. This compound also exhibits strong inhibitory activity against muscarinic M1 and serotonin 5HT2A receptors, with Kis of 9.5 nM and 4 nM, respectively. Additionally, clozapine hydrochloride serves as a selective agonist for the muscarinic M4 receptor, demonstrating an EC50 of 11 nM. This profile makes clozapine hydrochloride valuable for research related to schizophrenia and other neuropsychiatric disorders.

Cat. No.

A45999

CAS No.

71675-92-8

Esamisulpride

Synonyms: (S)-Amisulpride; (S)-Aramisulpride; (S)-DAN 2163

Esamisulpride is a potent antagonist of the dopamine D2 and D3 receptors, exhibiting Ki values of 4.43 nM for D2R and 0.72 nM for D3R. Additionally, it functions as a 5-HT7 receptor antagonist with a Ki of 900 nM. This compound is primarily employed in research related to schizophrenia and depression, providing valuable insights into dopaminergic and serotonergic system modulation.

Cat. No.

A46007

CAS No.

1159977-64-6

Ziprasidone amino acid

Synonyms: Ziprasidone Impurity C; Ziprasidone open ring impurity

Ziprasidone amino acid is a known impurity of Ziprasidone, functioning primarily as a 5-HT (serotonin) and dopamine receptor antagonist. This compound demonstrates significant antipsychotic activity, making it valuable in the study of neurological disorders. Its unique properties can aid researchers in investigating the mechanisms of antipsychotic effectiveness and receptor interactions in related drug development.

Cat. No.

A46013

CAS No.

2587360-22-1

Ecopipam hydrobromide

Synonyms: SCH 39166 hydrobromide

Ecopipam hydrobromide is a highly selective antagonist of dopamine D1 and D5 receptors, exhibiting dissociation constants (Kis) of 1.2 nM and 2.0 nM, respectively. It demonstrates over 40-fold selectivity compared to D2, D4, 5-HT, and α2a receptors. This compound is valuable for research investigating the pathophysiology of schizophrenia and obesity, making it a useful tool for studying dopaminergic signaling pathways and related disorders.

Cat. No.

A46025

CAS No.

108179-91-5

SKF-83566 hydrobromide

SKF-83566 hydrobromide is a selective antagonist of the D1-like dopamine receptors, exhibiting high blood-brain barrier permeability and oral bioavailability. This compound functions as a competitive inhibitor of the dopamine transporter (DAT), with an IC50 of 5.7 μM, and demonstrates a weaker antagonistic effect on the vascular 5-HT2 receptor (Ki=11 nM). Additionally, SKF-83566 selectively inhibits adenylyl cyclase 2 (AC2) over AC1 and AC5, making it a valuable tool for studying Parkinson's disease and nicotine dependence.

Cat. No.

A46080

CAS No.

898532-85-9

D3/5-HT receptor modulator-1

D3/5-HT receptor modulator-1 is a selective antagonist for dopamine D3 receptors and 5-HT2A receptors, while also functioning as a partial agonist at 5-HT1A receptors. With measured Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for the respective targets, this compound exhibits a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. Its unique pharmacological profile suggests potential applications in the development of atypical antipsychotic therapies and for studying dopaminergic and serotonergic signaling pathways.

Cat. No.

A46091

CAS No.

884305-07-1

Keto Ziprasidone

Keto Ziprasidone is a known impurity of the antipsychotic agent Ziprasidone, which functions primarily as a combined antagonist of serotonin (5-HT) and dopamine receptors. This compound is crucial for research applications focusing on drug metabolism and pharmacokinetics, particularly in understanding the potential effects of impurities on therapeutic efficacy and safety profiles. Its analysis can aid in the development of quality control measures in pharmaceutical formulations.

Cat. No.

A46093

CAS No.

131999-28-5

5-HT6/7 antagonist 1

5-HT6/7 Antagonist 1 is a potent antagonist of the 5-HT6, 5-HT7, and D2 receptors, exhibiting selectivity that spares M1 receptors and hERG channels. This compound's multifunctional activity makes it valuable for research into neuropharmacology and the modulation of serotonergic and dopaminergic systems. It provides a useful tool for studying disorders related to these receptor pathways, including anxiety, depression, and schizophrenia.

Cat. No.

A46100

CAS No.

884305-08-2

Hydroxy ziprasidone

Hydroxy ziprasidone is a known impurity of the antipsychotic agent ziprasidone, which functions primarily as a combined antagonist of both serotonin (5-HT) and dopamine receptors. This compound is useful for researchers studying the pharmacological properties and metabolic pathways of ziprasidone, as well as for quality control in the synthesis of pharmaceutical formulations. Its presence can provide insights into the drug's safety, efficacy, and potential side effects.

Cat. No.

A46109

CAS No.

47739-98-0

Clocapramine

Synonyms: Clocarpramine; 3-Chlorocarpipramine

Clocapramine is a selective antagonist of the 5-HT2A receptor, with additional inhibitory effects on D2 dopamine receptors. This compound exhibits notable properties in modulating serotonin and dopamine signaling, making it relevant for neuropharmacological research. Clocapramine can be utilized in studies related to psychiatric disorders, including depression and schizophrenia, as well as the characterization of receptor interactions in neural pathways.

Cat. No.

A49400

CAS No.

59453-24-6

Bromperidol hydrochloride

Synonyms: R-11333 hydrochloride

Bromperidol hydrochloride is an antipsychotic agent that primarily functions as a potent antagonist of central dopamine D2 receptors. It exhibits significant antipsychotic activity, making it valuable in the treatment of various psychotic disorders. Additionally, Bromperidol hydrochloride has demonstrated synergistic effects in combination with Spectinomycin, highlighting its potential in antimicrobial research against Mycobacteria.

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.

A53338

CAS No.

1254-47-3

Fluphenazine hydrochloride

Fluphenazine hydrochloride functions as a potent dopamine receptor antagonist, primarily targeting postsynaptic dopamine-2 receptors within mesolimbic, nigrostriatal, and tuberoinfundibular pathways. This compound exhibits significant biological activity by blocking neuronal voltage-gated sodium channels, leading to effects on behavior, such as the antagonism of methylphenidate-induced stereotyped gnawing and inhibition of climbing behavior in murine models. Fluphenazine hydrochloride is valuable for research into psychotic disorders and painful peripheral neuropathy related to diabetes, and it has demonstrated potential for inhibition of SARS-CoV-2.

Cat. No.

A53458

CAS No.

3093-66-1

Fluphenazine dimaleate

Fluphenazine dimaleate is a potent dopamine receptor antagonist primarily targeting postsynaptic dopamine-2 receptors in the mesolimbic, nigrostriatal, and tuberoinfundibular pathways. Its ability to antagonize neuronal voltage-gated sodium channels contributes to its effectiveness in modulating dopaminergic activity. Fluphenazine dimaleate is valuable in research addressing psychosis, diabetic neuropathy, and behavioral studies, including the inhibition of Methylphenidate-induced stereotyped behaviors in animal models. Emerging studies also suggest its potential in inhibiting SARS-CoV-2, positioning it as a multifaceted tool in scientific investigation.

Cat. No.

A55656

CAS No.

210688-56-5

PD 168568

PD 168568 is a potent and orally active antagonist of the dopamine receptor D4 (DRD4), featuring an isoindolinone structure. It demonstrates strong selectivity for the D4 receptor over D2 and D3 receptors, with Ki values of 8.8 nM, 1842 nM, and 2682 nM, respectively. This compound is valuable for research applications focusing on glioblastoma (GBM), providing insights into the role of DRD4 in tumor biology.

Cat. No.

A57750

CAS No.

1010382-72-5

PF-04363467

PF-04363467 is a selective antagonist of the dopamine D3 receptor (D3R). It demonstrates dose-dependent modulation of the electroencephalogram (EEG) profile in freely moving rats, highlighting its potential to influence neural activity. This compound effectively reduces opioid drug-seeking behavior while minimizing undesired side effects associated with D2 receptor antagonism. PF-04363467 is valuable for research into addiction, cognitive disorders, and mental illness.

Cat. No.

A58107

CAS No.

128022-68-4

ADX-10061

Synonyms: CEE 03-310; NNC 687

ADX-10061 is a potent dopamine D1 receptor antagonist exhibiting a Ki value of 9.1 nM for adenylyl cyclase and 5.8 nM for the D1 receptor, alongside much higher Ki values for D2 and 5-HT2 receptors. This selective inhibition allows for targeted investigations into dopamine-related pathways. ADX-10061 is a valuable tool for studies of schizophrenia and other neuropsychiatric disorders, facilitating the exploration of the therapeutic potential of dopamine modulation in various research contexts.

Cat. No.

A58437

CAS No.

298-45-3

Bulbocapnine

Bulbocapnine is an aporphine isoquinoline alkaloid that acts as an antagonist at dopamine and α-adrenergic receptors, alongside possessing anti-peroxidative properties. This compound has been shown to reduce intracellular dopamine levels and inhibit tyrosine hydroxylase activity with a Ki value of 0.20 mM. Additionally, Bulbocapnine decreases intracellular Ca2+ concentration and mitigates the dose-dependent inhibitory effects of dopamine on heart rate acceleration, making it a valuable tool for research in cardiovascular physiology and neurobiology.

Cat. No.

A58461

CAS No.

80428-29-1

Mafoprazine

Mafoprazine is a phenylpiperazine derivative that functions as a dopamine receptor antagonist, primarily targeting the D2 receptor. Its antipsychotic effects are thought to arise from its blockade of dopaminergic transmission, combined with α-adrenergic activity. Additionally, Mafoprazine may enhance the activity of dopamine metabolites, making it a valuable tool for research into the mechanisms underlying psychotic disorders and dopamine-related pathways.

Cat. No.

A58534

CAS No.

55905-53-8

Clebopride

Clebopride is an orally active dopamine receptor antagonist that primarily targets dopamine D2 receptors. This compound exhibits antiemetic and prokinetic properties, making it useful for investigating functional gastrointestinal disorders. Clebopride's ability to modulate dopamine signaling positions it as a valuable tool in pharmacological research relevant to gastrointestinal motility and related conditions.

Cat. No.

A58843

CAS No.

36504-94-6

(±)-Butaclamol hydrochloride

Synonyms: AY-23,028; dl-Butaclamol hydrochloride

(±)-Butaclamol hydrochloride is a neuroleptic agent that acts as an antagonist for adrenergic and dopamine receptors. It effectively antagonizes stereotyped behaviors and emesis induced by amphetamine and apomorphine, as well as inhibiting discriminative avoidance behavior. Additionally, it induces catalepsy in rat models, making it a valuable tool for research in behavioral pharmacology and neuropharmacology.

Cat. No.

A59549

CAS No.

883631-51-4

Seridopidine

Seridopidine is a potent dopamine receptor antagonist that primarily targets D2 and D3 receptors. It exhibits significant antipsychotic activity, making it valuable for research in neurological and psychiatric disorders. This compound is useful in studies investigating the roles of dopamine in the central nervous system, particularly in understanding mechanisms underlying schizophrenia and related conditions.

Cat. No.

A59551

CAS No.

1783978-03-9

PNU-177864 hydrochloride

PNU-177864 hydrochloride is a potent and selective antagonist of the dopamine D3 receptor. This compound is known to influence phospholipid metabolism in vivo and exhibits potential anti-schizophrenia activity. It serves as a valuable tool for researchers exploring the role of dopamine receptors in neurological disorders and for developing therapeutic strategies.