Dopamine Receptors

Cat. No.

A59890

CAS No.

14008-44-7

Metopimazine

Synonyms: EXP999; RP9965

Metopimazine is a selective dopamine D2 receptor antagonist belonging to the phenothiazine class. It primarily targets the chemoreceptor trigger zone, effectively inhibiting nausea and vomiting associated with chemotherapy while maintaining low central side effects due to limited blood-brain barrier penetration. This compound is indicated for the management of chemotherapy-induced nausea and vomiting, though caution is advised regarding its application in acute gastroenteritis due to potential risks. Metopimazine is primarily utilized in research related to anti-dopaminergic anti-emetic therapies.

Cat. No.

A59891

CAS No.

1173023-36-3

L-745870 hydrochloride

L-745870 hydrochloride is a potent and selective antagonist of the dopamine D4 receptor, exhibiting a Ki of 0.43 nM. This compound displays significantly lower affinity for D2 and D3 receptors, with Ki values of 960 nM and 2300 nM, respectively, and has moderate interaction with 5-HT2 receptors, sigma sites, and α-adrenoceptors. L-745870 hydrochloride is suited for research applications investigating the role of dopamine D4 receptors in neuropsychiatric disorders and drug development.

Cat. No.

A59892

CAS No.

166591-11-3

Adrogolide hydrochloride

Synonyms: ABT-431 hydrochloride; DAS-431 hydrochloride

Adrogolide hydrochloride is a stable prodrug that converts to the dopamine D1 receptor agonist A-86929. It exhibits significant activity in attenuating the symptoms of Parkinson's disease in marmoset models, alleviating MPTP-induced motor impairments and reducing the risk of dyskinesias. Additionally, Adrogolide hydrochloride has demonstrated the ability to reverse cognitive deficits induced by Risperidone in non-human primate studies, making it a valuable tool for neurological research applications.

Cat. No.

A59893

CAS No.

189060-98-8

NGB 2904

NGB 2904 is a potent and selective antagonist of the dopamine D3 receptor, demonstrating a Ki value of 1.4 nM. This compound exhibits high selectivity for the D3 receptor compared to other targets, including D2, 5-HT2, and α1 receptors, with Kis ranging from 217 to >10,000 nM. NGB 2904 effectively antagonizes Quinpirole-stimulated mitogenesis, making it a valuable tool for research into dopamine-related pathways and potential therapeutic applications in neuropsychiatric disorders.

Cat. No.

A59894

CAS No.

1386162-69-1

ML417

ML417 is a selective agonist for the D3 dopamine receptor (D3R), demonstrating an EC50 of 38 nM. This compound effectively stimulates D3R-mediated β-arrestin translocation, facilitates G protein signaling, and induces pERK phosphorylation while exhibiting minimal interference with other GPCR pathways. ML417 also offers neuroprotective effects against toxin-induced neurodegeneration of dopaminergic neurons, making it a valuable tool for studying neurodegenerative diseases and dopamine-related disorders.

Cat. No.

A59895

CAS No.

108050-82-4

Roxindole hydrochloride

Synonyms: EMD 38362

Roxindole hydrochloride is a potent agonist of dopamine autoreceptors, primarily targeting the D2-like subtype with low nanomolar affinity. This compound exhibits significant antipsychotic and antidepressant properties, making it valuable in the research of both positive and negative symptoms of schizophrenia. Additionally, Roxindole acts as a 5-HT1A agonist and a 5-HT uptake inhibitor, demonstrating high affinity for the 5-HT1A receptor (IC50=0.9 nM), contributing to its multifaceted therapeutic potential.

Cat. No.

A59896

CAS No.

7681-67-6

Propionylpromazine hydrochloride

Synonyms: Propiopromazine hydrochloride

Propionylpromazine hydrochloride is a dopamine receptor D2 (DRD2) antagonist. This compound exhibits potential in the modulation of dopaminergic signaling, making it relevant for studies related to Parkinson's disease and other disorders associated with dopamine dysregulation. Its ability to inhibit DRD2 may aid in understanding the physiological and pathological roles of dopamine in various neurological contexts.

Cat. No.

A59897

CAS No.

74115-08-5

SKF 83822

SKF 83822 is an atypical agonist of the dopamine D1 receptor, primarily activating adenylyl cyclase (AC) without influencing phospholipase C (PLC). This compound enhances cAMP production through AC stimulation, making it valuable for research into dopamine signaling pathways. SKF 83822 is particularly relevant in studies investigating schizophrenia and related neuropsychiatric disorders.

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.

A59902

CAS No.

495-40-9

Butyrophenone

Synonyms: 1-Phenylbutan-1-one; 1-Phenyl-1-butanone

Butyrophenone is a dopamine receptor (DA Receptor) antagonist that plays a significant role in neuropharmacological studies. This compound is primarily utilized in research focused on mental disorders such as schizophrenia and bipolar disorder. Its ability to modulate dopaminergic signaling makes it valuable for investigating the underlying mechanisms of these conditions and potential therapeutic interventions.

Cat. No.

A59903

CAS No.

675599-62-9

PG01037 dihydrochloride

PG01037 dihydrochloride is a potent and selective antagonist of the dopamine D3 receptor, with a dissociation constant (Ki) of 0.7 nM. This compound is valuable in research applications exploring the role of dopamine signaling in various neurological and psychiatric disorders. Its ability to inhibit D3 receptor activity makes it a pivotal tool for investigating potential therapeutic interventions and understanding dopamine-related pathways.

Cat. No.

A59904

CAS No.

83898-65-1

Domperidone monomaleate

Synonyms: R33812 monomaleate

Domperidone monomaleate is a selective antagonist of the dopamine D2 receptor. This compound exhibits notable antiemetic and prokinetic properties by influencing the chemoreceptor trigger zone and enhancing gastrointestinal motility. It is primarily utilized in research related to gastrointestinal disorders and neuropharmacology.

Cat. No.

A59905

CAS No.

100999-26-6

CY 208-243

CY 208-243 is a selective agonist of the dopamine D1 receptor, demonstrating significant antiparkinsonian activity. This compound is valuable for researchers investigating dopamine signaling pathways and related neurodegenerative conditions. Its specificity for the D1 receptor allows for precise modulation of dopaminergic activity, making it a potent tool in the study of Parkinson's disease and other related disorders.

Cat. No.

A59906

CAS No.

92169-45-4

Neuromedin N

Synonyms: Neuromedin N (rat, mouse, porcine, canine)

Neuromedin N is a potent dopamine D2 receptor modulator that enhances agonist binding in rat neostriatal membranes. This compound plays a significant role in the investigation of dopaminergic signaling pathways and their implications in neurobiology. Neuromedin N's ability to influence dopamine receptor activity makes it valuable for research into neuropsychiatric disorders and related therapeutic strategies.

Cat. No.

A59907

CAS No.

24678-13-5

Lenperone

Synonyms: AHR 2277 free base

Lenperone is an antipsychotic compound that primarily targets dopamine receptors. It exhibits notable efficacy in alleviating depressive symptoms associated with psychotic disorders. Research applications include studying its effects on neurotransmitter modulation and exploring its potential in psychiatric treatment protocols.

Cat. No.

A59908

CAS No.

166173-78-0

Fallypride

Fallypride is a potent antagonist of the dopamine D2 and D3 receptors, providing valuable insights into dopaminergic function. As a radiolabeled compound (Fallypride-18F), it serves as an effective positron emission tomography (PET) radiotracer for studying neurological disorders and neuropharmacology. Its application in imaging facilitates the exploration of dopamine-related mechanisms in various psychiatric and neurodegenerative conditions.

Cat. No.

A59909

CAS No.

982-24-1

Clopenthixol

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.

Cat. No.

A59911

CAS No.

444724-92-9

Dopamine D4 receptor antagonist-1

Dopamine D4 receptor antagonist-1 is a selective antagonist for the dopamine D4 receptor (DRD4), exhibiting a Ki of 9.0 nM for the Hd4.2 cell line. This compound is valuable for research into the pathophysiology of schizophrenia, providing insights into dopaminergic signaling pathways and potential therapeutic interventions. Its specificity and potency make it a useful tool for studying DRD4-related biological processes.

Cat. No.

A59912

CAS No.

23694-17-9

Sultopride hydrochloride

Synonyms: LIN-1418 hydrochloride

Sultopride hydrochloride is a selective antagonist of the dopamine D2 receptor, exerting its primary mechanism of action through blocking dopamine signaling. This compound is chiefly utilized in research investigating the role of dopamine in neuropsychiatric disorders and the pharmacological modulation of dopaminergic pathways. Its ability to selectively inhibit D2 receptor activity makes it a valuable tool for exploring dopamine-related biological processes and the development of therapeutic agents.

Cat. No.

A59913

CAS No.

2258608-78-3

UCM-1306

UCM-1306 is a potent allosteric modulator of the human dopamine D1 receptor, exhibiting oral bioactivity. This compound enhances the maximal effect of endogenous dopamine at both human and murine D1 receptors, making it a valuable tool in Parkinson’s disease research. UCM-1306 is useful for investigating motor symptoms and for addressing cognitive impairments often associated with prolonged Parkinson’s disease.

Cat. No.

A59914

CAS No.

4093-35-0

Bromopride

Bromopride is a selective, irreversible antagonist of the dopamine D2 receptor, demonstrating significant utility in pharmacological research. This compound effectively crosses the blood-brain barrier, inhibiting the vomiting center and enhancing gastrointestinal motility, thereby exhibiting both antiemetic and prokinetic properties. Bromopride's ability to block dopamine-mediated vomiting reflexes and stimulate gastrointestinal smooth muscle contraction makes it a valuable reagent for investigating digestive system disorders, particularly gastric hypomotility, nausea, and vomiting, without adversely affecting abdominal wall healing in animal models.

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.

A59916

CAS No.

170858-33-0

Sonepiprazole

Synonyms: PNU-101387G; U-101387G

Sonepiprazole is a selective D4 dopamine receptor antagonist, exhibiting Ki values of 3.6 nM for the rat D4 receptor and 10.1 nM for the human D4.2 receptor, while showing weaker affinities of 5147 nM and 7430 nM for the rat D2 dopamine and histamine H1 receptors, respectively. This compound demonstrates potential for modulating dopaminergic signaling and is useful in investigating the role of D4 receptors in neurological and psychiatric conditions. Sonepiprazole may serve as a valuable tool for researchers studying the therapeutic implications of dopamine receptor antagonism.

Cat. No.

A59918

CAS No.

53515-91-6

Haloperidol lactate

Haloperidol lactate is a potent antipsychotic agent primarily targeting dopamine receptors. It is commonly utilized in the management of acute and chronic schizophrenia, as well as Gilles de la Tourette's syndrome. Additionally, Haloperidol lactate is valuable for research on psychotic disorders, aiding in the exploration of therapeutic pathways and interventions.

Cat. No.

A59919

CAS No.

66104-22-1

Pergolide

Synonyms: LY127809 free base

Pergolide is an ergot-derived dopamine receptor agonist that primarily targets D1 and D2 dopamine receptors. This compound demonstrates significant biological activity in modulating dopaminergic signaling, making it a valuable tool in the study of Parkinson's disease and related neurological disorders. Pergolide is commonly utilized in research to explore therapeutic mechanisms and potential treatments for motor function impairments associated with dopaminergic deficiencies.