Dopamine Receptors

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.

A56868

CAS No.

932544-59-7

MLS6357

MLS6357, a D3 dopamine receptor (D3R)-selective positive allosteric modulator and antagonist, demonstrates significant antagonist activity in D3R-mediated assays, including BRET-based β-arrestin recruitment and Go-BRET assays, with IC50 values of 13 μM, 14 μM, and 17 μM respectively. It shows selectivity for D3R, with no notable activity on other dopamine receptor subtypes (D1R, D2R, D4R, D5R) at concentrations above 100 μM. MLS6357 serves as a valuable tool for investigating neuropsychiatric disorders, particularly in the context of substance use disorders.

Cat. No.

A57674

CAS No.

14698-07-8

Tipepidine citrate

Tipepidine citrate is a non-narcotic antitussive agent that inhibits dopamine D2 receptor-mediated GIRK current, effectively activating ventral tegmental area (VTA) dopamine neurons with an IC50 of 7.0 μM for IDA(GIRK). This compound demonstrates additional biological activities, including the activation of AMP-activated protein kinase (AMPK) and exhibiting antidepressant-like effects. Tipepidine citrate has also been shown to enhance the analgesic effect of carbamazepine and to improve metabolic parameters such as adipose tissue fibrosis and glucose intolerance in models of obesity induced by a high-fat diet.

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.

A57855

CAS No.

115688-97-6

PD 128483

PD 128483 is a selective agonist of the dopamine autoreceptor, primarily engaging the D2 receptor subtype. This compound is instrumental in research related to neurological diseases, facilitating studies on dopamine signaling and its implications in disorders such as schizophrenia and Parkinson’s disease. Its ability to modulate dopamine release provides valuable insights into neuropharmacology and therapeutic interventions.

Cat. No.

A57997

CAS No.

2888568-58-7

Heterobivalent ligand-1

Heterobivalent ligand-1 is a potent heterobivalent ligand targeting the Adenosine A2A-dopamine D2 receptor heteromer, exhibiting binding affinities of 2.1 nM for A2AR and 0.13 nM for D2R. This compound is valuable for studying receptor heteromerization and signal transduction in neurological research. Its unique design enables exploration of the functional interplay between these receptors in various biological contexts.

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.

A58366

CAS No.

90060-42-7

Nolomirole

Synonyms: CHF 1035 free base

Nolomirole is a selective agonist for the dopamine D2 receptor and the α2-adrenoceptor. It has demonstrated the ability to mitigate heart failure symptoms in models induced by Monocrotaline, such as improved cardiac output. This compound offers valuable insights for research into therapeutic strategies for cardiac dysfunction and heart failure.

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.

A58440

CAS No.

154189-24-9

Sibenadet hydrochloride

Synonyms: AR-C68397AA

Sibenadet hydrochloride is a dual agonist of the D2 dopamine receptor and the β2-adrenoceptor. It exhibits significant bronchodilator activity and has been shown to effectively inhibit sensory nerve activity in animal models of chronic obstructive pulmonary disease (COPD). Research indicates that Sibenadet hydrochloride reduces reflex cough, mucus production, and tachypnoea, making it a valuable tool for studying respiratory disorders and potential therapeutic interventions.

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.

A58462

CAS No.

75011-65-3

Ibopamine hydrochloride

Synonyms: SB 7505 hydrochloride; SKF 100168 hydrochloride

Ibopamine hydrochloride is an orally active dopamine derivative that primarily targets adrenergic and dopaminergic receptors. This compound exhibits agonistic effects leading to positive inotropic and vasodilatory actions, ultimately enhancing hemodynamics and renal function in models of heart failure. It can also be hydrolyzed to yield the active metabolite Epinine. Ibopamine hydrochloride is valuable for research applications focused on cardiovascular diseases, particularly congestive heart failure, owing to its favorable safety profile.

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.

A58580

CAS No.

154189-40-9

Sibenadet

Synonyms: AR-C68397AA free base; AR-C68397XX

Sibenadet is a dual agonist for dopamine D2 and β2-adrenoceptors, exhibiting selective activity at the β2-adrenoceptor. It has been shown to inhibit capsaicin-induced plasma protein extravasation in rat trachea, effectively suppressing edema resulting from sensory nerve fiber activation through β2-adrenoceptor activation. Sibenadet holds potential for advancing research into chronic obstructive pulmonary disease (COPD).

Cat. No.

A58605

CAS No.

548-42-5

Agroclavine

Agroclavine is a natural ergot alkaloid that acts as a D1 dopamine receptor and α1-adrenoceptor agonist. This compound exhibits notable biological activities, including anticancer and antimicrobial properties. Agroclavine is of interest in research applications related to dopamine signaling pathways, cancer therapeutics, and antimicrobial studies.

Cat. No.

A58671

CAS No.

80428-31-5

Mafoprazine methanesulfonate

Mafoprazine methanesulfonate is a phenylpiperazine derivative that primarily targets dopamine D2 receptors and exhibits α-adrenergic activity. This compound is known for its antipsychotic properties, potentially enhancing the activity of dopamine metabolites. It is valuable for research applications in understanding neurotransmitter pathways and assessing therapeutic interventions in psychiatric disorders.

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.

A58886

CAS No.

14862-80-7

UCSF34

UCSF34 is a Haloperidol analogue that selectively binds to the human D2L receptor, exhibiting an estimated pKi of 7.49. This compound is significant for its potential applications in schizophrenia research, facilitating the investigation of dopamine receptor modulation and related therapeutic strategies.

Cat. No.

A59082

CAS No.

1643462-64-9

(Rac)-Tavapadon

Synonyms: (Rac)-PF-06649751; (Rac)-CVL-751

(Rac)-Tavapadon is a potent and selective non-catechol agonist of the dopamine D1 receptor. It demonstrates full agonism in the Gs activation assay (EC50 = 0.8 nM) and partial agonism in the β-arrestin2 recruitment assay (EC50 = 68 nM). This compound exhibits significant antiparkinsonian activity, making it valuable for research into neurodegenerative diseases and dopamine signaling pathways.

Cat. No.

A59314

CAS No.

1400742-42-8

BB-22

BB-22 is a potent CB1 receptor ligand that acts as a dopamine activator. It exhibits a high affinity for CB1 receptors with a Ki value of 0.11 nM and demonstrates effective activation with an EC50 value of 2.9 nM. This compound may be valuable in studying the roles of endocannabinoid and dopaminergic systems in various neurological and psychiatric disorders.

Cat. No.

A59361

CAS No.

1159908-42-5

N-Arachidonyldopamine-d8

N-Arachidonyldopamine-d8 is a deuterium-labeled derivative of N-Arachidonyldopamine. This stable isotope is utilized in metabolic studies, allowing for precise tracking of molecular interactions and pathways in biological systems. Its key applications include research in neurobiology and pharmacology, particularly in understanding endocannabinoid signaling and dopamine receptor interactions.

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.

Cat. No.

A59565

CAS No.

250266-51-4

PNU-177864

PNU-177864 is a selective, orally active antagonist of the dopamine D3 receptor. It is known to induce phospholipid metabolism in vivo and exhibits potential anti-schizophrenia effects. This compound is valuable for research focused on dopaminergic modulation and the exploration of therapeutic strategies for schizophrenia.

Cat. No.

A59852

CAS No.

1217443-99-6

(S)-SCH-23390 hydrochloride

Synonyms: SCH-23388 hydrochloride

(S)-SCH-23390 hydrochloride is a potent dopamine D1-like receptor antagonist, specifically targeting the D1 and D5 receptor subtypes with Ki values of 0.2 nM and 0.3 nM, respectively. This compound is widely utilized in neuropharmacology research to elucidate the role of dopamine signaling in various physiological and pathological processes. Its application in investigating dopaminergic dysfunction makes it valuable for studies related to neurological disorders and therapeutic interventions.