Dopamine Receptors

Cat. No.

A60096

CAS No.

1261396-31-9

Ropinirole-d7 hydrochloride

Synonyms: SKF 101468-d7 hydrochloride

Ropinirole-d7 hydrochloride is a deuterium-labeled analog of Ropinirole hydrochloride, functioning as a potent agonist for D2 and D3 dopamine receptors. With a Ki value of 29 nM for the D2 receptor, it demonstrates strong biological activity, exhibiting pEC50 values of 7.4, 8.4, and 6.8 for human D2, D3, and D4 receptors, respectively, while showing no affinity for D1 receptors. This compound is particularly relevant in research focused on Parkinson's disease and neuropharmacology.

Cat. No.

A60097

CAS No.

219125-63-0

Dopamine D4 receptor ligand 2

Dopamine D4 receptor ligand 2 is a selective ligand targeting the dopamine D4 receptor, exhibiting a potent inhibitory effect with an IC50 of 0.057 nM. In contrast, the compound demonstrates much lower affinity for D2 (>1000 nM), 5-HT1A (220 nM), and α1 (270 nM) receptors. This selectivity positions it as a valuable tool for studies investigating the role of dopamine D4 in neuropharmacology and related research areas.

Cat. No.

A60099

CAS No.

3052236-39-9

Dopamine D3 receptor antagonist-2

Dopamine D3 receptor antagonist-2 is a selective antagonist for the dopamine D3 receptor, exhibiting a Ki value of 2.16 nM. This compound serves as a multitarget bitopic ligand and has potential applications in the study and treatment of various central nervous system disorders, including schizophrenia and addiction-related conditions. Its specificity for the D3 receptor makes it a valuable tool for research into dopamine-mediated neuropharmacology.

Cat. No.

A60100

CAS No.

1354030-25-3

UNC10099984A

UNC10099984A is a functionally selective ligand for the dopamine D2 receptor, exhibiting a Ki value of 4.6 nM and an EC50 value of 6.2 nM for β-arrestin. This compound is particularly valuable for investigating central nervous system disorders associated with D2 receptor modulation, facilitating research into dopamine signaling pathways and their therapeutic implications.

Cat. No.

A60101

CAS No.

131615-52-6

TISCH

TISCH is a potent and selective iodinated ligand that targets CNS D1 dopamine receptors, demonstrating a high affinity with a Kd value of 0.205 nM in rat striatal tissue. Its ability to cross the blood-brain barrier allows for effective distribution in regions with substantial D1 receptor density, making it a valuable pharmacological tool for characterizing these receptors. Additionally, TISCH, when labeled with I-123, has potential applications as an in vivo imaging agent for studying D1 dopamine receptor function in the central nervous system.

Cat. No.

A60102

CAS No.

150013-70-0

PD-143188

Synonyms: CI 1007

PD-143188 is a selective agonist of dopamine (DA) receptors, exhibiting Ki values of 25.5 nM for human D2 receptors and 16.6 nM for D3 receptors, while demonstrating lower affinity for D4.2 receptors (Ki=90.9 nM). This compound inhibits dopamine release, synthesis, and metabolism, leading to a reduction in cellular cyclic AMP levels, and demonstrates potential antipsychotic activity. PD-143188 is valuable for research in psychopharmacology and the exploration of dopamine-related pathways in neurological studies.

Cat. No.

A60103

CAS No.

155210-57-4

BAM-1110

BAM-1110 is a dopamine receptor agonist that demonstrates dose-dependent antiparkinsonian effects in MPTP-treated monkey models of Parkinson's disease. Its ability to activate dopamine receptors makes it a valuable tool for investigating Parkinson's disease and other neurological disorders. Additionally, BAM-1110 is characterized by minimal side effects, enhancing its suitability for research applications in this field.

Cat. No.

A60106

CAS No.

81855-35-8

CQP-201403

CQP-201403 is a selective dopamine receptor agonist that activates dopamine receptors to modulate neurotransmission. This compound is primarily utilized in the study of neurological diseases, offering insights into dopaminergic signaling and potential therapeutic pathways. Its application in research facilitates the exploration of mechanisms underlying conditions such as Parkinson's disease and schizophrenia.

Cat. No.

A60108

CAS No.

264262-71-7

SB-414796

SB-414796 is a selective antagonist of the dopamine D3 receptor, exhibiting potent inhibitory activity with a Ki value of 4 nM. This compound demonstrates significantly lower affinity for the D2 receptor, noted at 400 nM. It is capable of crossing the blood-brain barrier, making it suitable for investigating the role of dopamine D3 receptors in neuropharmacology and potential therapeutic applications related to related neuropsychiatric disorders.

Cat. No.

A60109

CAS No.

3033883-15-4

D3R/MOR antagonist 1

D3R/MOR Antagonist 1, a dual antagonist targeting the D3 receptor and the mu-opioid receptor, exhibits affinities of Ki values at 46.5 nM and 691 nM, respectively. This compound is designed to potentially elicit analgesic effects while minimizing opioid misuse liability through D3R antagonism. Its unique mechanism makes it a valuable tool for research in pain management and substance use disorders.

Cat. No.

A60110

CAS No.

189061-11-8

NGB 2904 hydrochloride

NGB 2904 hydrochloride is a selective antagonist of the dopamine D3 receptor, exhibiting a Ki value of 1.4 nM. This compound demonstrates a strong preference for the D3 receptor over other targets, including D2, 5-HT2, α1, D4, D1, and D5 receptors, as evidenced by significantly higher Ki values. NGB 2904 hydrochloride effectively antagonizes Quinpirole-stimulated mitogenesis, making it a valuable tool for research in dopamine signaling and related neurological studies.

Cat. No.

A60111

CAS No.

112192-04-8

Roxindole

Synonyms: EMD 49980

Roxindole is a potent agonist of dopamine autoreceptors, specifically targeting the D2-like subtype with low nanomolar affinity. This compound exhibits significant biological activity relevant to the study of both positive and negative symptoms associated with schizophrenia. Additionally, Roxindole functions as a 5-HT1A agonist and a serotonin uptake inhibitor, highlighting its potential utility in antipsychotic and antidepressant research applications.

Cat. No.

A60112

CAS No.

82668-33-5

U-99194

Synonyms: U-99194A free base; PNU-99194A; JPC-211

U-99194 is a selective and potent antagonist of the dopamine D3 receptor. This compound effectively inhibits D3 receptor activation induced by endogenous dopamine and exogenous D3 agonists, as demonstrated by its ability to negate the IPSC-suppressive effects of the D3 agonist PD 128907 in rat hippocampal slices. U-99194 also significantly suppresses nicotine-induced tremors in mice, making it a valuable tool for investigating dopamine D3 receptor-related motor disorders, especially those involving kinetic tremors.

Cat. No.

A60113

CAS No.

30909-51-4

Flupenthixol decanoate

Flupenthixol decanoate is a dopamine D2 receptor antagonist known for its antipsychotic properties. This compound is commonly utilized in research focused on schizophrenia and depression, enabling investigations into the underlying mechanisms of these psychiatric disorders. Its long-acting formulation supports studies on sustained therapeutic effects and dosing regimens.

Cat. No.

A60114

CAS No.

2882828-95-5

Dopamine D3 receptor ligand-2

Dopamine D3 receptor ligand-2 is a selective antagonist targeting the D3 dopamine receptor, exhibiting a Ki of 11.4 nM. This compound demonstrates high selectivity, showing minimal affinity for the D2 receptor with a Ki of 1228 nM. It is valuable for studies related to neurological disorders, addiction research, and the exploration of dopaminergic pathways.

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.

A60119

CAS No.

2040055-84-1

PF-4363467

PF-4363467 is a selective antagonist of the dopamine D3 and D2 receptors, demonstrating a Ki value of 3.1 nM for D3R and 692 nM for D2R. This compound effectively reduces opioid drug-seeking behavior while minimizing the associated side effects typically linked to D2 receptor antagonism. PF-4363467 is valuable for research applications focused on addiction and neuropharmacology, providing insights into dopaminergic modulation in therapeutic contexts.

Cat. No.

A60120

CAS No.

778630-77-6

Onzigolide

Synonyms: BIM-23A760; TBR-760

Onzigolide is a chimeric compound that acts as a potent agonist at dopamine type 2 (D2R) and somatostatin type 2 (SSTR2) receptors. This dual receptor activation may play a crucial role in modulating neuroendocrine and neurological functions. It is particularly relevant in research focused on neuropsychiatric disorders and endocrine-related conditions, contributing to the understanding of receptor interactions and their implications in therapeutic contexts.

Cat. No.

A60121

CAS No.

2846077-70-9

D4R antagonis-2

D4R antagonist-2 is a selective antagonist of the D4 dopamine receptor, exhibiting an IC50 of 6.52 µM. This compound demonstrates favorable in vitro pharmacokinetic properties and effective brain penetration. D4R antagonist-2 is suitable for research applications related to Parkinson's disease and other neurological disorders.

Cat. No.

A60122

CAS No.

37517-26-3

Pipotiazine palmitate

Pipotiazine palmitate is a dopamine receptor antagonist primarily used as an antipsychotic agent. As a long-acting phenothiazine derivative, it is suitable for intramuscular administration, providing sustained therapeutic effects. This compound is valuable in research applications focused on mental illnesses, particularly schizophrenia, facilitating studies into its neuropharmacological effects and treatment strategies.

Cat. No.

A60123

CAS No.

2813335-07-6

(-)-IHCH7041

(-)-IHCH7041 is a selective and orally active agonist of the dopamine D2 receptor, exhibiting a Ki value of 22.44 nM. It effectively activates the Gαi1 protein and β-arrestin2 signaling pathways with EC50 values of 1.38 nM and 2.75 nM, respectively. This compound has demonstrated potential in enhancing cognitive function and memory capacity, making it valuable for research into neurological disorders, including Alzheimer's disease.

Cat. No.

A60124

CAS No.

171752-56-0

Adrogolide

Synonyms: ABT-431; DAS-431

Adrogolide is a prodrug of A-86929, functioning as a selective agonist of the dopamine D1 receptor. Upon administration, Adrogolide is rapidly converted to A-86929 in the plasma, enhancing locomotor activity and improving behavioral outcomes. Additionally, it has been shown to reduce cocaine-seeking behavior, making it a valuable compound for research into the mechanisms underlying Parkinson's disease and addiction-related behaviors.

Cat. No.

A60125

CAS No.

20012-10-6

SKF 38393 hydrobromide

Synonyms: (±)-SKF-38393 hydrobromide

SKF 38393 hydrobromide is a selective agonist of the dopamine D1 receptor (D1DR), exhibiting a binding affinity characterized by an IC50 value of 110 nM. This compound is widely utilized in research to investigate the role of D1 receptors in various neurological processes, including cognition and motor control. Its specificity for D1DR makes it valuable for studies focused on dopaminergic signaling pathways and related diseases.

Cat. No.

A60126

CAS No.

67383-44-2

RU-24213 hydrochloride

RU-24213 hydrochloride is a selective agonist for the D-2 dopamine receptor, known to modulate dopaminergic signaling. Additionally, it acts as an antagonist at the kappa-opioid receptor, contributing to its pharmacological profile. This compound has been observed to induce stereotyped behaviors, making it valuable for research in neuropharmacology and the exploration of dopamine-related conditions.

Cat. No.

A60127

CAS No.

87056-78-8

Quinagolide

Synonyms: CV205-502

Quinagolide is a non-ergot dopamine D(2) receptor agonist that enhances dopamine activity. It is primarily utilized in the modulation of endocrine function, particularly in the suppression of hyperprolactinemia and its associated clinical symptoms. Quinagolide's significant biological activity makes it a valuable reagent for research in endocrine disorders and drug development, facilitating the study of dopamine's role in various physiological processes.