Dopamine Receptors

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.

A59954

CAS No.

67469-57-2

GBR 12783

GBR 12783 is a selective dopamine uptake inhibitor that targets dopamine receptors with high potency. It effectively inhibits [3H]dopamine uptake in striatal synaptosomes from rats and mice, exhibiting IC50 values of 1.8 nM and 1.2 nM, respectively. This compound has been shown to enhance memory performance and increase hippocampal acetylcholine release in rodent models, making it valuable for research in neuropharmacology and cognitive function studies.

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.

A59959

CAS No.

1347744-96-0

A-412997 dihydrochloride

A-412997 dihydrochloride is a selective agonist of the dopamine D4 receptor. It has been shown to enhance cognitive performance in rodent models, making it a valuable tool for investigating neuropsychiatric disorders. This compound can be employed in research focused on understanding the role of dopamine D4 receptor modulation in cognitive function and its implications in various psychiatric conditions.

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.

A59962

CAS No.

97548-97-5

Quinelorane dihydrochloride

Synonyms: LY163502

Quinelorane dihydrochloride is a potent agonist of the dopamine D3 and D2 receptors, facilitating modulation of dopaminergic signaling pathways. This compound shows promise in the investigation of neurological and psychiatric disorders, offering valuable insights into the mechanistic underpinnings of related conditions. Research applications may include studies on dopamine receptor function, neuropharmacology, and potential therapeutic interventions.

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.

A59965

CAS No.

1638667-81-8

DETQ

DETQ is an allosteric potentiator of the dopamine D1 receptor, enhancing receptor activity through a unique binding site. In HEK293 cells expressing the human D1 receptor, DETQ significantly increases cyclic AMP levels with an EC50 of 5.8 nM and a binding affinity (Kb) of 26 nM. The compound exhibits approximately 30-fold reduced potency at rodent D1 receptors and shows no activity against the human D5 receptor. This specificity makes DETQ a valuable tool for research involving dopamine signaling pathways and their implications in neurobiology.

Cat. No.

A59966

CAS No.

1257326-23-0

NPEC-caged-dopamine

NPEC-caged-dopamine is a photolabile compound designed to release dopamine upon ultraviolet light activation (360 nm). This compound serves as a valuable tool for studies on dopamine signaling, facilitating targeted activation of D1 receptors. Research applications include investigating the dynamic roles of dopamine in neurobiology and the modulation of neural circuits.

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.

A59968

CAS No.

5845-67-0

Cyclo(glycyl-L-leucyl)

Synonyms: Cyclo(leu-gly)

Cyclo(glycyl-L-leucyl) is a neuropeptide that specifically inhibits dopamine receptors, playing a crucial role in modulating dopaminergic signaling. This compound has been shown to down-regulate dopamine receptor activity and reduce dopaminergic supersensitivity, particularly in the context of morphine-induced analgesia in animal models. Cyclo(glycyl-L-leucyl) holds promise for potential therapeutic applications in preventing tardive dyskinesias and L-DOPA-induced dyskinesias, making it valuable for research in neuropharmacology and movement disorders.

Cat. No.

A59969

CAS No.

115092-85-8

Carmoxirole hydrochloride

Synonyms: EMD 45609 hydrochloride

Carmoxirole hydrochloride is a selective agonist of the dopamine D2 receptor, demonstrating significant peripheral activity. It is primarily used in research related to antihypertensive mechanisms and cardiovascular physiology. This compound is valuable for studies exploring dopamine receptor signaling and its implications in blood pressure regulation.

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.

A59974

CAS No.

85976-54-1

(R)-Preclamol

Synonyms: (+)-3-PPP

(R)-Preclamol is a dopamine agonist that stimulates both autoreceptors and postsynaptic receptors. It has been demonstrated to inhibit the locomotor activity of mice and rats at low doses, making it a valuable tool for research in neuropharmacology and behavior studies related to dopamine signaling. This compound can be utilized in studies investigating the effects of dopamine modulation on various physiological processes and behavioral outcomes.

Cat. No.

A59975

CAS No.

62717-63-9

SKF-75670 hydrobromide

SKF-75670 hydrobromide is a potent partial agonist of the Dopamine D1 receptor. This compound exhibits significant activity in modulating dopamine signaling pathways, making it a valuable tool for studying neuropharmacology and the effects of dopaminergic modulation. Additionally, SKF-75670 hydrobromide serves as an antagonist to cocaine, providing insights into addiction mechanisms and potential therapeutic strategies. Its applications are crucial for research in neurological disorders and drug interactions involving the dopamine system.

Cat. No.

A59976

CAS No.

483-34-1

(-)-Isocorypalmine

Synonyms: Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine

(-)-Isocorypalmine is a potent ligand for dopamine receptors, specifically isolated from the crude base fraction of Corydalis chaerophylla. This compound demonstrates high affinity, with a Km value of 4.63 ± 0.71 μM, as confirmed by recombinant CYP719A21. It holds significant promise for research in neuropharmacology and studies related to dopamine signaling pathways.

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.

A59980

CAS No.

146725-34-0

MFZ 2-13

Synonyms: O-456

MFZ 2-13 is an N-demethylated intermediate and N-nor-analogue of MFD 2-12 that targets the human dopamine receptor. It functions as an inhibitor of dopamine uptake, exhibiting an IC50 of 1.4 nM. This compound is valuable for research in neuropharmacology and the study of psychoactive substances.

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.

A59982

CAS No.

189681-70-7

Aplindore

Synonyms: DAB-452

Aplindore is a potent dopamine D2 receptor agonist, exhibiting a pKi value of 9.1. This compound is significant in the study of Parkinson's disease, as it aids in elucidating dopaminergic signaling pathways. Its activity provides valuable insights into therapeutic strategies for managing symptoms associated with dopaminergic deficits.

Cat. No.

A59985

CAS No.

1399442-97-7

Matsupexolum

Synonyms: Matsupexole

Matsupexolum is a dopamine receptor agonist that selectively activates dopamine receptors, facilitating neurotransmission. This compound demonstrates significant biological activity in modulating dopaminergic signaling pathways and can be utilized in research focused on neuropharmacology, psychiatry, and the study of movement disorders. Its application may provide insights into the therapeutic potential for conditions such as schizophrenia and Parkinson's disease.