Dopamine Receptors

Cat. No.

A60074

CAS No.

52423-56-0

Bromopride hydrochloride

Bromopride hydrochloride is a selective, irreversible dopamine D2 receptor antagonist with oral bioactivity. It effectively crosses the blood-brain barrier to inhibit the vomiting center while promoting gastrointestinal motility by enhancing smooth muscle contraction. This compound is valuable for research into digestive system disorders, including gastric hypomotility, nausea, and vomiting, and demonstrates no harmful effects on abdominal wall healing in the context of postoperative abdominal infections.

Cat. No.

A60075

CAS No.

264869-71-8

SLV310

SLV310 is an orally active antagonist of the dopamine D2 receptor, exhibiting a Ki value of 5 nM, and also acts as a serotonin reuptake inhibitor. It effectively antagonizes Apomorphine-induced climbing behavior and 5-HTP-induced serotonin syndrome in murine models, with an ED50 of 5.6 and 5.9 mg/kg, respectively. This compound serves as a valuable tool for antipsychotic research, particularly in studies related to schizophrenia.

Cat. No.

A60077

CAS No.

179089-90-8

CP-293019

CP-293019 is a selective antagonist of the dopamine D4 receptor, characterized by a Ki value of 3.4 nM. This compound effectively inhibits apomorphine-induced hyperactivity in rat models, making it a valuable tool for research into neuropharmacology and the role of dopamine receptors in behavioral studies. Its application extends to studies exploring the mechanisms underlying dopamine-related disorders.

Cat. No.

A60078

CAS No.

75067-66-2

Bromperidol decanoate

Synonyms: R46541

Bromperidol decanoate is a dopamine receptor antagonist primarily utilized in the treatment of schizophrenia. Its notable biological activity includes the inhibition of dopaminergic pathways, which contributes to its antipsychotic effects. This compound is relevant in research focused on psychotropic drug development and the exploration of dopamine-related disorders.

Cat. No.

A60079

CAS No.

871351-60-9

Ordopidine

Synonyms: ACR-325

Ordopidine is a selective dopamine D2 receptor antagonist that effectively inhibits hyperactivity induced by psychostimulants. This compound is valuable for neurological research, providing insights into the modulation of dopaminergic pathways and the study of related disorders. Its application may facilitate the exploration of therapeutic strategies for conditions such as schizophrenia and other dopamine-related disorders.

Cat. No.

A60081

CAS No.

1982347-43-2

VK4-116

VK4-116 is a selective antagonist of the Dopamine D3 receptor (D3R) with a Ki value of 6.84 nM. This compound effectively inhibits Oxycodone-induced hyperlocomotion and locomotor sensitization in mouse models, demonstrating its potential as a therapeutic agent for addiction-related behaviors. Furthermore, VK4-116 has been shown to prevent the acquisition of Oxycodone-induced conditioned place preference (CPP) in rat models, highlighting its applications in addiction research.

Cat. No.

A60086

CAS No.

24677-86-9

Lenperone hydrochloride

Synonyms: AHR 2277

Lenperone hydrochloride is a dopamine antagonist primarily used in the study of neurological disorders. This antipsychotic compound has been shown to reduce gastroesophageal sphincter pressure in healthy canine models, providing insights into its physiological effects. It serves as a valuable reagent for research applications focused on antipsychotic mechanisms and the treatment of various neurological diseases.

Cat. No.

A60088

CAS No.

3052236-36-6

Dopamine D3 receptor antagonist-1

Dopamine D3 receptor antagonist-1 is a selective antagonist of the dopamine D3 receptor, exhibiting a binding affinity with a Ki value of 1.58 nM. This compound is of particular interest in the study of central nervous system disorders, as it may play a role in modulating dopaminergic signaling pathways. Its unique bitopic ligand properties suggest applications in researching both psychiatric and neurodegenerative conditions, providing valuable insights into therapeutic interventions.

Cat. No.

A60090

CAS No.

52669-92-8

Dehydrate haloperidol

Dehydrate haloperidol is a selective antagonist of the human dopamine D2 receptor, exhibiting a pKd of 8 and a pKi of 8. This compound is primarily utilized in research focused on schizophrenia and related disorders, providing insights into dopamine signaling pathways and their role in neuropsychiatric conditions.

Cat. No.

A60093

CAS No.

158985-08-1

L-750667

L-750667 is a selective antagonist of the dopamine D4 receptor. This compound has been shown to specifically bind to dopamine D4 receptors in the rat retina, exhibiting a Kd value of 0.06 nM. L-750667 plays a significant role in the regulation of the light-sensitive cAMP pool, making it a valuable tool for studying dopamine signaling pathways and their implications in neurobiology and vision research.

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.

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.

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.

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.

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.

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.

A60128

CAS No.

2983777-91-7

D3R ligand 1

D3R ligand 1 is a potent and selective antagonist targeting the dopamine receptor D3R, with a Ki value of 66 nM. Utilizing a THPB template, this compound effectively inhibits both G-protein- and β-arrestin-mediated signaling pathways. D3R ligand 1 is valuable for researchers investigating dopamine receptor signaling and its implications in neuropharmacology.

Cat. No.

A60130

CAS No.

58939-37-0

A-69024

A-69024 is a selective antagonist of the dopamine D-1 receptor, demonstrating a Ki value of 12.6 nM for D-1 and a significantly higher Ki value of 1290 nM for the D-2 receptor. This compound's specificity enables researchers to investigate the role of dopamine D-1 receptor modulation in various neurological and psychiatric disorders. A-69024 is valuable for studies examining dopamine-related pathways and potential therapeutic approaches.

Cat. No.

A60140

CAS No.

1032714-06-9

Dopamine D2 receptor antagonist-3

Dopamine D2 receptor antagonist-3 is a selective antagonist of the dopamine D2 receptor, displaying a pIC50 of 5.52. This compound demonstrates antipsychotic effects, evidenced by its ability to reduce apomorphine-induced agitation in rat models. It is a valuable tool for research into psychiatric and neurological disorders, facilitating the study of dopaminergic signaling pathways and potential therapeutic interventions.

Cat. No.

A60141

CAS No.

1021868-80-3

L-750667 triHydrochloride

L-750667 triHydrochloride is a selective antagonist of the D4 dopamine receptor, exhibiting a Ki value of 0.51 nM. Its radiolabeled derivative, [125I]L-750667, demonstrates a Kd of 0.16 nM for D4 receptor binding. This compound is capable of reversing dopamine-induced inhibition of cAMP accumulation, making it a valuable tool for investigating the distribution and function of D4 dopamine receptors in the central nervous system. L-750667 triHydrochloride has significant applications in neuroscience and psychiatry research.

Cat. No.

A60142

CAS No.

873445-73-9

SV 293

SV 293 is a selective antagonist that primarily targets dopamine D2 receptors with a binding affinity that is 100-fold greater than that of D3 and D4 receptor subtypes. This compound exhibits neutral antagonist activity and effectively blocks the effects of the full agonist quinpirole in forskolin-dependent adenylate cyclase inhibition assays and electrophysiological assays. SV 293 serves as a valuable pharmacological tool for investigating the role of D2-like receptor subtypes in dopamine-related pathways associated with neurological, neuropsychiatric, and movement disorders.

Cat. No.

A60147

CAS No.

86580-77-0

BRL 34778

BRL 34778 is a highly selective dopamine D2 receptor antagonist with a Ki value of 2.14 nM, demonstrating significant potency in receptor inhibition. It exhibits antipsychotic properties while minimizing extrapyramidal side effects and sedation. This compound is valuable for investigating neurological disorders, particularly schizophrenia, and contributes to research focused on the modulation of dopaminergic pathways in the brain.