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Dopamine receptor agonists and antagonists act on the five G protein-coupled receptors that respond to dopamine. The receptors form two groups, with D1 and D5 in the D1-like class and D2, D3 and D4 in the D2-like class. D1-like receptors stimulate adenylyl cyclase, whereas D2-like receptors inhibit it and lower cyclic adenosine monophosphate (cAMP) levels. Dopamine signaling controls movement, reward, motivation and hormone release, and is studied in Parkinson's disease and psychiatric research. Ligands here include the agonist rotigotine HCl, the D2 antagonists L-741626 and domperidone, and the D3-preferring ligand BP897.
ST 198 is a selective D3 receptor (D3R) antagonist that demonstrates oral bioactivity. It effectively inhibits nicotine-induced conditioned place preference (CPP) at specific doses targeting D3R. This compound is valuable for research investigating neurological diseases and the mechanisms underlying dopaminergic signaling.
Dopamine D3 receptor antagonist-3 is a selective positive allosteric modulator-antagonist targeting the D3 dopamine receptor (D3R) that effectively penetrates the blood-brain barrier. It demonstrates robust antagonist activity in D3R-mediated β-arrestin recruitment assays, exhibiting an IC50 of 2.5 μM and a Kd of 0.49 μM, and in D3R-mediated Go-BRET assays, with an IC50 of 0.34 μM. This reagent is suitable for investigating neuropsychiatric disorders, including substance use disorder, providing valuable insights into D3R's role in these conditions.
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Synonyms: (-)-PW0464
Razpipadon ((-)-PW0464) is a dopamine receptor partial agonist with a specific affinity for the D1 receptor. This compound is crucial for research into dopamine-mediated psychiatric disorders, as it allows for the investigation of receptor activity and its impact on neurochemical signaling. Razpipadon serves as a valuable tool for elucidating the role of dopamine in various neurological and psychiatric conditions.
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Timiperone is an antipsychotic compound that exhibits a strong affinity for the dopamine D2 receptor in the brain. It demonstrates significant antipsychotic activity and effectively inhibits stereotyped behaviors. Timiperone is primarily utilized in research related to schizophrenia, contributing to the understanding of dopaminergic pathways involved in this disorder.
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.
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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.
Synonyms: SKF-104557
N-Despropyl Ropinirole (SKF-104557) is a potent agonist targeting dopamine D2 and D3 receptors. As an active metabolite of Ropinirole, it exhibits full agonistic activity at human D2 and D3 receptors while acting as a partial agonist at the hD4 receptor. This compound is valuable for research applications investigating dopaminergic signaling and potential therapeutic strategies for diseases such as Parkinson's and schizophrenia.
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.
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.
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.
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.
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(±)-N-Propylnorapomorphine functions as a dopamine D2-receptor agonist, selectively activating the D2 receptor pathway. This compound demonstrates significant biological activity related to dopaminergic signaling, making it valuable for research in neuropharmacology and the study of dopamine-related disorders. Its application extends to investigating the physiological and behavioral effects of dopamine modulation.
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Synonyms: 2-Bromolisuride; Bromlisuride
Bromerguride is an analogue of the ergot-derived dopamine agonist Lisuride, functioning primarily as a central antidopaminergic agent. This compound is utilized in pharmacological research to investigate the modulation of dopaminergic pathways and their implications in neurological conditions. Its unique properties make it a valuable tool for studying dopamine receptor interactions and their effects on various biological systems.
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4-Amino-PPHT is a derivative of PPHT that selectively targets dopamine D-2 receptors, exhibiting a binding affinity characterized by a Ki value of 6.8 nM. This compound is essential for investigating the role of dopamine signaling in neuropharmacology and related research applications. It provides a valuable tool for studies focused on neuropsychiatric disorders and the development of therapeutic agents targeting dopamine receptors.
CJB-090 dihydrochloride is a partial agonist targeting dopamine D3 receptors. This compound demonstrates unique partial agonist properties in vitro and has been shown to provoke yawning responses in monkeys with a history of cocaine use. CJB-090 is also effective in reducing the reinstatement of cocaine-induced behaviors, making it a valuable tool for studies on addiction and dopamine receptor functions.
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.
Dopamine D2 receptor agonist-2 is a selective agonist targeting the dopamine D2 receptor, exhibiting a binding affinity with a Ki value of 11.2 nM. This compound demonstrates biased agonism, making it a valuable tool for investigating mechanisms underlying antipsychotic effects. It is suitable for research applications focused on the modulation of dopamine signaling and the study of psychiatric disorders.
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.
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FAUC 3019 is a partial agonist of the dopamine D4 receptor. This compound demonstrates a significant stimulatory effect on penile erection in male rats, particularly at low concentrations. FAUC 3019 is a valuable tool for exploring the physiological mechanisms underlying erectile function and has potential applications in the study of sexual health and related disorders.
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.
BP14979 is a selective agonist of the dopamine D3 receptor, primarily utilized in the investigation of neurological disorders. Its structural properties allow for the modulation of D3 receptor efficacy, making it a valuable tool in the development of ligands with enhanced selectivity and affinity. By understanding the differences in efficacy compared to D3 receptor antagonists, BP14979 offers significant potential for optimizing therapeutic agents in drug development.
Pramipexole-d7-1 dihydrochloride is a deuterium-labeled analog of Pramipexole dihydrochloride, a selective agonist of dopamine D2-type receptors. This compound effectively penetrates the blood-brain barrier and exhibits Ki values of 2.2 nM, 3.9 nM, 0.5 nM, and 1.3 nM for the D2-type receptor, D2, D3, and D4 receptors, respectively. Pramipexole-d7-1 dihydrochloride is valuable for research on Parkinson's disease and restless legs syndrome, facilitating advanced studies in neuropharmacology and the pharmacokinetics of dopamine receptor interactions.
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.
Dopamine D2 receptor agonist-3 is a selective partial agonist for the D2 receptor, exhibiting a pEC50 of 8.3. Additionally, it acts as an antagonist at the D3 receptor with a pEC50 of less than 5.5. This compound is valuable for research into dopamine receptor signaling pathways and may provide insights into neuropsychiatric disorders.
R(+)-6-Bromo-APB hydrobromide acts as a dopamine (DA) agonist, influencing dopaminergic signaling pathways. Research has demonstrated that it notably enhances the expression of μ-opioid receptor (MOR) mRNA in the nucleus accumbens. This compound is valuable for investigating the interplay between dopamine and opioid systems in neurobiological studies.
