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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.
Synonyms: OPC 34712
Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD).
Synonyms: Ro10-5824
Ro 10-5824 dihydrochloride is a selective dopamine D4 receptor partial agonist, with Ki of 5.2 nM.
Bifeprunox is a potent partial agonist for the dopamine D2 receptor and the 5-HT1A receptor, exhibiting a pKi of 7.19 for cortex 5-HT1A and 8.83 for striatum D2. It demonstrates a pEC50 of 6.37 for hippocampus 5-HT1A. This compound is utilized in research related to antipsychotic mechanisms and is particularly relevant for studies focusing on schizophrenia.
PD 158771 is an antipsychotic agent that acts as a partial agonist at D2 and D3 dopamine receptors (Ki = 42.0 nM and 13.7 nM, respectively) and as an agonist at 5-HT1A receptors (Ki = 2.6 nM). This dual activity allows PD 158771 to demonstrate potential in modulating dopaminergic and serotonergic signaling. It is primarily utilized in research focused on understanding the mechanisms underlying psychotic disorders and the development of novel antipsychotic therapies.
Didesmethyl cariprazine is a metabolite of Cariprazine that acts as a partial agonist at D2 and D3 dopamine receptors while serving as a full agonist at the 5-HT1A receptor and an antagonist at the 5-HT2B receptor. With Ki values of 1.41 nM, 0.056 nM, 1.7 nM, and 0.52 nM for human D2L, human D3, human 5-HT1A, and human 5-HT2B, respectively, Didesmethyl cariprazine demonstrates significant interactions with these targets. This compound has been shown to dose-dependently inhibit the spontaneous activity of rat midbrain dopaminergic neurons, making it valuable for research in neuropharmacology and behavioral studies.
Synonyms: OPC-14597 monohydrate
Aripiprazole monohydrate is a potent partial agonist of the dopamine D2 receptor and an inverse agonist at the 5-HT2B and 5-HT2A receptors. Additionally, it exhibits partial agonist functionality at 5-HT1A, 5-HT2C, D3, and D4 receptors. This compound is primarily utilized in research focused on schizophrenia and has also been explored for potential applications in treating COVID-19.
Synonyms: PF-06649751; CVL-751
Tavapadon is a selective partial agonist of the dopamine D1 and D5 receptors. This orally active compound demonstrates significant efficacy in promoting motor function and alleviating disability, making it a promising candidate for research into Parkinson’s disease therapies. Tavapadon’s unique pharmacological profile supports its potential application in neurologic studies and drug development aimed at addressing dopamine-related disorders.
UCSF924 is a potent and selective partial agonist of the dopamine D4 receptor (DRD4), exhibiting an EC50 of 4.2 nM. This compound demonstrates no off-target effects on over 320 non-olfactory GPCRs, making it a valuable tool for research. UCSF924 is primarily used in studies related to neuropsychiatric disorders, facilitating a better understanding of the role of DRD4 in various neurological conditions.
SKF 83959 is a selective partial agonist of the dopamine D1-like receptors, demonstrating Ki values of 1.18 nM for D1 and 7.56 nM for D5, while exhibiting lower affinity for D2 and D3 receptors at 920 nM and 399 nM, respectively. Additionally, SKF 83959 acts as a potent allosteric modulator of the sigma-1 receptor. This compound is primarily utilized in research focused on cognitive dysfunction, Alzheimer's disease, and depression, providing insights into potential therapeutic pathways.
SKF 77434 hydrobromide is a selective partial agonist of the dopamine D1 receptor. This compound exhibits key biological activity in modulating dopaminergic pathways, making it valuable for research into addiction mechanisms, particularly cocaine addiction. Its specificity for the D1 receptor supports investigations into the role of dopamine signaling in various neuropsychiatric conditions.
SKF 83959 hydrobromide is a potent partial agonist of the dopamine D1-like receptors, demonstrating Ki values of 1.18 nM for D1, 7.56 nM for D5, and significantly higher values for D2 and D3 receptors. This compound also acts as a powerful allosteric modulator of the sigma (σ)-1 receptor and belongs to the benzazepine class. SKF 83959 hydrobromide is utilized in research focused on cognitive dysfunction, with applications in studying Alzheimer's disease and depression.
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.
BP 897 is a potent partial agonist of the dopamine D3 receptor and exhibits weak antagonistic activity at the D2 receptor. With a high affinity for the D3 receptor (Ki=0.92 nM) and significantly lower affinity for the D2 receptor (Ki=61 nM), BP 897 is a valuable tool for studying dopaminergic signaling. This compound is primarily used in research related to neuropsychiatric disorders and the role of dopamine receptors in therapeutic contexts.
FAUC 346 is a highly selective partial agonist of the dopamine D3 receptor, exhibiting an EC50 of 1.5 nM. This compound demonstrates significant biological activity in modulating dopaminergic signaling, making it a valuable tool for research focused on neuropharmacology and psychiatric disorders. FAUC 346 can be utilized to explore the therapeutic potential of D3 receptor modulation in various neurological conditions.
Ro 10-5824 is a selective partial agonist of the dopamine D4 receptor (D4R), exhibiting a Ki value of 5.2 nM. This compound is noted for its ability to enhance novel object exploration in C57BL/6 mice, making it a valuable reagent for studies investigating cognitive behaviors and dopaminergic signaling. Ro 10-5824 is useful in research applications related to neuropharmacology and the understanding of psychiatric disorders.
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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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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.
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.
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.
FAUC-312 is a tetrahydropyrimidine that acts as a selective partial agonist of the dopamine D4 receptor, exhibiting a Ki value of 1.5 nM. This compound modulates dopaminergic signaling and has potential applications in researching neuropsychiatric disorders, including schizophrenia and attention deficit hyperactivity disorder (ADHD). Its specificity towards the D4 receptor allows for the exploration of receptor-specific pathways and therapeutic interventions.
Synonyms: DAB-452 fumarate
Aplindore fumarate is a partial agonist of the dopamine D2 receptor, primarily utilized in neurological research. This compound has shown potential in studies related to Parkinson's disease and schizophrenia, offering insights into dopaminergic signaling pathways. Its activity makes it a valuable tool for investigating therapeutic strategies and understanding the underlying mechanisms of these disorders.
