Dopamine Receptors

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  1. Dopamine D-1 Receptor Antagonist

    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.
  2. D2R Agonist

    UNC9975 is a D2 receptor (D2R) agonist that demonstrates signaling bias through β-arrestin-mediated pathways while also acting as an antagonist of Gi-regulated cAMP production and a partial agonist for D2R/β-arrestin-2 interactions. This compound is valuable for research in antipsychotic drug development, facilitating the exploration of novel therapeutic approaches targeting dopaminergic signaling.
  3. Noncatechol Agonist

    Noncatechol agonist-1 is a potent noncatechol agonist primarily targeting the dopamine D1 receptor (D1R). It demonstrates full efficacy in activating both the D1R-G protein and D1R-β-arrestin2 pathways, with pEC50 values of 8.41 for D1R-mediated cAMP production and 7.7 for β-arrestin2 recruitment. This compound is valuable for research applications investigating dopamine signaling and its implications in neurobiology and pharmacology.
  4. Dopamine D1 Receptor Agonist

    Zelandopam free base is a specific agonist of the dopamine D1 receptor, demonstrating notable renal vasodilatory effects. This compound is effective in mitigating acute renal failure induced by Cisplatin, making it a valuable tool for research investigating renal protection and dopamine receptor signaling. Its oral bioactivity further enhances its utility in pharmacological studies related to renal function and neurotransmitter interactions.
  5. Dopamine D1 Receptor Agonist

    SKF 38393 is a selective agonist of the dopamine D1 receptor that activates the cAMP signaling pathway, enhancing dopamine release in the developing rat striatum. This compound has been shown to inhibit the proliferation of MCF-7 breast cancer cells with an IC50 of 0.1 μM. SKF 38393 is instrumental in research focused on neurodevelopmental disorders, dopamine-related diseases such as Parkinson's, and cancer biology.
  6. D3 Dopamine Receptor Agonist

    7-Hydroxy-DPAT is a selective agonist of the D3 dopamine receptor, known for its ability to modulate locomotor behavior and influence dopamine metabolism in the brain. This compound demonstrates significant pharmacological activity that can be utilized in research focused on neurological diseases and disorders. Its selectivity for the D3 receptor makes it a valuable tool for studies investigating dopamine-related pathways and their implications in various neurological conditions.
  7. D3R Agonist

    OS-3-106 is a potent and selective agonist of the dopamine D3 receptor (D3R), demonstrating a high binding affinity with a Ki value of 0.2 nM. This compound serves as a valuable tool in the study of D3R-mediated pathways, particularly in the context of psychoactive substance addiction research. Its specificity and efficacy make it suitable for exploring mechanisms underlying dopamine signaling and addiction-related behaviors.
  8. D1 Receptor Agonist

    SKF83822 hydrobromide is a potent agonist of the dopamine D1 receptor, primarily engaging Gs/olf signaling pathways to activate adenylyl cyclase. It is effective in stimulating intracellular cAMP production, making it a valuable tool for research in neuropharmacology and the study of dopamine-related disorders. Its selectivity for D1 receptors over PLC-coupled D1-like receptors underscores its utility in elucidating D1-mediated signaling processes.
  9. Dopamine D2 Receptor Agonist

    PF-00217830 is a selective agonist of the dopamine D2 receptor, demonstrating substantial efficacy in modulating dopaminergic signaling. It has been shown to inhibit spontaneous locomotor activity as well as reduce 2,5-dimethoxy-4-iodoamphetamine-induced head twitches in rodent models. This compound is valuable for studying the role of dopamine in neuropharmacology and assessing potential therapeutic strategies for disorders associated with dopamine dysregulation.
  10. Dopamine D2 Receptor Antagonist

    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.
  11. D4 dopamine receptor antagonist

    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.
  12. Dopamine Receptor Inhibitor

    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.
  13. Dopamine Receptor

    LY 171859 is a selective D2 receptor agonist that also displays notable reductase activity. This compound demonstrates enzymatic function within the cytoplasm of various tissues, including liver, lung, and kidney, and exhibits significant reductase activity in both rat and human blood. The reduction process mediated by LY 171859 is NADPH-dependent, with an apparent Km of 14.8 μM, and specifically incorporates the A-side hydrogen of NADPH into the reaction product. Additionally, this compound's enzymatic activity is sensitive to inhibition by cyanide and thiol reagents, making it a useful tool for studying dopamine receptor signaling and associated metabolic pathways.
  14. MOR Agonist

    MOR agonist-2 is a potent agonist of the mu-opioid receptor (MOR) with a Ki value of 564 nM, and it acts as an antagonist at the dopamine D3 receptor (D3R) with a Ki of 7.26 nM. This compound exhibits analgesic properties through its partial agonism at MOR, making it a valuable tool for research in pain management. Additionally, its D3R antagonism may help mitigate opioid misuse liability, offering potential therapeutic benefits in addiction studies.
  15. Antioxidant/Antitumor Agent

    Vanicoside E is an antioxidant and antitumor agent that targets L-Tyrosine and L-DOPA, demonstrating inhibitory activity with IC50 values of 45.23 μM and 189.96 μM, respectively. This compound is utilized in research focused on oxidative stress and tumor biology, making it valuable in studies aimed at understanding cancer progression and developing therapeutic strategies. Its properties support investigations into the modulation of key biochemical pathways relevant to tumor growth and survival.
  16. Dopamine D2 Receptor Antagonist

    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.
  17. Dopamine D1 Receptor Agonist

    Zelandopam anhydrous is a selective agonist of the dopamine D1 receptor, exhibiting potent renal vasodilatory effects. This compound demonstrates significant potential in alleviating acute renal failure induced by Cisplatin. It is valuable for research in nephrology and may aid in exploring therapeutic approaches for renal pathologies.
  18. Dopamine Antagonist

    Isoremoxipride is a dopamine antagonist that selectively targets the dopamine D2 receptor. This 3-methoxy isomer demonstrates significant affinity for the receptor, making it a valuable tool for investigating dopamine-related pathways. Its research applications include studies on neuropsychiatric disorders and the role of dopamine in various neurological conditions.
  19. D4R Antagonist

    D4R antagonist-1 is a selective antagonist of the dopamine D4 receptor (D4R) with an IC50 of 6.87 µM. This compound exhibits significant potential for use in research related to neurological disorders, including Parkinson's disease. Its ability to modulate D4R activity makes it a valuable tool for investigating the role of dopamine signaling in various physiological and pathological processes.
  20. D2R Agonist

    rel-Quinpirole dihydrochloride is a selective dopamine D2 receptor agonist that acts primarily on the D2R target. This compound exhibits significant biological activity in modulating dopamine signaling pathways and is utilized in research applications related to neurological diseases, including Parkinson's disease and schizophrenia. Its use can facilitate the investigation of dopaminergic functions and the development of potential therapeutic strategies.
  21. Dopamine Autoreceptor Antagonist

    AJ-76, classified as a dopamine autoreceptor antagonist, plays a crucial role in modulating dopamine levels in the brain. Research shows that AJ-76 enhances the synthesis and turnover of dopamine while exhibiting minimal influence on serotonin and norepinephrine activity. Additionally, AJ-76 effectively counteracts the sedative effects associated with low-dose apomorphine and demonstrates a modest antagonistic effect at postsynaptic dopamine receptors, making it a valuable tool for research in neuropharmacology and the study of dopamine-related disorders.
  22. Dopamine Agonist

    Lergotrile is a potent, orally active dopamine agonist that functions primarily as a prolactin secretion inhibitor. It exerts its biological activity by activating adenohypophyseal dopamine receptors, leading to the inhibition of prolactin release from the pituitary gland. This compound holds potential for research applications related to Parkinson's disease and other dopaminergic disorders.
  23. Antipsychotic Agent

    Piquindone is a potent antipsychotic agent that primarily targets the D2 dopaminergic receptor subtype, exhibiting sodium-dependent binding characteristics. This compound demonstrates significant biological activity relevant to the modulation of dopaminergic signaling and is utilized in research focused on schizophrenia and related neuropsychiatric disorders.
  24. D3 Receptor Antagonist

    Dopamine D3 receptor ligand-6 is a selective antagonist of the dopamine D3 receptor. This compound is valuable for investigating mechanisms involved in substance use disorders, including opioid and psychostimulant addiction. Its specificity for the D3 receptor makes it an important tool in pharmacological studies aimed at understanding and potentially mitigating addiction-related behaviors.
  25. Dopamine D(3)-Receptor Antagonist

    S33084 is a selective antagonist of the dopamine D(3) receptor, exhibiting pKi values of 8.72, 8.62, and 6.82 for cloned rat dopamine D3, native rat dopamine D3, and D2 receptors, respectively. This pharmacological profile indicates its potency and specificity in targeting the D(3) receptor. S33084 is primarily utilized in research focusing on neuropharmacology, aiding investigations into the role of dopamine signaling in various neurological disorders.
  26. Antidepressant Agent

    MeSeI is an antidepressant agent that weakly inhibits monoamine oxidase (MAO) A and B, exhibiting an IC50 value of 198.8 µM. It modulates the activity of dopamine receptor D2 and norepinephrine receptors α2 and β1, demonstrating antidepressant-like effects in animal models. MeSeI is administered orally, making it a convenient candidate for further research into mood disorders and related pharmacological applications.
  27. Neuroleptic Agent

    Fluphenazine decanoate dihydrochloride is a long-acting phenothiazine neuroleptic agent that primarily targets dopamine D2 receptors. It exhibits potent antipsychotic activity, making it valuable for the study of schizophrenia and related disorders. This compound is useful in research aimed at understanding neuropharmacology and the mechanisms underlying psychiatric conditions.
  28. Dopamine-Blocking Agent

    Oxiperomide is an orally active dopamine-blocking agent that primarily targets dopamine receptors. It exhibits significant antagonistic activity, making it useful for studying dopaminergic signaling pathways and related neurophysiological processes. This compound is applicable in research involving neuropsychiatric disorders and the exploration of dopamine's role in various physiological functions.
  29. Dopamine Uptake Inhibitor

    GBR-12879 dihydrochloride is a potent dopamine uptake inhibitor that selectively targets the dopamine transporter. Its primary mechanism involves preventing the reabsorption of dopamine, thus enhancing dopaminergic signaling. This compound is widely utilized in research to investigate the role of dopamine in neurological disorders and to explore potential therapeutic strategies for conditions such as depression and schizophrenia.
  30. Drug Metabolite

    Piribedil N-oxide is a metabolite of the dopamine receptor agonist Piribedil, primarily functioning as a drug metabolite. This compound retains the ability to interact with dopamine receptors, contributing to studies on dopamine signaling pathways and pharmacokinetics. Its characterization is essential for understanding the metabolic fate of Piribedil and its potential implications in neurological research and therapeutic applications.
  31. Dopamine D4 Receptor Agonist

    ABT-724 is a potent and highly selective agonist of the dopamine D4 receptor, exhibiting an EC50 of 12.4 nM for the human receptor. It also demonstrates efficacy as a partial agonist at the rat and ferret D4 receptors, with EC50 values of 14.3 nM and 23.2 nM, respectively. ABT-724 shows minimal activity against dopamine D1, D2, D3, and D5 receptors, making it a valuable tool for exploring the role of the D4 receptor in neurological conditions and potential therapeutic applications for erectile dysfunction.
  32. Dopamine D2 Receptor Agonist

    Quinelorane is a potent dopamine D2 receptor agonist. It has been shown to facilitate semen ejaculation while inhibiting penile erection in rat models. This compound is valuable for investigating mechanisms underlying sexual dysfunction and related therapeutic approaches.
  33. Stable Isotope

    Molindone-d8 is a deuterated form of the antipsychotic agent molindone, primarily used as a stable isotope in scientific research. Its primary mechanism involves dopamine receptor antagonism, reducing the effects of dopamine and helping to mitigate symptoms of schizophrenia. This labeled compound is particularly valuable in pharmacokinetic studies and metabolic research, allowing for precise tracking and analysis of drug behavior in biological systems.
  34. Stable Isotope

    Ropinirole-d3 is a deuterated analog of Ropinirole, primarily targeting D3 and D2 dopamine receptors. As a potent agonist, Ropinirole exhibits a Ki value of 29 nM for the D2 receptor, alongside pEC50 values of 7.4, 8.4, and 6.8 for human D2, D3, and D4 receptors, respectively. This stable isotope is useful in pharmacokinetic studies and can provide insights into the mechanism of action related to dopaminergic therapies, particularly in the context of Parkinson's disease research.
  35. Bisbenzylisoquinoline Alkaloid Secoderivative

    S-Secoantioquine is a bisbenzylisoquinoline alkaloid secoderivative that primarily targets dopamine receptors. It exhibits weak displacement activity on the 3H-SCH 23390 binding site and demonstrates certain displacement activity on the 3H-raclopride binding site in rat striate membrane experiments. This compound is useful for research in neuropharmacology and may aid in understanding the mechanisms of dopaminergic signaling.
  36. D3 Receptor Agonist

    PF 219061 is a selective agonist of the dopamine D3 receptor, exhibiting an EC50 of 15 nM. This compound demonstrates rapid absorption and efficient liver blood clearance, making it suitable for studying female sexual dysfunction. Its specificity for the D3 receptor allows for exploration of its potential therapeutic applications in related disorders.
  37. Dopamine D4 Receptor Agonist

    A-412997 is a selective agonist of the Dopamine D4 receptor, exhibiting Ki values of 12 nM for rat and 7.9 nM for human receptors. This compound has been demonstrated to enhance short-term memory and cognitive functions in rodent models, making it a valuable tool for research into psychiatric disorders and cognitive enhancement. Its specificity and potency facilitate studies on the Dopamine D4 receptor's role in neurobiology and medicine.
  38. Serotonin-Norepinephrine-Dopamine Releasing Agent

    4-Bromoamphetamine hydrochloride is a potent serotonin-norepinephrine-dopamine releasing agent (SNDRA) that exhibits significant stimulant effects. This compound plays a crucial role in neurological research, particularly in studies examining neurotransmitter release and potential neurotoxicity. Notably, 4-Bromoamphetamine hydrochloride has been associated with long-term depletion of serotonin, making it relevant for investigations into neurodegenerative conditions and the mechanisms of neurotransmitter regulation.
  39. Dopamine Receptor-blocking Agent

    (±)-Butaclamol hydrochloride is a dopamine receptor-blocking agent primarily utilized in neuropharmacological research. As the (+)-enantiomer of butaclamol, it demonstrates strong binding affinity to dopamine receptors, making it useful for studying dopamine-mediated pathways. This compound is often applied in the investigation of psychiatric disorders and the development of antipsychotic medications.
  40. Dopamine D2 Receptor Antagonist

    ADR 851 is a potent antagonist of the dopamine D2 receptor, known for its role in neurotransmitter signaling. This compound demonstrates significant activity in modulating dopaminergic pathways and has been utilized in research related to antiemetic therapies. Its effectiveness in targeting the D2 receptor makes it a valuable tool for studies investigating the mechanisms of nausea and emesis.
  41. Dopamine Receptor Agonist

    PD-168077 is a selective agonist for the dopamine D4 receptor, exhibiting a binding affinity (Ki) of 9 nM. This compound demonstrates significant biological activity in modulating dopaminergic signaling pathways, making it a useful tool for research focused on neuropharmacology and psychiatric disorders. Its specificity for the D4 receptor allows for targeted studies in areas such as schizophrenia and addiction, facilitating the exploration of therapeutic interventions.
  42. Dopamine D1 Receptor Agonist

    A-86929 functions as a potent and selective agonist for the dopamine D1 receptor, exhibiting a pKi value of 7.3. It has been shown to significantly induce rotational behavior in the 6-OHDA-induced unilateral nigrostriatal lesion rat model and improve motor function in the MPTP-induced Parkinson's disease marmoset model. Additionally, A-86929 may provide therapeutic insights for reducing cocaine-seeking behavior in rat studies and reversing Haloperidol-induced cognitive deficits in rhesus monkeys. This compound is valuable for research focused on neurological disorders.
  43. Dopamine Receptor Antagonist

    (-)-OSU6162 is a potent presynaptic dopamine receptor antagonist, primarily targeting the D2 dopamine receptor subtype. It exhibits inhibitory effects on dopamine release, making it valuable for research on dopaminergic signaling and its implications in neuropsychiatric disorders. This compound is useful for studying the role of dopamine in various biological systems and can aid in the development of treatments for conditions such as schizophrenia and addiction.
  44. D4 Receptor Antagonist

    PD-89211 is a selective antagonist of the dopamine D4 receptor, exhibiting a Ki value of 3.7 nM. It effectively reverses Quinpirole-induced [3H]thymidine uptake in CHOpro5 cells, with an IC50 of 2.1 nM. This compound plays a significant role in regulating dopamine and norepinephrine metabolism in the hippocampus, making it valuable for research into central nervous system disorders, including schizophrenia.
  45. Dopaminergic Agonist

    GYKI-32887 is a selective dopaminergic agonist that primarily targets dopamine receptors. This compound is notable for its ability to reduce motor activity levels in rodent models, making it a valuable tool for studying dopaminergic signaling pathways and motor function disorders. Its application spans across neuropharmacological research, particularly in understanding the mechanisms of drug action in neurological conditions.
  46. hD2R Activator

    Boc-MIF-1-Am is a potent enhancer of the human dopamine D2 receptor, exhibiting an EC50 value of 17.82 nM. This bioconjugate of melanostatin (MIF-1) and amantadine is primarily utilized in the study of dopaminergic signaling pathways and their implications in neurological disorders. Although Boc-MIF-1-Am demonstrates key biological activity, it has been noted to exhibit mild neurotoxicity at a concentration of 200 μM in SH-SY5Y cells, making careful consideration necessary in experimental designs.
  47. D2 Receptor Agonist

    Sumanirole is a highly selective D2 receptor full agonist, exhibiting an ED50 of approximately 46 nM. This compound is significant in the research of Parkinson's disease and restless leg syndrome, providing insights into dopaminergic signaling pathways. Its potent agonistic activity at the D2 receptor makes it valuable for exploring therapeutic strategies in these neurological disorders.
  48. Dopamine Receptor Control

    Aripiprazole N1-oxide is a metabolite of the atypical antipsychotic drug Aripiprazole, produced through the activity of cytochrome P450 isoforms CYP2D6 and CYP3A4. This compound primarily targets dopamine receptors, influencing dopaminergic signaling pathways. Aripiprazole N1-oxide is significant in research related to psychiatric disorders, enabling the study of receptor modulation and metabolic pathways in drug efficacy and safety.
  49. D1 Receptor Antagonist

    rel-Ecopipam hydrobromide is a potent D1 receptor antagonist with a Ki value of 1.30 nM. This compound effectively inhibits dopamine D1 receptor activity, making it a valuable tool for research in neuropharmacology and the study of dopamine signaling pathways. Its unique mechanism of action positions it for investigations into the role of D1 receptors in various neurobiological processes and potential therapeutic targets for neurological disorders.
  50. Dopamine Receptors Agonist

    Dinoxyline is a potent agonist of dopamine receptors, exhibiting high affinity with Ki values of 7 nM, 6 nM, 5 nM, and 43 nM for D1, D2, D3, and D4 receptors, respectively. This compound is valuable for investigating dopaminergic signaling pathways and their implications in neurological research. Its ability to selectively engage dopamine receptors makes it an essential tool for studies related to mood disorders, addiction, and other neurological conditions.

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