Dopamine Receptors

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  1. Lisuride Analogue

    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.
  2. PPHT Derivatives

    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.
  3. Dopamine Receptor

    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.
  4. Dopamine Receptor Agonist

    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.
  5. Dopamine Receptor Antagonist

    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.
  6. Dopamine Receptor

    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.
  7. Dopamine D2 Receptor Antagonist

    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.
  8. Dopamine Receptor

    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.
  9. Stable Isotope

    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.
  10. D2 Receptor Partial Agonist

    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.
  11. Stable Isotope

    Ropinirole-d7 hydrochloride is a deuterium-labeled analog of Ropinirole hydrochloride, functioning as a potent agonist for D2 and D3 dopamine receptors. With a Ki value of 29 nM for the D2 receptor, it demonstrates strong biological activity, exhibiting pEC50 values of 7.4, 8.4, and 6.8 for human D2, D3, and D4 receptors, respectively, while showing no affinity for D1 receptors. This compound is particularly relevant in research focused on Parkinson's disease and neuropharmacology.
  12. Dopamine Receptor Antagonist

    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.
  13. Functionally Selective Ligand for Dopamine D2 Receptor

    UNC10099984A is a functionally selective ligand for the dopamine D2 receptor, exhibiting a Ki value of 4.6 nM and an EC50 value of 6.2 nM for β-arrestin. This compound is particularly valuable for investigating central nervous system disorders associated with D2 receptor modulation, facilitating research into dopamine signaling pathways and their therapeutic implications.
  14. Dopamine Receptor Inhibitor

    TISCH is a potent and selective iodinated ligand that targets CNS D1 dopamine receptors, demonstrating a high affinity with a Kd value of 0.205 nM in rat striatal tissue. Its ability to cross the blood-brain barrier allows for effective distribution in regions with substantial D1 receptor density, making it a valuable pharmacological tool for characterizing these receptors. Additionally, TISCH, when labeled with I-123, has potential applications as an in vivo imaging agent for studying D1 dopamine receptor function in the central nervous system.
  15. Dopamine Receptor Agonist

    BAM-1110 is a dopamine receptor agonist that demonstrates dose-dependent antiparkinsonian effects in MPTP-treated monkey models of Parkinson's disease. Its ability to activate dopamine receptors makes it a valuable tool for investigating Parkinson's disease and other neurological disorders. Additionally, BAM-1110 is characterized by minimal side effects, enhancing its suitability for research applications in this field.
  16. Dopamine Receptor Agonist

    CQP-201403 is a selective dopamine receptor agonist that activates dopamine receptors to modulate neurotransmission. This compound is primarily utilized in the study of neurological diseases, offering insights into dopaminergic signaling and potential therapeutic pathways. Its application in research facilitates the exploration of mechanisms underlying conditions such as Parkinson's disease and schizophrenia.
  17. Dopamine D3 Receptor Antagonist

    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.
  18. D3R/MOR Antagonist

    D3R/MOR Antagonist 1, a dual antagonist targeting the D3 receptor and the mu-opioid receptor, exhibits affinities of Ki values at 46.5 nM and 691 nM, respectively. This compound is designed to potentially elicit analgesic effects while minimizing opioid misuse liability through D3R antagonism. Its unique mechanism makes it a valuable tool for research in pain management and substance use disorders.
  19. Dopamine D3 Receptor Antagonist

    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.
  20. D3 receptor antagonist

    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.
  21. Dopamine D2 Receptor Antagonist

    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.
  22. D3 Receptor Ligand

    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.
  23. Dopamine Receptor Inhibitor

    Opromazine hydrochloride is a dopamine receptor inhibitor known for its sedative and antiemetic effects. It primarily reduces dopaminergic activity by blocking dopamine receptors in the brain, making it useful in the treatment of psychiatric disorders such as schizophrenia and psychosis. Additionally, studies have investigated its metabolites through various microsomal enzymes, highlighting differences in formation rates and the variability of drug-metabolizing enzymes in human liver and placenta microsomes, which is essential for understanding its pharmacokinetic profile.
  24. D3/D2 Receptor Antagonist

    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.
  25. D2R/SSTR2 Agonist

    Onzigolide is a chimeric compound that acts as a potent agonist at dopamine type 2 (D2R) and somatostatin type 2 (SSTR2) receptors. This dual receptor activation may play a crucial role in modulating neuroendocrine and neurological functions. It is particularly relevant in research focused on neuropsychiatric disorders and endocrine-related conditions, contributing to the understanding of receptor interactions and their implications in therapeutic contexts.
  26. D4R Antagonist

    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.
  27. Antipsychotic Agent

    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.
  28. Dopamine D2 Receptor Agonist

    (-)-IHCH7041 is a selective and orally active agonist of the dopamine D2 receptor, exhibiting a Ki value of 22.44 nM. It effectively activates the Gαi1 protein and β-arrestin2 signaling pathways with EC50 values of 1.38 nM and 2.75 nM, respectively. This compound has demonstrated potential in enhancing cognitive function and memory capacity, making it valuable for research into neurological disorders, including Alzheimer's disease.
  29. D-2 Dopamine Receptor Agonist

    RU-24213 hydrochloride is a selective agonist for the D-2 dopamine receptor, known to modulate dopaminergic signaling. Additionally, it acts as an antagonist at the kappa-opioid receptor, contributing to its pharmacological profile. This compound has been observed to induce stereotyped behaviors, making it valuable for research in neuropharmacology and the exploration of dopamine-related conditions.
  30. Neuroleptic Agent

    (±)-Butaclamol hydrochloride is a neuroleptic agent that acts as an antagonist for adrenergic and dopamine receptors. It effectively antagonizes stereotyped behaviors and emesis induced by amphetamine and apomorphine, as well as inhibiting discriminative avoidance behavior. Additionally, it induces catalepsy in rat models, making it a valuable tool for research in behavioral pharmacology and neuropharmacology.
  31. Dopamine Activator/CB1 Receptor Ligand

    BB-22 is a potent CB1 receptor ligand that acts as a dopamine activator. It exhibits a high affinity for CB1 receptors with a Ki value of 0.11 nM and demonstrates effective activation with an EC50 value of 2.9 nM. This compound may be valuable in studying the roles of endocannabinoid and dopaminergic systems in various neurological and psychiatric disorders.
  32. Stable Isotope

    N-Arachidonyldopamine-d8 is a deuterium-labeled derivative of N-Arachidonyldopamine. This stable isotope is utilized in metabolic studies, allowing for precise tracking of molecular interactions and pathways in biological systems. Its key applications include research in neurobiology and pharmacology, particularly in understanding endocannabinoid signaling and dopamine receptor interactions.
  33. Dopamine receptor/α-adrenergic receptor antagonist/antiperoxidant

    Bulbocapnine is an aporphine isoquinoline alkaloid that acts as an antagonist at dopamine and α-adrenergic receptors, alongside possessing anti-peroxidative properties. This compound has been shown to reduce intracellular dopamine levels and inhibit tyrosine hydroxylase activity with a Ki value of 0.20 mM. Additionally, Bulbocapnine decreases intracellular Ca2+ concentration and mitigates the dose-dependent inhibitory effects of dopamine on heart rate acceleration, making it a valuable tool for research in cardiovascular physiology and neurobiology.
  34. D2 dopamine receptor and β2-adrenocepto agonist

    Sibenadet hydrochloride is a dual agonist of the D2 dopamine receptor and the β2-adrenoceptor. It exhibits significant bronchodilator activity and has been shown to effectively inhibit sensory nerve activity in animal models of chronic obstructive pulmonary disease (COPD). Research indicates that Sibenadet hydrochloride reduces reflex cough, mucus production, and tachypnoea, making it a valuable tool for studying respiratory disorders and potential therapeutic interventions.
  35. Dopamine Receptor Antagonist

    Mafoprazine is a phenylpiperazine derivative that functions as a dopamine receptor antagonist, primarily targeting the D2 receptor. Its antipsychotic effects are thought to arise from its blockade of dopaminergic transmission, combined with α-adrenergic activity. Additionally, Mafoprazine may enhance the activity of dopamine metabolites, making it a valuable tool for research into the mechanisms underlying psychotic disorders and dopamine-related pathways.
  36. Dopamine Receptor Antagonist

    Clebopride is an orally active dopamine receptor antagonist that primarily targets dopamine D2 receptors. This compound exhibits antiemetic and prokinetic properties, making it useful for investigating functional gastrointestinal disorders. Clebopride's ability to modulate dopamine signaling positions it as a valuable tool in pharmacological research relevant to gastrointestinal motility and related conditions.
  37. Dopamine D2/β2-adrenoceptor Agonist

    Sibenadet is a dual agonist for dopamine D2 and β2-adrenoceptors, exhibiting selective activity at the β2-adrenoceptor. It has been shown to inhibit capsaicin-induced plasma protein extravasation in rat trachea, effectively suppressing edema resulting from sensory nerve fiber activation through β2-adrenoceptor activation. Sibenadet holds potential for advancing research into chronic obstructive pulmonary disease (COPD).
  38. D1 Dopamine Agonist

    Agroclavine is a natural ergot alkaloid that acts as a D1 dopamine receptor and α1-adrenoceptor agonist. This compound exhibits notable biological activities, including anticancer and antimicrobial properties. Agroclavine is of interest in research applications related to dopamine signaling pathways, cancer therapeutics, and antimicrobial studies.
  39. A2AR-D2R Heteromer Ligand

    Heterobivalent ligand-1 is a potent heterobivalent ligand targeting the Adenosine A2A-dopamine D2 receptor heteromer, exhibiting binding affinities of 2.1 nM for A2AR and 0.13 nM for D2R. This compound is valuable for studying receptor heteromerization and signal transduction in neurological research. Its unique design enables exploration of the functional interplay between these receptors in various biological contexts.
  40. D3R PAM-Antagonist

    MLS6357, a D3 dopamine receptor (D3R)-selective positive allosteric modulator and antagonist, demonstrates significant antagonist activity in D3R-mediated assays, including BRET-based β-arrestin recruitment and Go-BRET assays, with IC50 values of 13 μM, 14 μM, and 17 μM respectively. It shows selectivity for D3R, with no notable activity on other dopamine receptor subtypes (D1R, D2R, D4R, D5R) at concentrations above 100 μM. MLS6357 serves as a valuable tool for investigating neuropsychiatric disorders, particularly in the context of substance use disorders.
  41. DRD4 Antagonist

    PD 168568 is a potent and orally active antagonist of the dopamine receptor D4 (DRD4), featuring an isoindolinone structure. It demonstrates strong selectivity for the D4 receptor over D2 and D3 receptors, with Ki values of 8.8 nM, 1842 nM, and 2682 nM, respectively. This compound is valuable for research applications focusing on glioblastoma (GBM), providing insights into the role of DRD4 in tumor biology.
  42. D3R Antagonist

    PF-04363467 is a selective antagonist of the dopamine D3 receptor (D3R). It demonstrates dose-dependent modulation of the electroencephalogram (EEG) profile in freely moving rats, highlighting its potential to influence neural activity. This compound effectively reduces opioid drug-seeking behavior while minimizing undesired side effects associated with D2 receptor antagonism. PF-04363467 is valuable for research into addiction, cognitive disorders, and mental illness.
  43. Dopamine Autoreceptor Agonist

    PD 128483 is a selective agonist of the dopamine autoreceptor, primarily engaging the D2 receptor subtype. This compound is instrumental in research related to neurological diseases, facilitating studies on dopamine signaling and its implications in disorders such as schizophrenia and Parkinson’s disease. Its ability to modulate dopamine release provides valuable insights into neuropharmacology and therapeutic interventions.
  44. Haloperidol Analogue

    UCSF34 is a Haloperidol analogue that selectively binds to the human D2L receptor, exhibiting an estimated pKi of 7.49. This compound is significant for its potential applications in schizophrenia research, facilitating the investigation of dopamine receptor modulation and related therapeutic strategies.
  45. Dopamine Receptor Antagonist

    Seridopidine is a potent dopamine receptor antagonist that primarily targets D2 and D3 receptors. It exhibits significant antipsychotic activity, making it valuable for research in neurological and psychiatric disorders. This compound is useful in studies investigating the roles of dopamine in the central nervous system, particularly in understanding mechanisms underlying schizophrenia and related conditions.
  46. Dopamine D2 Receptor Agonist

    U 101958 is a potent full agonist of the dopamine D4 receptor, exhibiting a pEC50 of 8.7 in HEK293 cells expressing the D4 receptor. This compound demonstrates significant biological activity and is valuable for research in neuropharmacology, particularly in studies examining the role of dopamine signaling in psychiatric disorders. Its selectivity for the D4 receptor can aid in the exploration of D4-mediated effects in various biological systems.
  47. Dopamine D1 Receptor PAM

    LY3154885 is an orally active positive allosteric modulator (PAM) targeting the dopamine D1 receptor. This compound enhances receptor activity, facilitating increased dopaminergic signaling. Its favorable drug-drug interaction profile makes it a valuable tool for research into dopamine-related pathways and potential therapeutic applications in neuropsychiatric disorders.
  48. Dopamine Receptor

    Quinagolide is a non-ergot dopamine D(2) receptor agonist that enhances dopamine activity. It is primarily utilized in the modulation of endocrine function, particularly in the suppression of hyperprolactinemia and its associated clinical symptoms. Quinagolide's significant biological activity makes it a valuable reagent for research in endocrine disorders and drug development, facilitating the study of dopamine's role in various physiological processes.
  49. D3R Ligand

    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.
  50. D1 Receptor Agonist

    A-77636 is a potent and selective orally active agonist of the dopamine D1 receptor, demonstrating a pEC50 of 8.13 and an EC50 of 1.1 nM. It exhibits a high affinity for the dopamine D1 receptor with a pKi value of 7.40 ± 0.09 (Ki = 39.8 nM). Due to its pharmacological profile, A-77636 is primarily utilized in research related to Parkinson's disease and other dopamine-related disorders.

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