GPCR/G Protein

Items 3101-3150 of 6966

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  1. Dopamine Receptor Ligand

    (-)-Isocorypalmine is a potent ligand for dopamine receptors, specifically isolated from the crude base fraction of Corydalis chaerophylla. This compound demonstrates high affinity, with a Km value of 4.63 ± 0.71 μM, as confirmed by recombinant CYP719A21. It holds significant promise for research in neuropharmacology and studies related to dopamine signaling pathways.
  2. Dopamine Receptor Antagonist

    Moperone is a potent antagonist of D2 and D3 dopamine receptors, with IC50 values of 1.0 nM for both targets. This compound exhibits significant biological activity in the modulation of dopaminergic signaling pathways, making it a valuable tool for research into psychiatric disorders and neurological conditions. Moperone is particularly useful in studies examining the role of dopamine receptors in behavior and cognition.
  3. Psychoactive Substance

    MFZ 2-13 is an N-demethylated intermediate and N-nor-analogue of MFD 2-12 that targets the human dopamine receptor. It functions as an inhibitor of dopamine uptake, exhibiting an IC50 of 1.4 nM. This compound is valuable for research in neuropharmacology and the study of psychoactive substances.
  4. Dopamine Receptor Antagonist

    A-437203 is a selective antagonist for the dopamine D3 receptor, exhibiting Ki values of 71 nM for D2, 1.6 nM for D3, and 6220 nM for D4 receptors. This compound is valuable for research into dopamine-related pathways and offers potential applications in studying neuropsychiatric disorders. Its specificity for the D3 receptor makes it a useful tool for exploring the role of this receptor in various biological processes and assessing new therapeutic strategies.
  5. Dopamine D2 Receptor Agonist

    Aplindore is a potent dopamine D2 receptor agonist, exhibiting a pKi value of 9.1. This compound is significant in the study of Parkinson's disease, as it aids in elucidating dopaminergic signaling pathways. Its activity provides valuable insights into therapeutic strategies for managing symptoms associated with dopaminergic deficits.
  6. Dopamine Receptor Agonist

    Matsupexolum is a dopamine receptor agonist that selectively activates dopamine receptors, facilitating neurotransmission. This compound demonstrates significant biological activity in modulating dopaminergic signaling pathways and can be utilized in research focused on neuropharmacology, psychiatry, and the study of movement disorders. Its application may provide insights into the therapeutic potential for conditions such as schizophrenia and Parkinson's disease.
  7. Dopamine Receptor Modulator

    Glovadalenum is a positive allosteric modulator of the dopamine D1 receptor. This compound enhances dopamine receptor signaling, making it valuable for research in neuropharmacology and neurodegenerative diseases. Its modulation of dopaminergic pathways offers potential insights into the treatment of conditions such as schizophrenia and Parkinson's disease.
  8. Stable Isotope

    Propionylpromazine-d6 hydrochloride is a deuterium-labeled derivative of Propionylpromazine hydrochloride, a potent dopamine receptor D2 (DRD2) antagonist. This reagent is primarily utilized in pharmacological research focusing on Parkinson's disease, enabling the study of dopamine signaling pathways and receptor interactions. The stable isotope labeling provides enhanced analytical precision, making it suitable for advanced bioanalytical applications.
  9. Dopamine D2/D3 Receptor Antagonist

    Trazpiroben is a selective antagonist of the dopamine D2 and D3 receptors, primarily utilized for investigating the pathophysiology and treatment of moderate-to-severe gastroparesis. Its inhibition of these receptors plays a significant role in regulating gastrointestinal motility. Trazpiroben is a valuable tool for researchers exploring the therapeutic potential and underlying mechanisms of dopamine-related gastrointestinal disorders.
  10. Dopamine Receptor Inhibitor

    Fosopamine hydrochloride is a dopamine receptor D agonist, primarily targeting the dopamine receptor pathways. It has demonstrated significant utility in research related to hypertension, aiding in the exploration of cardiovascular mechanisms and blood pressure regulation. This compound may provide insights into both the physiological and pathological roles of dopamine signaling in hypertension-related studies.
  11. Dopamine Agonist

    PD 120697 is an orally active dopamine agonist that primarily targets dopamine receptors. It exhibits significant inhibition of striatal dopamine synthesis and reduces dopaminergic neuronal firing, leading to decreased spontaneous locomotor activity. PD 120697 also effectively reverses depression induced by Reserpine, making it a valuable tool for studying dopamine-related disorders and potential therapeutic interventions.
  12. D2 Receptor Antagonist

    Eticlopride is a selective antagonist of the dopamine D2 receptor, demonstrating a high binding affinity for dopamine D2 as well as for α1-adrenergic, α2-adrenergic, 5HT1, and 5HT2 receptors, with Kis of 0.09, 112, 699, 6220, and 830 nM, respectively. This compound is primarily utilized in research related to antipsychotic drug development and elucidation of dopamine's role in neuropsychiatric disorders. Its pharmacological profile supports investigations into dopamine receptor modulation and its implications in various neurological conditions.
  13. D3 Receptor Ligand

    Dopamine D3 receptor ligand-3 is a selective ligand for the D3 receptor, exhibiting a high affinity with a Ki value of 3.6 nM. This compound demonstrates significant selectivity for the D3 receptor over the D2 receptor, with a Ki of 353 nM. It serves as a valuable tool for research applications focusing on dopaminergic signaling and related neurological disorders.
  14. Dopamine Receptor Inhibitor

    PD 128907 is a selective dopamine D3 receptor inhibitor that effectively modulates dopaminergic signaling. The active (+) enantiomer exhibits high affinity for rat D3 receptors and demonstrates significant inhibitory effects on neuronal firing in the ventral tegmental area and substantia nigra pars compacta, with EC50 values of 33 nM and 38 nM, respectively. Additionally, it inhibits dopamine release in the caudate putamen with an EC50 of 66 nM. While PD 128907 primarily targets D3 receptors, evidence suggests its actions may also involve D2 autoreceptors, making it a valuable tool for exploring dopamine receptor pharmacology and neurobehavioral research.
  15. D2 Agonist

    Naxagolide hydrochloride is a selective agonist of the dopamine D2 receptor. This compound exhibits significant dopaminergic activity, making it valuable in research focused on Parkinsonism and related movement disorders. It serves as a potential therapeutic agent for understanding the modulation of dopaminergic signaling in neurological studies.
  16. Dopamine Agonist

    CGS 15873A is an orally active benzopyranopyridine derivative that functions as a selective dopamine agonist. This compound activates dopamine receptors, making it valuable for studying the physiological and pharmacological roles of dopamine in the central nervous system. CGS 15873A is particularly relevant in research related to neurological disorders such as schizophrenia and Parkinson's disease.
  17. D3 Receptor Antagonist

    FAUC 365 is a highly selective antagonist for the dopamine D3 receptor, exhibiting a Ki value of 0.5 nM. It demonstrates significantly lower binding affinities at D4.4, D2short, and D2Long receptors, with Ki values of 340 nM, 2600 nM, and 3600 nM, respectively. FAUC 365 is primarily utilized in research related to schizophrenia and Parkinson's disease, providing valuable insights into dopamine receptor interactions and potential therapeutic interventions.
  18. Dopamine D3 Receptor Agonist

    SK609 hydrochloride is a selective agonist of the dopamine D3 receptor, exhibiting an EC50 of 1109 nM. This compound demonstrates significant biological activity in modulating dopamine signaling pathways, making it a valuable tool in Parkinson's disease research. Its unique properties facilitate the exploration of D3R-related mechanisms, contributing to the understanding of dopaminergic dysfunction in neurodegenerative disorders.
  19. Dopamine Receptor Modulator

    Raxlaprazine etomoxil is a small molecule compound that functions as a dopamine D2 and D3 receptor modulator. This compound shows high affinity for human recombinant D2L receptors, with an inhibition constant (Ki) of 1.95 nM, and effectively inhibits forskolin-stimulated cAMP accumulation with a half maximal effective concentration (EC50) of 3.72 nM. Raxlaprazine etomoxil is valuable for research focused on mental illnesses and neurological disorders.
  20. Dopamine D3 receptor ligand

    Dopamine D3 receptor ligand-1 is a potent and selective ligand for the dopamine D3 receptor, exhibiting a high affinity with a Ki value of 8 nM. This compound demonstrates an impressive 89-fold selectivity for the D3 receptor over the D2 receptor (D2 Ki = 715 nM). Its specificity makes it a valuable tool for investigating the D3 receptor's role in various neurobiological processes and for drug discovery efforts targeting dopamine-related disorders.
  21. Dopamine Receptor Inhibitor

    ADTN is a dopamine receptor inhibitor that modulates dopamine neurotransmission. It demonstrates the ability to reduce dopamine-related signaling, which may help target conditions associated with excessive dopamine activity. ADTN is applicable in research focused on mental health disorders and cognitive function modulation, providing insights into therapeutic strategies for related pathologies.
  22. Dopamine D2/D3 Agonist

    D-520 is a potent dopamine D2/D3 receptor agonist, demonstrating an EC50 of 4.73 nM and 2.18 nM for D2 and D3 receptors, respectively. This compound exhibits significant inhibitory effects on the formation of amyloid-beta (Aβ) aggregates and facilitates the disaggregation of both alpha-synuclein and Aβ aggregates in vitro. D-520 shows promising efficacy in animal models of Parkinson's disease, making it a valuable tool for research in Parkinson's disease and dementia associated with Parkinson’s disease.
  23. Stable Isotope

    Pramipexole-d5 is a deuterium-labeled derivative of Pramipexole, a selective dopamine D2-type receptor agonist that effectively crosses the blood-brain barrier. With binding affinities (Kis) of 2.2 nM, 3.9 nM, 0.5 nM, and 1.3 nM for the D2-type, D2, D3, and D4 receptors respectively, Pramipexole-d5 serves as a valuable tool for exploring dopamine receptor interactions. This compound is particularly relevant for research into neurodegenerative disorders such as Parkinson's disease and conditions like restless legs syndrome.
  24. Dopamine Receptor Inhibitor

    Metoclopramide dihydrochloride is a dopamine D2 receptor antagonist primarily used for its antiemetic effects. It demonstrates notable activity in managing nausea and vomiting, particularly in patients undergoing chemotherapy or surgery. This compound is also employed in research settings to explore the modulation of dopaminergic pathways and gastrointestinal motility.
  25. Dopamine Receptor Agonist

    PF2562 is a selective agonist of the dopamine D1 receptor, demonstrating a binding affinity with a Ki of 113 nM. It effectively stimulates cAMP production in human D1 receptor assays, exhibiting an EC50 value of 568 nM in HTRF assays. This compound is valuable for research applications involving dopamine receptor signaling and related neurological studies.
  26. Dopamine Receptor

    SK609 is a selective agonist of the dopamine D3 receptor, enhancing dopamine and norepinephrine levels in the cerebral cortex. This compound has demonstrated efficacy in suppressing dyskinesias in preclinical models of Parkinson's disease and alleviating muscle twitches caused by L-dopa treatment. Additionally, SK609 has been shown to improve performance in sustained attention tasks by significantly reducing both misses and false alarms. Research indicates that SK609 may offer therapeutic potential for mitigating movement and cognitive deficits associated with Parkinson's disease.
  27. Dopamine D2 Ligand

    UNC0006 is a β-arrestin-biased ligand targeting the dopamine D2 receptor. This compound is primarily utilized in the investigation of antipsychotic mechanisms and their effects on dopamine signaling pathways. Its unique bias towards β-arrestin pathways may offer new insights into therapeutic strategies for psychiatric disorders.
  28. D2 Receptor Antagonist

    Y-20024 hydrochloride is a selective D2 receptor antagonist known for its ability to cross the blood-brain barrier. It effectively inhibits Apomorphine-induced symptoms associated with attention deficit hyperactivity disorder (ADHD) in murine models and also mitigates Apomorphine-induced vomiting in canine subjects. This compound demonstrates prolactin-promoting activity and is valuable for research into neurological disorders such as ADHD and emesis.
  29. Dopamine Antagonist

    Neflumozide is a potent dopamine antagonist classified as a benzisoxazole derivative. It exhibits significant antipsychotic activity, making it a valuable tool for investigating psychosis and related conditions. This compound is useful in preclinical research aimed at understanding dopamine receptor modulation and its implications in psychiatric disorders.
  30. Dopamine D2 Receptor Antagonist

    Tropapride is a selective antagonist of the dopamine D2 receptor. It exhibits significant biological activity by modulating dopaminergic signaling, making it a valuable tool for investigating neurological disorders. This compound is commonly utilized in research focused on conditions such as schizophrenia, Parkinson's disease, and other related neurological dysfunctions.
  31. Dopamine Receptor Inhibitor

    Bulbocapnine hydrochloride is a potent dopamine receptor inhibitor that plays a significant role in modulating dopaminergic activity. This aporphine alkaloid is known to inhibit dopamine synthesis and exhibits neuroleptic-like properties, alongside anticonvulsant and antinociceptive effects. Its pharmacological profile makes it a valuable tool in research related to neurological disorders and the exploration of dopamine-related pathways.
  32. Dopamine D3 Receptor Agonist

    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.
  33. Dopamine Receptor

    3'-Fluorobenzylspiperone maleate is a selective ligand for dopamine D2 receptors, demonstrating significant potential in the modulation of dopaminergic activity. This compound has been shown to exhibit improved efficacy in alleviating behavioral disorders compared to placebo, making it a valuable tool for research into neuropsychiatric conditions and the pharmacological study of dopamine pathways. Its targeted action underscores its relevance in the investigation of dopamine-mediated therapeutic interventions.
  34. Dopamine D2/D5 Receptor Antagonist

    Molindone is a potent antagonist of dopamine D2 and D5 receptors, classified as an indole derivative. This compound exhibits significant biological activity in modulating dopaminergic neurotransmission and is primarily used in the research of schizophrenia and severe mental illnesses. Its mechanism of action makes it a valuable tool for studying dopaminergic pathways and their implications in psychiatric disorders.
  35. D2 Receptor Blocker

    Trimethobenzamide is a D2 receptor blocker that serves as an effective antiemetic. It is primarily used to prevent nausea and vomiting, making it valuable in various clinical settings. This compound can be utilized in research applications focused on gastrointestinal motility and central nervous system interactions.
  36. Dopamine D2-receptor Agonist

    5-OH-DPAT (5-Hydroxy-DPAT) is a potent and selective agonist of the dopamine D2 receptor, with minimal activity at 5-HT receptors. This compound is known to enhance male rat sexual behavior, providing insights into the role of dopamine in sexual function. As a valuable tool in neuropharmacology research, 5-OH-DPAT can be utilized to study dopamine receptor signaling and its implications in various behavioral models.
  37. D1-Dopamine Receptor Antagonist.

    Trepipam is a D1-dopamine receptor antagonist, primarily utilized for its neuroprotective properties. It has demonstrated efficacy in reducing self-injurious behavior in 6-OHDA-lesioned rats, making it a valuable tool in behavioral neuroscience studies. Trepipam has potential applications in researching conditions such as epilepsy and anxiety disorders, facilitating insights into dopaminergic signaling pathways.
  38. D1R/D2R Ligand

    (-)-MDO-NPA is a dual-target ligand for dopamine receptors D1R and D2R, functioning as an N-propylnorapomorphine analog. It demonstrates β-arrestin EC50 values of 1949 nM for D1R and 520 nM for D2R, and cAMP EC50 values of 717.5 nM for D1R and 7.7 nM for D2R. This compound is particularly valuable for studying dopamine-related disorders, including Parkinson's disease, and contributes to understanding receptor signaling pathways in pharmacological research.
  39. D2 Receptor Antagonist

    Tiapride is a selective antagonist of the D2 and D3 dopamine receptors, exhibiting IC50 values of 110-320 nM and 180 nM, respectively. This compound demonstrates anti-dyskinetic and anxiolytic properties, making it valuable in neurological research. Tiapride is classified as a neuroleptic agent and is utilized in studies related to movement disorders and anxiety-related conditions.
  40. SKF-77434 Enantiomer

    (S)-SKF-77434 is a selective enantiomer targeting the dopamine D1 receptor, exhibiting an IC50 value of 2800 nM. This compound is utilized in research focused on neuropsychiatric disorders, providing insights into dopamine receptor modulation. Its affinity for the D1 receptor makes it a valuable tool for exploring the mechanisms underlying cognitive and behavioral functions.
  41. D3R/MOR Antagonist

    D3R/MOR antagonist 2 targets the dopamine D3 receptor (D3R) and the mu-opioid receptor (MOR) as a dual antagonist. With affinities of Ki 361 nM for D3R and 85.2 nM for MOR, this compound exhibits potential analgesic effects through MOR partial agonism while simultaneously mitigating opioid misuse liability via D3R antagonism. It serves as a valuable tool for research in pain management and addiction pharmacology.
  42. D2R Antagonist

    SV 156 is a highly selective antagonist of the D2 dopamine receptor, exhibiting a Ki value of 2.5 nM for human D2 receptors. With approximately 40-fold selectivity for the D2 receptor over the D3 subtype, SV 156 is primarily utilized in research related to L-DOPA-associated abnormal involuntary movements (AIMs). This compound serves as a valuable tool for investigating the mechanisms underlying dopaminergic signaling and movement disorders.
  43. Dopamine D3 Receptor Antagonist

    (±)-BAK2-66 is a potent dopamine D3 receptor antagonist, exhibiting Ki values of 1 nM for the D3 receptor and 960 nM for the D2 receptor. This compound is valuable for research applications focused on modulating dopaminergic signaling and exploring mechanisms underlying addiction in animal models. Its selectivity makes it an important tool for studying the role of the D3 receptor in various neurological conditions.
  44. D2 Receptor Antagonist

    (S)-Remoxipride is a selective antagonist of the dopamine D2 receptor, exhibiting an IC50 value of 1.57 μM. This compound is primarily utilized in research pertaining to psychotic disorders, offering insights into dopaminergic signaling and its implications in various neuropsychiatric conditions. Its specificity for the D2 receptor makes it a valuable tool for studying the effects of dopamine modulation in both in vitro and in vivo settings.
  45. D3 Partial Agonist

    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.
  46. Dopamine Receptor Inhibitor

    Valbenazine dihydrochloride is a selective inhibitor of the vesicular monoamine transporter 2 (VMAT2) and primarily targets dopamine receptors. It is utilized in the treatment of tardive dyskinesia, offering therapeutic benefits for alleviating movement disorder symptoms linked to chronic dopamine receptor antagonism. Extensive preclinical studies support its efficacy, particularly in relation to the genetic factors contributing to tardive dyskinesia.
  47. D3 Antagonist

    AVE-5997 is a selective D3 dopamine receptor antagonist. It effectively reduces hyperactivity induced by MK-801, making it a valuable tool for studying dopaminergic dysregulation. This compound is particularly relevant in the research of schizophrenia and related neuropsychiatric disorders.
  48. D2 Receptor Antagonist

    N-Methylspiroperidol is a potent D2 receptor antagonist that plays a critical role in neuropharmacological research. It can be utilized in PET (Positron Emission Tomography) imaging studies, allowing for the investigation of binding dynamics to the 5-HT2C receptor. This compound is particularly valuable for assessing neurotransmitter interactions, including the competitive effects of dopamine, thereby enhancing our understanding of neuropsychiatric disorders.
  49. Dopamine D1/D2 Receptor Inhibitor

    (Z)-Flupenthixol decanoate is a potent antagonist of dopamine D1 and D2 receptors, functioning primarily to inhibit dopaminergic signaling. This compound exhibits significant antipsychotic activity, making it valuable in the study of psychiatric disorders and neuropharmacology. Research applications include investigations into the modulation of dopaminergic pathways and the evaluation of therapeutic strategies for schizophrenia and related conditions.
  50. Dopamine Receptor Antagonists

    SCH-23390 is a potent antagonist of dopamine D1-like receptors, exhibiting Ki values of 0.2 nM for the D1 subtype and 0.3 nM for the D5 subtype. This compound plays a significant role in behavioral research by shortening the latency period for cocaine-induced lever pressing in rat models. Additionally, SCH-23390 has been shown to eliminate generalized seizures induced by chemical convulsants, making it valuable in the study of neurological disorders associated with the dopamine system.

Items 3101-3150 of 6966

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