GPCR/G Protein

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  1. Dopamine Receptor Antagonist

    Pericyazine is a selective D2-dopamine receptor antagonist primarily utilized in the management of severe anxiety states and psychosis. This first-generation antipsychotic demonstrates key biological activities, including adrenolytic and anticholinergic effects, as well as potential extrapyramidal symptoms. Research applications of pericyazine extend to neuropharmacology, helping to elucidate the role of dopamine in psychiatric disorders.
  2. Dopamine Receptor Agonist

    PD-168077 maleate is a selective agonist targeting the dopamine D4 receptor, exhibiting a Ki value of 9 nM. This compound demonstrates the ability to activate dopamine signaling pathways, making it a valuable tool for research into neuropharmacology and psychiatric disorders. Its targeted mechanism is essential for studying the roles of dopamine receptor subtypes in various biological contexts.
  3. D2 Receptor Antagonist

    (S)-Remoxipride hydrochloride is a selective antagonist of the dopamine D2 receptor, exhibiting an IC50 value of 1.57 μM. This compound is primarily utilized in research related to psychotic disorders, aiding in the exploration of dopamine receptor pathways and their roles in neuropsychiatric conditions. Its specificity for the D2 receptor positions it as a valuable tool for studying schizophrenia and other related disorders.
  4. Dopamine Receptor Antagonist

    D-Tetrahydropalmatine is an isoquinoline alkaloid that functions as a dopamine receptor antagonist, with a preferential affinity for D1 receptors. This compound exhibits significant inhibitory activity against organic cation transporter 1 (OCT1). D-Tetrahydropalmatine is utilized in research focused on neurological disorders and the modulation of dopamine signaling pathways. Its unique properties make it a valuable tool in the exploration of receptor interactions and pharmacological investigations.
  5. Dopamine D3 Receptor Antagonist

    NGB 2904 is a potent and selective antagonist of the dopamine D3 receptor, demonstrating a Ki value of 1.4 nM. This compound exhibits high selectivity for the D3 receptor compared to other targets, including D2, 5-HT2, and α1 receptors, with Kis ranging from 217 to >10,000 nM. NGB 2904 effectively antagonizes Quinpirole-stimulated mitogenesis, making it a valuable tool for research into dopamine-related pathways and potential therapeutic applications in neuropsychiatric disorders.
  6. D3 Dopamine Receptor Agonist

    ML417 is a selective agonist for the D3 dopamine receptor (D3R), demonstrating an EC50 of 38 nM. This compound effectively stimulates D3R-mediated β-arrestin translocation, facilitates G protein signaling, and induces pERK phosphorylation while exhibiting minimal interference with other GPCR pathways. ML417 also offers neuroprotective effects against toxin-induced neurodegeneration of dopaminergic neurons, making it a valuable tool for studying neurodegenerative diseases and dopamine-related disorders.
  7. DRD2 Antagonist

    Propionylpromazine hydrochloride is a dopamine receptor D2 (DRD2) antagonist. This compound exhibits potential in the modulation of dopaminergic signaling, making it relevant for studies related to Parkinson's disease and other disorders associated with dopamine dysregulation. Its ability to inhibit DRD2 may aid in understanding the physiological and pathological roles of dopamine in various neurological contexts.
  8. Phospholipase D Inhibitor

    Halopemide is a potent inhibitor of phospholipase D (PLD), exhibiting IC50 values of 220 nM for human PLD1 and 310 nM for PLD2. In addition to its enzymatic inhibition, Halopemide functions as a dopamine receptor antagonist and exhibits psychotropic properties. This reagent is valuable for research applications exploring PLD-mediated signaling pathways and dopamine receptor interactions in various biological contexts.
  9. DA Receptor Antagonist

    Butyrophenone is a dopamine receptor (DA Receptor) antagonist that plays a significant role in neuropharmacological studies. This compound is primarily utilized in research focused on mental disorders such as schizophrenia and bipolar disorder. Its ability to modulate dopaminergic signaling makes it valuable for investigating the underlying mechanisms of these conditions and potential therapeutic interventions.
  10. Dopamine Receptor Antagonist

    PG01037 dihydrochloride is a potent and selective antagonist of the dopamine D3 receptor, with a dissociation constant (Ki) of 0.7 nM. This compound is valuable in research applications exploring the role of dopamine signaling in various neurological and psychiatric disorders. Its ability to inhibit D3 receptor activity makes it a pivotal tool for investigating potential therapeutic interventions and understanding dopamine-related pathways.
  11. Dopamine D2 Receptor Antagonist

    Domperidone monomaleate is a selective antagonist of the dopamine D2 receptor. This compound exhibits notable antiemetic and prokinetic properties by influencing the chemoreceptor trigger zone and enhancing gastrointestinal motility. It is primarily utilized in research related to gastrointestinal disorders and neuropharmacology.
  12. Dopamine Receptor Modulator

    Neuromedin N is a potent dopamine D2 receptor modulator that enhances agonist binding in rat neostriatal membranes. This compound plays a significant role in the investigation of dopaminergic signaling pathways and their implications in neurobiology. Neuromedin N's ability to influence dopamine receptor activity makes it valuable for research into neuropsychiatric disorders and related therapeutic strategies.
  13. Antipsychotic Compound

    Lenperone is an antipsychotic compound that primarily targets dopamine receptors. It exhibits notable efficacy in alleviating depressive symptoms associated with psychotic disorders. Research applications include studying its effects on neurotransmitter modulation and exploring its potential in psychiatric treatment protocols.
  14. Dopamine Receptor Antagonist

    Fallypride is a potent antagonist of the dopamine D2 and D3 receptors, providing valuable insights into dopaminergic function. As a radiolabeled compound (Fallypride-18F), it serves as an effective positron emission tomography (PET) radiotracer for studying neurological disorders and neuropharmacology. Its application in imaging facilitates the exploration of dopamine-related mechanisms in various psychiatric and neurodegenerative conditions.
  15. Dopamine Receptor Inhibitor

    Clopenthixol is a thiaquinoline compound that acts as an antagonist of D1 and D2 dopamine receptors. It exhibits inhibitory effects comparable to those of phenothiazine antipsychotics, making it valuable in the treatment of schizophrenia and other mental disorders. This compound is primarily utilized in research related to psychiatric conditions and the exploration of dopamine regulation in the central nervous system.
  16. Dopamine D2 Receptor Antagonist

    Sultopride hydrochloride is a selective antagonist of the dopamine D2 receptor, exerting its primary mechanism of action through blocking dopamine signaling. This compound is chiefly utilized in research investigating the role of dopamine in neuropsychiatric disorders and the pharmacological modulation of dopaminergic pathways. Its ability to selectively inhibit D2 receptor activity makes it a valuable tool for exploring dopamine-related biological processes and the development of therapeutic agents.
  17. Dopamine Receptor Antagonist

    Bromopride is a selective, irreversible antagonist of the dopamine D2 receptor, demonstrating significant utility in pharmacological research. This compound effectively crosses the blood-brain barrier, inhibiting the vomiting center and enhancing gastrointestinal motility, thereby exhibiting both antiemetic and prokinetic properties. Bromopride's ability to block dopamine-mediated vomiting reflexes and stimulate gastrointestinal smooth muscle contraction makes it a valuable reagent for investigating digestive system disorders, particularly gastric hypomotility, nausea, and vomiting, without adversely affecting abdominal wall healing in animal models.
  18. SR-2A/D2DR Inhibitor

    Octoclothepin maleate salt is a dual inhibitor of the SR-2A and D2 dopamine receptors. This compound exhibits significant central depressant activity, demonstrated in various observational and instrumental studies using rodent models. Its properties make it a valuable tool in neuropharmacological research, particularly in the study of neuroleptic effects and dopaminergic signaling pathways.
  19. D4 Receptor Antagonist

    Sonepiprazole is a selective D4 dopamine receptor antagonist, exhibiting Ki values of 3.6 nM for the rat D4 receptor and 10.1 nM for the human D4.2 receptor, while showing weaker affinities of 5147 nM and 7430 nM for the rat D2 dopamine and histamine H1 receptors, respectively. This compound demonstrates potential for modulating dopaminergic signaling and is useful in investigating the role of D4 receptors in neurological and psychiatric conditions. Sonepiprazole may serve as a valuable tool for researchers studying the therapeutic implications of dopamine receptor antagonism.
  20. Antipsychotic Agent

    Haloperidol lactate is a potent antipsychotic agent primarily targeting dopamine receptors. It is commonly utilized in the management of acute and chronic schizophrenia, as well as Gilles de la Tourette's syndrome. Additionally, Haloperidol lactate is valuable for research on psychotic disorders, aiding in the exploration of therapeutic pathways and interventions.
  21. Dopamine Receptor Agonist

    Pergolide is an ergot-derived dopamine receptor agonist that primarily targets D1 and D2 dopamine receptors. This compound demonstrates significant biological activity in modulating dopaminergic signaling, making it a valuable tool in the study of Parkinson's disease and related neurological disorders. Pergolide is commonly utilized in research to explore therapeutic mechanisms and potential treatments for motor function impairments associated with dopaminergic deficiencies.
  22. Stable Isotope

    Amisulpride-d5 is a deuterium-labeled derivative of Amisulpride, a selective antagonist of the dopamine D2 and D3 receptors. It exhibits high affinity with Kis of 2.8 nM and 3.2 nM for human D2 and D3 receptors, respectively. This stable isotope is utilized in pharmacokinetic studies, metabolic research, and tracer studies to investigate the pharmacological properties and dynamics of dopamine receptor interactions.
  23. Dopamine Agonist

    ADTN hydrobromide is a long-acting dopamine agonist that targets dopamine receptors to modulate dopaminergic signaling. It has been shown to significantly decrease the behavioral visual threshold in zebrafish models with dopamine depletion, indicating its potential utility in studying dopamine-related pathways and neuropharmacology. This compound is valuable for research applications exploring dopamine receptor functions and related disorders.
  24. D1R Agonist

    (Rac)-Razpipadon is a selective D1 dopamine receptor agonist, demonstrating potent G protein-biased signaling with an EC50 of 5.8 nM in Gs-cAMP assays. This non-catechol compound is valuable for exploring dopamine D1 receptor pathways and studying related neurobiological processes. Its high efficacy makes it suitable for research applications focused on neuropharmacology and the modulation of dopaminergic signaling.
  25. Dopamine D2 Receptor Modulator

    PAOPA is an allosteric modulator of the dopamine D2 receptor, derived from the analog of L-proline-L-leucine-glycine amide (PLG) peptide. This compound demonstrates significant potential in mitigating behavioral abnormalities in rodent models of schizophrenia. PAOPA enhances the receptor's affinity and promotes its binding to agonists, making it a valuable tool for research focused on neuropsychiatric disorders.
  26. Dopamine Receptor Antagonist

    Dopamine D2 receptor antagonist-1 is a negative allosteric modulator of the dopamine D2 receptor (D2R) that exhibits sub-micromolar affinity. This compound is utilized in research studying dopaminergic signaling pathways and provides insights into neurological disorders associated with D2R dysfunction. Its role in modulating receptor activity makes it a valuable tool for exploring pharmacological interventions in the central nervous system.
  27. Dopamine Receptor

    Quinpirole is a selective agonist of the dopamine D2 and D3 receptors, primarily targeting central nervous system functions. It is known to reduce hypothalamic norepinephrine concentrations, influencing dopaminergic signaling pathways. Quinpirole's unique mechanism results in decreased dopamine metabolites and potential increased levels of 3-methoxy-4-hydroxyphenylglycol (MHPG) sulfate, making it valuable for research on neuropharmacology and the modulation of mood and behavior.
  28. Dopamine D4 Receptor Agonist

    CP 226269 is a potent agonist of the dopamine D4 receptor, demonstrating significant calcium flux induction with an EC50 of 32 nM. This compound also stimulates phospholipid methylation (PLM) in SK-N-MC neuroblastoma cells, exhibiting an EC50 of 2.9 nM. CP 226269 is utilized in research related to schizophrenia and other neuropsychiatric disorders, providing valuable insights into dopamine receptor functions.
  29. Dopamine Receptor Modulator

    OPC 4392 hydrochloride is a modulator of dopamine receptors, acting as an agonist at presynaptic receptors while antagonizing postsynaptic D2 receptors. This compound has demonstrated the ability to reverse dopamine accumulation induced by Reserpine and inhibit stereotypic and climbing behaviors triggered by Apomorphine in mouse models. It serves as a valuable tool for investigating dopamine-related pathways and behaviors in neurological research.
  30. D1-like Dopamine Receptor PAM

    MLS1082 is a pyrimidone-derived positive allosteric modulator targeting the D1-like dopamine receptors. It exhibits an EC50 of 123 nM for enhancing dopamine-stimulated G protein signaling. This compound is valuable for research applications focused on dopamine receptor pharmacology and the modulation of neurotransmitter systems.
  31. Dopamine Receptor Antagonist

    Odapipam (NNC 756) is a selective dopamine D1 receptor antagonist, exhibiting high affinity with a Kd of 0.18 nM. This compound serves as a valuable tool in neuroscience research, particularly for studying dopaminergic signaling pathways and related neuropsychiatric disorders. In addition, Odapipam functions as an effective radiotracer for positron emission tomography (PET) imaging, enhancing the investigation of receptor dynamics in vivo.
  32. Dopamine Autoreceptor Agonist

    Preclamol hydrochloride is a selective dopamine autoreceptor agonist, primarily targeting the D2 dopamine receptor. This compound exhibits significant biological activity in modulating dopamine signaling, making it a valuable tool for investigating the pathophysiology of schizophrenia. Its applications extend to neuropharmacology studies, aiding in the development of therapeutic strategies for dopaminergic dysregulation.
  33. D3 Receptor Antagonist

    YQA14 is a high-affinity antagonist of the dopamine D3 receptor. It exhibits significant anti-opioid addiction activity, demonstrating the ability to inhibit morphine- and cocaine-induced conditioned place preference (CPP) in preclinical models. This compound is valuable for research into the mechanisms of addiction and the development of therapeutic strategies for substance use disorders.
  34. Dopamine Receptor Inhibitor

    7-Hydroxy-DPAT hydrobromide is a selective agonist for the D3 dopamine receptor, primarily impacting dopamine signaling pathways. This compound demonstrates significant biological activity in modulating locomotor behavior and influencing dopamine metabolism within the central nervous system. It serves as a valuable tool for research applications related to neuropharmacology and the study of dopamine-related disorders.
  35. Dopamine Receptor Agonist

    Talipexole is a selective dopamine receptor agonist primarily targeting D2-like receptors. It is proposed for use as an antiparkinsonian agent, demonstrating potential in improving motor function in Parkinson's disease models. Research applications include studying dopaminergic signaling pathways and exploring therapeutic options for neurodegenerative disorders.
  36. D3 Receptor Antagonist

    Mesdopetam hemitartrate is a selective antagonist of the dopamine D3 receptor, exhibiting a Ki value of 90 nM and an IC50 of 9.8 μM for human recombinant D3 receptors. This compound demonstrates psychomotor stabilizing effects, making it a valuable tool in the investigation of motor and psychiatric complications associated with Parkinson's disease. Its unique properties contribute to research aimed at understanding the underlying mechanisms of dopamine-related disorders.
  37. Dopamine D3 Receptor Antagonist

    Mesdopetam is a selective antagonist of the dopamine D3 receptor, displaying a Ki value of 90 nM and an IC50 of 9.8 μM for the human recombinant D3 receptor. This compound exhibits psychomotor stabilizing properties and is utilized in research focused on motor and psychiatric complications associated with Parkinson's disease. Its role in modulating dopamine signaling makes it valuable for studying therapeutic strategies in this context.
  38. DRD4 Antagonist

    PD 168568 dihydrochloride is a potent and orally active antagonist of the dopamine receptor D4 (DRD4). This compound exhibits selectivity for the D4 receptor, with Ki values of 8.8 nM for DRD4 compared to 1842 nM for DRD2 and 2682 nM for DRD3. PD 168568 dihydrochloride is applicable in glioblastoma (GBM) research, making it a valuable tool for investigating the role of DRD4 in cancer biology and potential therapeutic strategies.
  39. Dopamine

    AJ-76 hydrochloride is a potent antagonist of dopamine autoreceptors, exhibiting pKi values of 6.95, 6.67, 6.37, 6.21, and 6.07 for human D3, D4, D2 short, D2 long, and rat D2 receptors, respectively. This compound is valuable for research focused on dopamine receptor modulation and its implications in neurological disorders. Its specific receptor affinity allows for investigations into the roles of dopamine signaling in various physiological and pathological processes.
  40. Dopamine Receptor Inhibitor

    GBR 12783 is a selective dopamine uptake inhibitor that targets dopamine receptors with high potency. It effectively inhibits [3H]dopamine uptake in striatal synaptosomes from rats and mice, exhibiting IC50 values of 1.8 nM and 1.2 nM, respectively. This compound has been shown to enhance memory performance and increase hippocampal acetylcholine release in rodent models, making it valuable for research in neuropharmacology and cognitive function studies.
  41. Dopamine Receptor Antagonist

    Zuclopenthixol dihydrochloride is a thioxanthene derivative that functions as a mixed antagonist of dopamine D1 and D2 receptors. This compound is primarily utilized in schizophrenia research, aiding in the investigation of neurochemical pathways associated with the disorder. Its ability to modulate dopaminergic signaling makes it a valuable tool for studying the efficacy of antipsychotic therapies.
  42. Dopamine D3 Receptor Antagonist

    (-)-GSK598809 hydrochloride is a potent and selective antagonist of the dopamine D3 receptor (DRD3). It exhibits high affinity for DRD3, making it a valuable tool for studying dopamine-related pathways and their implications in neuropsychiatric disorders. This compound is suitable for research applications focused on drug development, behavioral studies, and understanding the role of dopamine in various physiological processes.
  43. Dopamine Receptor Antagonist

    RG-15 is a potent oral antagonist of the dopamine receptors, specifically targeting the human D2 and D3 receptors with pKi values of 8.23 and 10.49, respectively. It effectively inhibits dopamine-stimulated [35S]GTPγS binding, demonstrating an IC50 of 21.2 nM in rat striatal membranes, 36.7 nM in mouse A9 cells expressing human D2L receptors, and 7.2 nM in CHO cells expressing human D3 receptors. RG-15 also enhances dopamine turnover and biosynthesis in the mouse striatum and olfactory bulb, indicating potential antipsychotic properties. This compound is valuable for research into dopamine-related disorders and therapeutics.
  44. Dopamine D3 Receptor Antagonist

    Nafadotride is a selective antagonist of the dopamine D3 receptor. By inhibiting dopamine D3 receptor activity, Nafadotride modulates dopamine signaling pathways that are critical for regulating emotion, motivation, reward, and motor functions. This compound is suitable for research into the role of dopamine D3 receptors in neuropsychiatric disorders and behavior-related studies, providing insights into potential therapeutic targets.
  45. Dopamine D3/D2 Receptor Agonist

    Quinelorane dihydrochloride is a potent agonist of the dopamine D3 and D2 receptors, facilitating modulation of dopaminergic signaling pathways. This compound shows promise in the investigation of neurological and psychiatric disorders, offering valuable insights into the mechanistic underpinnings of related conditions. Research applications may include studies on dopamine receptor function, neuropharmacology, and potential therapeutic interventions.
  46. D3 Receptor Antagonist

    U-99194 maleate is a potent and selective antagonist of the dopamine D3 receptor, exhibiting a Ki value of 160 nM. This compound effectively inhibits both endogenously released dopamine and exogenous D3 agonist activation of the D3 receptor. In rat hippocampal slices, U-99194 maleate reverses the IPSC-suppressive effect induced by the D3 agonist PD 128907. Additionally, it demonstrates significant suppression of nicotine-induced tremors in mouse models, making it a valuable tool for investigating dopamine D3 receptor-mediated motor disorders, particularly in the context of kinetic tremors.
  47. Dopamine Receptor Blocker

    Dicarbine dihydrochloride is a dopamine receptor antagonist that modulates neurotransmission within multiple regions of the brain. By blocking dopamine receptors, it effectively mitigates the suppression of conditioned defense reflexes induced by stimulation of the mesencephalic reticular formation. This compound serves as a valuable tool in research addressing schizophrenia and alcoholic psychosis, facilitating insights into dopamine-related pathophysiology and therapeutic interventions.
  48. Dopamine Receptor Inhibitor

    Cyclo(glycyl-L-leucyl) is a neuropeptide that specifically inhibits dopamine receptors, playing a crucial role in modulating dopaminergic signaling. This compound has been shown to down-regulate dopamine receptor activity and reduce dopaminergic supersensitivity, particularly in the context of morphine-induced analgesia in animal models. Cyclo(glycyl-L-leucyl) holds promise for potential therapeutic applications in preventing tardive dyskinesias and L-DOPA-induced dyskinesias, making it valuable for research in neuropharmacology and movement disorders.
  49. D2 Receptor Agonist

    Carmoxirole hydrochloride is a selective agonist of the dopamine D2 receptor, demonstrating significant peripheral activity. It is primarily used in research related to antihypertensive mechanisms and cardiovascular physiology. This compound is valuable for studies exploring dopamine receptor signaling and its implications in blood pressure regulation.
  50. D2 Receptor Antagonist

    Alizapride is a selective antagonist of the D2 dopamine receptor, primarily used for its potent antiemetic properties. It exhibits effectiveness in managing nausea and vomiting, and is also applicable in the treatment of various human digestive disorders. Research involving Alizapride contributes to the understanding of dopamine's role in gastrointestinal function and the development of therapeutic strategies for related conditions.

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