GPCR/G Protein

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  1. CXCR

    CX4338 is a selective inhibitor of the chemokine receptor CXCR2, targeting CXCL8-mediated pathways. This compound effectively inhibits CXCR2-mediated cell migration by suppressing β-arrestin-2 recruitment and receptor internalization while enhancing MAPK activation. CX4338 demonstrates potent inhibition of CXCL8-induced chemotaxis in CXCR2-overexpressing cells and human neutrophils. In vivo studies have shown that CX4338 significantly reduces LPS-induced neutrophil infiltration in mouse bronchoalveolar lavage fluid, highlighting its potential for research in inflammatory and immune responses.
  2. CXCR4 Inhibitor

    TN14003 is a selective inhibitor of the CXCR4 receptor. It demonstrates significant antitumor activity by disrupting CXCR4-mediated signaling pathways, which are implicated in cancer cell survival, proliferation, and metastasis. This compound is primarily utilized in research focused on cancer treatment and understanding the role of the CXCR4 chemokine receptor in tumor progression.
  3. CXCR4 Antagonist

    CXCR4 antagonist 6 is a potent inhibitor of the CXCR4 receptor, displaying an IC50 value of 79 nM. This compound effectively inhibits CXCL12-induced cytosolic calcium flux with an IC50 of 0.25 nM, thereby significantly reducing CXCL12/CXCR4-mediated cell migration. Additionally, CXCR4 antagonist 6 demonstrates substantial efficacy in in vivo cancer metastasis models, making it a valuable tool for research in cancer biology and therapeutic development.
  4. CXCR Antagonist

    CXCR4 Antagonist 2 is a potent antagonist of the CXCR4 receptor, exhibiting an IC50 value of 47 nM. This compound effectively inhibits CXCR4-mediated signaling, making it a valuable tool for studying its role in various biological processes, including cancer metastasis, immune cell trafficking, and HIV infection. Its selective properties make it suitable for research applications aimed at understanding CXCR4 functions and developing therapeutic strategies targeting this receptor.
  5. CXCR4 Antagonist

    KRH-1636 is a potent CXCR4 antagonist, primarily targeting the CXCR4 receptor. This compound plays a significant role in HIV-1 research by inhibiting the interaction between the virus and the CXCR4 receptor, which is crucial for viral entry into host cells. KRH-1636 serves as a valuable tool for studying the mechanisms of HIV-1 infection and for exploring therapeutic strategies aimed at disrupting CXCR4-mediated pathways.
  6. Dopamine Receptor Antagonist

    (S)-SCH-23390 hydrochloride is a potent dopamine D1-like receptor antagonist, specifically targeting the D1 and D5 receptor subtypes with Ki values of 0.2 nM and 0.3 nM, respectively. This compound is widely utilized in neuropharmacology research to elucidate the role of dopamine signaling in various physiological and pathological processes. Its application in investigating dopaminergic dysfunction makes it valuable for studies related to neurological disorders and therapeutic interventions.
  7. D2/D3R Agonist

    Quinpirole hydrochloride functions as a high-affinity agonist for the dopamine D2 and D3 receptors. This compound is primarily utilized in research applications focused on neuropharmacology and the exploration of dopaminergic signaling pathways. Quinpirole hydrochloride serves as an important tool for studying the effects of dopamine receptor activation in various in vitro and in vivo models.
  8. Dopamine Receptor Agonist

    Pramipexole is a selective dopamine D2-type receptor agonist that effectively penetrates the blood-brain barrier. It exhibits high affinity with Kis of 2.2 nM for the D2-type receptor, 3.9 nM for D2, 0.5 nM for D3, and 1.3 nM for D4 receptors. This compound is utilized in research related to Parkinson's disease and restless legs syndrome, supporting studies aimed at understanding and treating these neurological disorders.
  9. D2 Receptor Antagonist

    Eticlopride hydrochloride is a selective antagonist of the dopamine D2 receptor, demonstrating high binding affinity for D2, α1-adrenergic, α2-adrenergic, and various serotonin receptors. This compound has KIs of 0.09 nM for D2, 112 nM for α1, 699 nM for α2, 6220 nM for 5HT1, and 830 nM for 5HT2. Eticlopride hydrochloride is primarily utilized in research related to antipsychotic mechanisms and dopamine signaling pathways.
  10. D1/D5 Dopamine Receptor Agonist

    Dihydrexidine hydrochloride is a potent and selective agonist of the D1-like dopamine receptors (D1/D5), exhibiting an IC50 of 10 nM for the D1 receptor. This compound demonstrates significant antiparkinsonian activity, making it valuable in neurological research. Additionally, Dihydrexidine hydrochloride has been shown to stimulate YAP phosphorylation, indicating its potential role in cellular signaling studies.
  11. Dopamine D2 Receptors Agonist

    Lisuride is an orally active agonist of the dopamine D2 receptor, primarily utilized in neurological research. This ergot derivative is valuable for investigating conditions such as Parkinson's disease, migraine disorders, and hyperprolactinemia. Its ability to modulate dopamine activity makes Lisuride a significant compound for studying dopaminergic pathways and associated therapeutic strategies.
  12. Na+/Ca2+ Channel Blocker

    Flunarizine is a potent dual blocker of Na+ and Ca2+ channels, specifically targeting T-type channels. It acts as a D2 dopamine receptor antagonist, exhibiting notable anticonvulsive and antimigraine properties. Additionally, flunarizine demonstrates peripheral vasodilatory effects, making it useful in research related to neurological disorders and vascular function.
  13. Antipsychotic Drug

    Piperacetazine is a phenothiazine antipsychotic that primarily functions as a dopamine receptor antagonist. It has demonstrated inhibitory effects on the transcriptional activity of the PAX3::FOXO1 fusion protein, along with antitumor activity, exhibiting an IC50 of 7.627 μM against PANC-1 cells. This compound is applicable in research related to schizophrenia, pancreatic cancer, and other tumor types, making it a valuable tool for studying both neuropsychiatric disorders and cancer biology.
  14. Dopamine Receptor Antagonist

    Tetrahydroberberine is a potent dopamine D2 receptor antagonist, which modulates dopaminergic signaling pathways. Its biological activity includes potential gastrointestinal benefits, such as enhancing gastric function and alleviating gastric pressure. This compound is of interest in research applications focused on neuropharmacology and gastrointestinal physiology.
  15. Drd2 Agonist

    UNC9995 is a β-arrestin2-biased agonist of the dopamine receptor Drd2. This compound inhibits NLRP3 inflammasome activation by promoting the interaction between β-arrestin2 and NLRP3, thereby preventing neuronal degeneration. Furthermore, UNC9995 activates Drd2/β-arrestin2 signaling, which mitigates the transcription of inflammation-related genes induced by the JAK/STAT3 pathway. Research shows that UNC9995 enhances depressive behavior in mouse models and improves astrocyte dysfunctions, making it a valuable tool for studying neuroinflammatory processes and mood disorders.
  16. Dopamine D2 Receptor Agonist

    MLS1547 is a potent G protein-biased agonist of the dopamine D2 receptor (D2R) with a Ki value of 1.2 μM. It effectively stimulates G protein-mediated signaling pathways, exhibiting an EC50 of 0.37 μM in calcium mobilization assays. Additionally, MLS1547 functions as an antagonist for dopamine-stimulated β-arrestin recruitment to the D2R, demonstrating an IC50 of 9.9 μM. This compound is valuable for investigating D2R signaling mechanisms and exploring therapeutic strategies for disorders associated with dopamine dysregulation.
  17. Dopamine Receptor Antagonist

    Zuclopenthixol is a thioxanthene derivative that functions as a mixed antagonist of dopamine D1 and D2 receptors. This compound has demonstrated antipsychotic properties and is primarily utilized in research related to neuropharmacology and the treatment of schizophrenia. Its ability to modulate dopaminergic signaling makes it a valuable tool for studying dopamine-related disorders and therapeutic interventions.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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.
  23. 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.
  24. 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.
  25. 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.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. 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.
  41. 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.
  42. 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.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. 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.
  48. 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.
  49. 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.
  50. 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.

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