GPCR/G Protein

Items 6101-6150 of 6966

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  1. S1P1 Agonist

    S1P1 agonist 6 hemicalcium is a selective agonist of the sphingosine-1-phosphate receptor 1 (S1P1), primarily functioning to inhibit lymphocyte trafficking. This mechanism results in the reduction of autoimmune responses, making it a valuable tool for studying various autoimmune diseases. Its immunosuppressive properties allow researchers to investigate potential therapeutic applications in immune modulation and related research areas.
  2. LPA Receptor Agonist

    2ccPA sodium is a potent lysophosphatidic acid (LPA) receptor agonist. By activating LPA receptors and inhibiting the activity of the autotaxin (ATX) enzyme, it plays a significant role in regulating cell proliferation, migration, and apoptosis. This compound is valuable for research into various biological processes and disease states, including cancers, inflammation, and fibrosis.
  3. S1P1 Receptor Agonist

    BMS-960 is a potent and selective agonist of the S1P1 receptor. It has been demonstrated to modulate immune responses and improve vascular function, making it a valuable tool in the study of immune and vascular diseases. Research applications include exploring pathways related to inflammation, lymphocyte trafficking, and cardiovascular health.
  4. S1P4 Receptor Antagonist

    CYM50358 hydrochloride is a potent and selective antagonist of the sphingosine-1-phosphate 4 (S1P4) receptor. This compound exhibits significant biological activity by inhibiting S1P4-mediated signaling pathways, making it a valuable tool in research focused on the immune response and inflammation. Its application extends to the study of influenza infection, facilitating investigations into viral pathogenesis and potential therapeutic interventions.
  5. S1PR1 Agonist

    S1PR1 Agonist 1 is a potent agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), a member of the G protein-coupled receptor family. This compound modulates cellular signaling pathways linked to immune response and inflammation, making it a valuable tool for investigating autoimmune diseases. Its application extends to research focused on understanding the role of sphingolipid signaling in various physiological and pathological conditions.
  6. Sphingosine 1-phosphate Receptor Modulator

    CS-0777 is a selective sphingosine 1-phosphate receptor-1 modulator that exhibits oral bioavailability. This compound is primarily utilized in research focused on autoimmune diseases, where it influences immune cell trafficking and potentially alters disease progression. Its mechanism of action offers valuable insights into the therapeutic targeting of sphingosine pathways in various pathological conditions.
  7. S1PR1 Agonist

    RP101442 is a selective and potent agonist of the sphingosine-1-phosphate receptor 1 (S1PR1), exhibiting an EC50 of 2.6 nM. Additionally, it shows activity toward S1PR5 with an EC50 of 171 nM. This compound is primarily utilized in research exploring immune responses and neuroprotection, making it valuable for studies on inflammatory diseases and related therapeutic areas.
  8. S1PR1 Agonist

    S1PR1 Agonist 2 is a potent agonist targeting the S1P receptor 1 (S1PR1). This compound, derived from sphingosine-1-phosphate (S1P), engages G protein-coupled receptors, influencing various physiological processes. S1PR1 Agonist 2 is primarily utilized in research studies focused on autoimmune diseases, facilitating the exploration of therapeutic strategies in this area.
  9. S1P5 Receptor Antagonist

    S1P5 receptor antagonist 1 is a selective antagonist targeting the S1P5 receptor, characterized by an EC50 of 0.1 nM and a Ki of 4.4 nM. This compound is capable of inhibiting the migration of natural killer cells towards sphingosine 1-phosphate in vitro, while leaving T cell migration unaffected. S1P5 receptor antagonist 1 is employed in research focused on central nervous system diseases, providing insights into the modulation of immune responses within the brain.
  10. LPAR1 Antagonist

    LPAR1 Antagonist 2 is a selective antagonist of the lysophosphatidic acid receptor 1 (LPAR1), demonstrating an average IC50 of 130 nM. This compound is utilized in research to investigate the role of LPAR1 in various physiological and pathological processes, including cancer progression and neurodegenerative diseases. Its inhibition of LPAR1 signaling makes it a valuable tool for studying receptor-mediated pathways and developing therapeutic strategies targeting this receptor.
  11. Drug Isomer

    (Rac)-1-Oleoyl lysophosphatidic acid is an isomer of 1-Oleoyl lysophosphatidic acid that acts as a potent bioactive lipid. This compound primarily targets the lysophosphatidic acid (LPA) receptors, modulating various cellular responses associated with cell proliferation, migration, and survival. Its application in research includes studies focused on cancer biology, wound healing, and neurobiology, contributing to a better understanding of LPA signaling pathways and their role in disease processes.
  12. LPAR1 antagonist

    BMT-136088 is an LPAR1 antagonist that effectively inhibits the activity of the lysophosphatidic acid receptor 1. This compound can be utilized as a positron emission tomography (PET) radioligand for the quantitative assessment of specific binding to LPA1 in lung tissues. Its application in research can enhance the understanding of LPAR1’s role in various biological processes and pathological conditions.
  13. LPL Receptor Antagonist

    S1P2 antagonist 1 is a potent oral antagonist of the sphingosine-1-phosphate receptor 2 (S1P2). It demonstrates significant biological activity in inhibiting pathways associated with fibrotic diseases. This compound is suitable for research applications exploring the modulation of fibrogenesis and related pathological conditions.
  14. LPA Inhibitor

    L-NASPA ammonium is an effective LPA inhibitor that targets lysophosphatidic acid signaling pathways. It is utilized in research focused on platelet activation and related cellular processes. By inhibiting LPA, this compound aids in elucidating the mechanisms underlying platelet function and potential therapeutic interventions in related disorders.
  15. SPNS2 Inhibitor

    Spns2-IN-3 is a selective SPNS2 inhibitor that targets sphingolipid metabolism. This compound exhibits significant biological activity in modulating sphingolipid pathways, making it crucial for research applications involving cellular signaling and lipid biology. Its unique structure may facilitate the development of drug carriers, enhancing the delivery and penetration of therapeutic molecules across biological membranes, particularly in dermatological settings.
  16. S1P1 antagonist

    (R)-VPC44116 is a selective antagonist of the sphingosine-1-phosphate receptor 1 (S1P1). This compound is primarily utilized in lipid signaling research and plays a crucial role in studying immune response, cell migration, and vascular development. Its ability to modulate S1P1 activity makes it valuable for investigating various pathophysiological conditions, including autoimmune diseases and cardiovascular disorders.
  17. Phospholipid

    1-Arachidonoyl-2-hydroxy-sn-glycero-3-PA is a phospholipid that features arachidonic acid at the sn-1 position and serves as a precursor to 1-arachidonoyl glycerol. This compound exhibits potent binding to the LPA2/EDG4 receptor, with an EC50 value of approximately 10 nM. Its biological activity includes the inhibition of TNF-α and IL-6 secretion in wild-type dendritic cells activated by LPS, as well as the reduction of HT-29 human colon carcinoma cell differentiation into goblet cells upon sodium butyrate treatment. This makes it a valuable tool for studying inflammation and cancer biology.
  18. SPC Receptor Antagonist

    KRO-105714 is a selective antagonist of the sphingosine phosphocholine receptor (SPC Receptor) and the sphingosine-1-phosphate receptor 1 (S1P1 Receptor), with an IC50 of 79.2 nM. This compound effectively inhibits SPC-induced cell proliferation in NIH3T3 cells (IC50 = 5.6 nM), as well as SPC-induced cell migration (IC50 = 0.59 μM) and tube formation in human umbilical vein endothelial cells (HUVECs). Additionally, KRO-105714 suppresses the generation of pro-inflammatory cytokines IL-4 and IL-5, demonstrating its potential for use in anti-inflammatory research, particularly in mouse models of atopic dermatitis.
  19. LPA Receptor Antagonist

    LPA Receptor Antagonist-1 functions as a selective antagonist of lysophosphatidic acid (LPA) receptors, which play a crucial role in various cellular signaling pathways. This compound demonstrates significant biological activity by inhibiting LPA-mediated responses, making it a valuable tool for research into cellular processes related to cancer, fibrosis, and neurodegenerative diseases. Researchers can utilize LPA Receptor Antagonist-1 to investigate the implications of LPA signaling in multiple biological contexts.
  20. S1PR1 ligand

    S1PR1 ligand 1 is a specific agonist targeting the S1PR1 receptor with an IC50 of 8.7 nM. This compound demonstrates favorable brain permeability, making it suitable for exploring S1PR1 functions in neurological disorders. Additionally, S1PR1 ligand 1 can be labeled with 18F for imaging studies, facilitating research into its role in brain pathologies.
  21. S1PR3 antagonist

    VPC 01091 is a selective antagonist of the sphingosine-1-phosphate receptor 3 (S1PR3). This compound effectively inhibits S1PR3-mediated signaling pathways, which are implicated in various physiological processes including immune regulation and vascular dynamics. VPC 01091 serves as a valuable tool for research applications aimed at exploring the role of S1PR3 in pathophysiology and therapeutic interventions.
  22. S1P1 Receptor Agonist

    ACT-209905 is an agonist of the S1P1 receptor, demonstrating potent inhibition of glioblastoma (GBM) cell growth and migration. In addition to its antitumor properties, ACT-209905 exhibits immunomodulating activity, making it a valuable tool for investigating autoimmune diseases. This compound is suitable for research applications aimed at elucidating the roles of S1P1 signaling in cancer and immune regulation.
  23. Sphingosine-1-phosphate Receptor 1 Agonist

    AUY954 is a selective agonist of the sphingosine-1-phosphate receptor 1, exhibiting an EC50 of 1.2 nM for the human S1P1 receptor. This compound demonstrates significant biological activity in modulating immune responses and is primarily utilized in research focused on experimental autoimmune neuritis. AUY954's selective action makes it a valuable tool for studying the role of sphingosine-1-phosphate signaling in various autoimmune conditions.
  24. S1P1 Receptor Partial Agonist

    BMS-986104 hydrochloride is a selective partial agonist of the S1P1 receptor, involved in modulating sphingosine-1-phosphate signaling pathways. This compound exhibits potential therapeutic effects in the context of autoimmune diseases by influencing lymphocyte trafficking and immune response. It serves as a valuable tool for research aimed at understanding and developing treatments for various autoimmune disorders.
  25. LPA Inhibitor

    L-NASPA is a potent lysophosphatidic acid (LPA) inhibitor that plays a significant role in research related to platelet activation. By blocking LPA signaling pathways, L-NASPA enables the investigation of its effects on cellular processes involved in thrombosis and inflammation. This compound is valuable for studies aimed at understanding the physiological and pathological roles of LPA in various biological contexts.
  26. LPL Receptor Modulator

    S1PR1-MO-1 is a modulator of the sphingosine-1-phosphate receptor (S1PR1) that plays a critical role in various cellular processes. It exhibits significant biological activity in regulating inflammatory responses and hyperproliferative conditions. This reagent is primarily utilized in research focused on understanding and developing therapeutic strategies for inflammatory diseases and related disorders.
  27. Antispasmodic Opioid Alkaloid

    Pargeverine hydrochloride is an antispasmodic opioid alkaloid that primarily targets muscarinic cholinergic receptors, exhibiting a moderate and non-selective blockade. This compound is utilized in research to investigate mechanisms underlying painful spasms and their management. Its application in understanding muscle contraction and relaxation makes it a valuable reagent in pharmacological studies.
  28. M1 Muscarinic Agonist

    McN-A-343 is a selective M1 muscarinic agonist that enhances muscarinic transmission in sympathetic ganglia. This compound significantly inhibits muscarine-induced catecholamine secretion in isolated perfused rat adrenal glands and plays a role in neuronal firing regulation. Additionally, McN-A-343 activates enteroendocrine L cells to promote the release of glucagon-like peptide 1 (GLP-1) and modulates α-melanocyte stimulating hormone (α-MSH) secretion from the pituitary gland. Its capacity to reduce colonic inflammation and oxidative stress makes McN-A-343 a valuable tool for studying ulcerative colitis.
  29. mAChR Antagonist

    4-Piperidyl N-(2-biphenyl)carbamate is a competitive antagonist of muscarinic acetylcholine receptors (mAChR), exhibiting notable selectivity for the M2 and M3 subtypes. With pKi values of 7.33 for M2 and 7.51 for M3, this compound demonstrates a markedly higher affinity compared to β2 adrenergic receptors, which has a pKi of 4.94. This specificity makes it a valuable tool for research into mAChR-related signaling pathways and potential therapeutic applications in various neurological disorders.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 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.
  35. 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.
  36. 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.
  37. 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.
  38. 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.
  39. 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.
  40. Dopamine D-1 Receptor Antagonist

    A-69024 is a selective antagonist of the dopamine D-1 receptor, demonstrating a Ki value of 12.6 nM for D-1 and a significantly higher Ki value of 1290 nM for the D-2 receptor. This compound's specificity enables researchers to investigate the role of dopamine D-1 receptor modulation in various neurological and psychiatric disorders. A-69024 is valuable for studies examining dopamine-related pathways and potential therapeutic approaches.
  41. D2R Agonist

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

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

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

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

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

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

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

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

    Dopamine D2 receptor antagonist-3 is a selective antagonist of the dopamine D2 receptor, displaying a pIC50 of 5.52. This compound demonstrates antipsychotic effects, evidenced by its ability to reduce apomorphine-induced agitation in rat models. It is a valuable tool for research into psychiatric and neurological disorders, facilitating the study of dopaminergic signaling pathways and potential therapeutic interventions.
  50. D4 dopamine receptor antagonist

    L-750667 triHydrochloride is a selective antagonist of the D4 dopamine receptor, exhibiting a Ki value of 0.51 nM. Its radiolabeled derivative, [125I]L-750667, demonstrates a Kd of 0.16 nM for D4 receptor binding. This compound is capable of reversing dopamine-induced inhibition of cAMP accumulation, making it a valuable tool for investigating the distribution and function of D4 dopamine receptors in the central nervous system. L-750667 triHydrochloride has significant applications in neuroscience and psychiatry research.

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