GPCR/G Protein

Items 4501-4550 of 6966

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  1. PGF2α Analog

    15-Keto Bimatoprost is a potent prostaglandin F2α (PGF2α) analog that primarily targets ocular tissues. This compound exhibits significant biological activity in reducing intraocular pressure, making it valuable for research into therapies for glaucoma and other ocular hypertension conditions. Its mechanism of action facilitates enhanced aqueous humor outflow, providing insight into the regulation of intraocular pressure in various in vitro and in vivo studies.
  2. NSAID

    Alclofenac (lysinate) is a non-steroidal anti-inflammatory drug (NSAID) that functions primarily as a prostaglandin H2 synthase inhibitor. It exhibits significant anti-inflammatory and analgesic properties, making it valuable for the study of conditions such as rheumatoid arthritis, degenerative joint disease, and ankylosing spondylitis. This compound is an essential tool for researchers investigating inflammatory pathways and evaluating potential therapeutic interventions in related diseases.
  3. hDP Agonist

    L-644698 is a highly selective agonist of the human recombinant prostaglandin D2 (PGD2) receptor (hDP), exhibiting Ki values of 0.9 nM for hDP and significantly higher values for other receptors (hEP2, hEP3, hEP4). This compound stimulates cyclic AMP production with an EC50 of 0.5 nM, making it a valuable tool for researching PGD2 receptor signaling pathways and their implications in various biological processes. Its specificity and potency render L-644698 an essential reagent for studies aimed at understanding the role of hDP in physiological and pathological states.
  4. Prostaglandin Receptor

    15-keto-17-phenyl trinor Prostaglandin F2α is a potent analog targeting prostaglandin receptors. It demonstrates significant biological activity by slightly reducing intraocular pressure in normal cynomolgus monkeys and effectively acting as a miotic agent in felines, notably decreasing pupil diameter. This compound is useful for research applications related to ocular physiology and the pharmacological effects of prostaglandin analogs.
  5. EP4 Receptor Antagonist

    ASP7657 free base is a potent orally active antagonist of the EP4 receptor, exhibiting binding affinities (Kis) of 2.21 nM for human EP4 and 6.02 nM for rat EP4 receptors. This compound demonstrates significant biological activity in modulating inflammatory responses and is particularly useful in research focused on conditions related to pain, inflammation, and various immune disorders. Its selective action on the EP4 receptor makes it an important tool for investigating therapeutic strategies in relevant disease models.
  6. EP1/EP3 Receptor Agonist

    Nocloprost is an orally active agonist of the EP1 and EP3 receptors, functioning as a prostaglandin E2 (PGE2) analog. This compound demonstrates significant biological activity by inhibiting evoked [3H]ACh release, showcasing its potential in neuroprotective research. Nocloprost exhibits gastroprotective and ulcer-healing properties, effectively accelerating the healing of chronic gastric ulcers and promoting mucosal growth in experimental models. As such, it serves as a valuable reagent for studying gastrointestinal health and related therapeutics.
  7. EP4 receptor Agonist

    EP4 receptor agonist 3 selectively targets the EP4 receptor, functioning as an effective agonist. This compound is utilized in research applications related to inflammatory bowel disease, particularly in colitis models in mice induced by dextran sulfate sodium (DSS). Its activation of the EP4 receptor pathway offers valuable insights into potential therapeutic strategies and mechanisms underlying gastrointestinal inflammation.
  8. Thromboxane A2 Receptor Antagonist

    CGS-22652 is a potent antagonist of the thromboxane A2 receptor. It exhibits selective inhibitory properties against thromboxane A2 synthase, making it valuable in studies investigating the role of thromboxane A2 in cardiovascular conditions. CGS-22652 is particularly relevant for research on coronary artery thrombosis and related thrombotic disorders.
  9. EP1 Receptor Agonist

    17-Phenyl trinor prostaglandin E2 ethyl amide is a potent agonist of the EP1 receptor. This compound has been shown to exacerbate renal dysfunction and contribute to the progression of glomerulosclerosis. It serves as a valuable tool for studying the roles of EP1 receptor activation in renal pathophysiology and related research applications.
  10. Prostacycline Analogue

    6β-Prostaglandin I1 is a stable analog of prostaglandin I2 (PGI2) that exhibits resistance to hydrolysis in aqueous environments. This compound is known for its ability to significantly reduce gastric acid secretion, with an ID50 of approximately 3.0 μg/kg/min when administered via intravenous injection. Its unique properties make it valuable for research applications in gastrointestinal physiology and the study of prostaglandin signaling pathways.
  11. Thromboxane Synthetase Inhibitor

    UK 34787 is a selective thromboxane synthetase inhibitor that exhibits minimal activity against cyclooxygenase and prostacyclin synthetase. This compound is utilized in research to study thromboxane's role in cardiovascular function and various pathophysiological conditions. Its specificity makes it a valuable tool in investigating the therapeutic potential of thromboxane modulation in disease models.
  12. Thromboxane Synthase Inhibitor

    Wy 27569 is a thromboxane synthase inhibitor that modulates prostaglandin balance by decreasing pro-thrombotic thromboxane A2 (TXA2) and increasing anti-thrombotic prostacyclin (PGI2). This compound is known for its vascular selectivity and ability to effectively lower blood pressure. Wy 27569 is utilized in research on cardiovascular diseases, including hypertension and angina, making it valuable for understanding thrombotic processes and vascular health.
  13. Thromboxane A2 Synthetase Inhibitor

    Nafagrel hydrochloride is a potent thromboxane A2 synthetase inhibitor. This compound effectively prevents thrombus formation, demonstrated in a rat model of acute arterial thrombosis. It is valuable for research applications related to cardiovascular disease, thrombosis, and related therapeutic interventions.
  14. TAX2 Antagonist

    I-SAP is a radioiodinated antagonist of the thromboxane A2 (TXA2)/prostaglandin H2 (PGH2) receptor. This compound effectively inhibits receptor binding, which can be altered by histidine-modifying agents such as diethyl-pyrocarbonate (DEPC). I-SAP is utilized in research related to cardiovascular biology, particularly in studies examining TXA2 signaling pathways and their physiological effects.
  15. Prostaglandin Receptor Antagonist

    AH22921 is a selective antagonist of the EP4 prostaglandin receptor, inhibiting the activation of adenylate cyclase by prostaglandins in CHO cells. This compound is characterized by its ability to shift the PGE2 concentration-response curve to the right, demonstrating its non-competitive antagonistic effect specifically on EP4 receptors. Notably, AH22921 does not influence the PGE2 concentration-response curve in NPE cells that express EP2 receptors, making it a valuable tool for studying EP4 receptor signaling in varied biological contexts.
  16. Prostaglandin Analog

    N-Cyclopropyl bimatoprost is a prostaglandin analog that primarily targets the prostaglandin receptors. It has been shown to exhibit significant biological activity in modulating intraocular pressure and can be utilized in research related to glaucoma and other ocular conditions. Additionally, this compound may be important for investigating epithelial-associated pathologies, providing insights into its therapeutic potential.
  17. Enantiomer

    15β-Travoprost is an enantiomer of Travoprost that functions as a selective full agonist of the FP prostaglandin receptor. It exhibits high affinity for the receptor and is primarily used in research applications focusing on glaucoma treatment and intraocular pressure modulation. This compound's unique chemical properties make it a valuable tool in studying FP receptor-related biological processes and developing therapeutic strategies targeting ocular conditions.
  18. Endogenous Hormone

    Prostaglandin D2 serinol amide is an endogenous hormone that acts as a weak inhibitor of the hydrolysis of [3H]2-oleoylglycerol. This compound is relevant for studies investigating lipid metabolism and signaling pathways associated with inflammatory responses. Its unique mechanism makes it a valuable tool for researchers exploring the role of prostaglandins in various physiological and pathophysiological processes.
  19. Thromboxane Synthetase Inhibitor

    Dazoxiben is an effective thromboxane synthetase inhibitor that functions to reduce thromboxane production, thereby influencing platelet aggregation and vasoconstriction. This compound is particularly relevant in the investigation of vascular conditions, such as Raynaud's syndrome, where thromboxane overproduction may play a critical role. Its oral bioavailability makes it suitable for in vivo studies on thromboxane-related pathologies.
  20. Bronchoconstrictor

    16,16-Dimethylprostaglandin E1 is a synthetic analog of prostaglandin E1 that primarily acts as a bronchoconstrictor by inducing contraction of smooth muscle tissue. Its ability to elicit vascular smooth muscle contractions makes it valuable in studying respiratory function and vascular dynamics. Additionally, 16,16-Dimethylprostaglandin E1 has been shown to suppress cellular elongation induced by indomethacin, providing insights into its potential applications in inflammatory research.
  21. TP Agonist

    I-BOP is a potent thromboxane A2 receptor (TP) agonist with a binding affinity (KD) of 0.61 nM. It facilitates cellular proliferation by activating the PI3K signaling pathway in vascular smooth muscle cells. Additionally, I-BOP exhibits a biphasic, dose-dependent modulation of excitatory postsynaptic potentials in hippocampal neurons, making it a valuable tool for research in vascular biology and neurophysiology.
  22. EP1 Antagonist

    MF266-1 is a selective antagonist of the E prostanoid receptor 1 (EP1), demonstrating a Ki value of 3.8 nM. It exhibits moderate selectivity for the thromboxane A2 receptor (TP). This compound has potential applications in the research of arthritis and related inflammatory conditions.
  23. TXA2/H1 antagonist

    KF15766 is an orally active dual antagonist of thromboxane A2 (TXA2) and histamine H1 receptors, exhibiting inhibition constants (Kis) of 740 nM and 20 nM, respectively. This compound demonstrates significant potential for therapeutic applications in antiallergic research, allowing for the exploration of its effects on allergic responses and related disorders. Its dual-target mechanism makes KF15766 an important tool in the study of asthma and other allergic conditions.
  24. Prostacyclin Agonist

    BMY 42393 is an orally active prostacyclin agonist that modulates monocyte and macrophage functions, effectively suppressing their atherogenic activity and cytokine production. This compound is particularly valuable for research focused on atherosclerosis and its related mechanisms, providing insights into cardiovascular health and inflammatory response pathways.
  25. IOP Reducing Agent

    PGF2α-isopropyl ester is a derivative of Prostaglandin F2α that functions as an intraocular pressure (IOP) reducing agent. It primarily enhances the uveoscleral outflow of aqueous humor, effectively decreasing IOP. This compound is utilized in research related to glaucoma and related ocular conditions, though it may cause side effects such as conjunctival hyperemia and ocular irritation.
  26. PGHS-2 Inhibitor

    15(S)-HpEPE is a lipoxygenase-derived hydrolysis product of polyunsaturated fatty acids (PUFAs), serving as a potential inhibitor of prostaglandin H synthase 2 (PGHS-2). This compound has been shown to downregulate PGHS-2 expression, making it a valuable tool for research focused on inflammatory pathways and associated diseases. Its biological activity is of interest in studies examining the modulation of prostaglandin synthesis and the regulation of inflammatory responses.
  27. 15(R) Stereoisomer of PGA1

    15-epi Prostaglandin A1 (15-epi PGA1) is the 15(R) stereoisomer of Prostaglandin A1. This compound primarily induces renal vasodilation, enhances the excretion of sodium in urine, and lowers arterial pressure in hypertensive models. Its biological activity makes it a valuable tool for research in cardiovascular and renal physiology, as well as studies focused on hypertension.
  28. PTGR2 Inhibitor

    RJG-2036 is a potent covalent inhibitor of human prostaglandin reductase 2 (PTGR2) with an IC50 value of 100 nM. This compound effectively inhibits NADPH-dependent reduction, leading to a significant decrease in the secretion of proinflammatory cytokines such as TNF-α and various eicosanoids in LPS-stimulated THP-1 macrophages. RJG-2036 serves as a valuable tool for investigating the molecular mechanisms underlying inflammatory diseases.
  29. TxA2 Synthase/Receptor Inhibitor

    Picotamide monohydrate is a dual inhibitor of thromboxane A2 (TxA2) synthase and its receptor, exhibiting significant antiplatelet activity. This compound has been shown to reduce microalbuminuria and inhibit the progression of carotid plaques in diabetic models. Picotamide monohydrate serves as a valuable tool for investigating both acute and chronic cardiovascular diseases in research settings.
  30. TBXA2R Antagonist

    Domitroban is a thromboxane A2 receptor (TBXA2R) antagonist that effectively inhibits platelet aggregation. This compound is valuable for research focused on cardiovascular diseases, particularly in the context of thrombosis. Its antagonistic action on TBXA2R makes it an essential tool for studying platelet-related disorders and developing therapeutics for cardiovascular conditions.
  31. Prostaglandin E2 Inhibitor

    Seprilose is a potent inhibitor of prostaglandin E2 synthesis, acting primarily by targeting the relevant enzymatic pathways involved in its production. This compound demonstrates significant anti-inflammatory activity, making it valuable for research applications focused on inflammation and related disorders. Seprilose can be utilized in studies examining the role of prostaglandins in various physiological and pathological processes.
  32. Prostaglandin E1 Metabolite

    Prostaglandin B1 (PGB1) is a metabolite of Prostaglandin E1, acting as a ligand for prostanoid receptors. It plays a significant role in various biological processes, including mediating inflammation and regulating vascular functions. PGB1 is widely used in research to explore its physiological effects and potential therapeutic applications in cardiovascular and inflammatory diseases.
  33. Thromboxane Synthase Inhibitor

    Imitrodast is a selective thromboxane synthase inhibitor, effectively blocking the conversion of arachidonic acid to thromboxane A2. This compound demonstrates significant activity in modulating bronchoconstriction and possesses potential applications in research related to respiratory disorders and cardiovascular diseases. Its mechanism may help elucidate the role of thromboxane in various pathological conditions.
  34. TXA2 Receptor Antagonist

    KT2-962 is a thromboxane A2 (TXA2) receptor antagonist and a potent hydroxyl radical scavenger (IC50=500 nM). This compound has been shown to significantly reduce myocardial infarct size and the incidence of ventricular fibrillation. In a canine model of ischemia/reperfusion, KT2-962 demonstrated notable cardioprotective effects, making it valuable for research into myocardial ischemia-reperfusion injury and TXA2-mediated vascular diseases.
  35. PTGER2 Agonist

    15(S)-Fluprostenol is a potent agonist of the PTGER2 receptor. It has been shown to decrease the expression of Oviductal glycoprotein 1 (OVGP1), indicating its potential role in regulating reproductive processes. This compound is useful in research applications related to prostaglandin signaling pathways and reproductive biology studies.
  36. Platelet Aggregation Inhibitor

    Octimibate is a non-prostaglandin platelet aggregation inhibitor, acting primarily to prevent platelet activation and aggregation. This compound is utilized in research focused on cardiovascular diseases, specifically in the contexts of atherosclerosis and thrombosis, to elucidate the underlying mechanisms and potential therapeutic strategies for these conditions.
  37. Prostaglandin Analog

    (15R)-Bimatoprost is a prostaglandin analog that primarily targets the prostaglandin receptor pathways. This compound is utilized in the research of glaucoma and ocular hypertension, providing valuable insights into their mechanisms and treatment options. As an isomer of Bimatoprost, (15R)-Bimatoprost features an inverted (β) hydroxyl group at C-15, which may contribute to its unique biological activities.
  38. Antiulcer Compound

    Spizofurone is an anti-ulcer compound that enhances gastric mucosal blood flow, demonstrating significant oral bioactivity. It shares a mechanism of action similar to PGE2, functioning through both local and systemic pathways to promote ulcer healing by improving blood supply to the gastric mucosa. This compound is valuable for research into the strategies for treating and managing gastric ulcers.
  39. Thromboxane Synthase Inhibitor

    Rolafagrel is a selective inhibitor of thromboxane synthase, a key enzyme involved in the synthesis of thromboxane A2, which plays a pivotal role in platelet aggregation and vascular contraction. This compound has significant implications in cardiovascular research, facilitating the study of thromboxane-mediated pathways and their contribution to various cardiovascular disorders. Its use may aid in the development of therapeutic strategies targeting thromboxane-related conditions.
  40. EP3 Antagonist

    EP3 Antagonist 4 is a selective antagonist of the EP3 receptor, exhibiting a Ki value of 2 nM for human EP3. It demonstrates low in vivo clearance and high oral bioavailability, as evidenced by pharmacokinetic studies in rats. This compound is primarily utilized in the research of beta cell dysfunction in diabetes, contributing to our understanding of metabolic disorders and potential therapeutic interventions.
  41. Endogenous Hormone

    Prostaglandin F2α alcohol methyl ether is a G protein-coupled receptor that acts as an analog of the endogenous hormone prostaglandin F2α. This compound exhibits significant biological activity in pain modulation, potentially serving as a nociceptive mediator in the spinal cord. It is applicable in research exploring reproductive biology, particularly in the context of luteinizing hormone function and associated signaling pathways.
  42. Antihypertensive Agent

    15-Deoxy-16-hydroxy-16-vinyl-PGE2 Me ester is a PGE2 analogue exhibiting antihypertensive properties. This compound functions primarily by modulating vascular tone and promoting vasodilation, making it a valuable tool in cardiovascular disease research. Its utility in studying mechanisms of hypertension and potential therapeutic effects on related disorders further underscores its significance in the field of cardiovascular pharmacology.
  43. Prostaglandin Receptor Control

    15-OH Tafluprost is a synthetic analog of prostaglandin F2α (PGF2α) that targets prostaglandin receptors to modulate vascular responses. It effectively alleviates endothelin-1 (ET-1)-induced impairments in optic nerve head (ONH) blood flow and counteracts contraction of isolated ciliary artery segments. This compound is pertinent for investigating mechanisms of intraocular pressure regulation and potential therapeutic approaches for glaucoma-related vascular dysfunction.
  44. DP2 Receptor Inhibitor

    CRTh2 antagonist 4 is a selective inhibitor of the DP2 receptor, displaying an IC50 value of 212 nM and a binding affinity with a Ki of 37 nM. This compound is useful in the investigation of TH2 lymphocyte-related pathways and has potential applications in understanding and treating severe allergic diseases.
  45. Prostaglandin Receptor Agonist

    Δ17-6-keto Prostaglandin F1α is a prostaglandin receptor agonist derived from the cyclooxygenase pathway of eicosapentaenoic acid (EPA). This compound is known to exhibit key biological activity, potentially influencing inflammatory responses and vascular dynamics. Research suggests that Δ17-6-keto PGF1α, along with other 3-series COX products from EPA, may play a role in mitigating the risk of glaucoma, particularly in populations with diets rich in marine sources of EPA.
  46. EP4 Receptor Agonist

    EP4 Receptor Agonist 1 is a selective agonist for the EP4 receptor, demonstrating a human pEC50 value of 6.3. This compound is pivotal for studying the physiological roles of EP4 in various biological processes. Research applications include exploring mechanisms related to inflammation, pain modulation, and potential therapeutic avenues for diseases where EP4 signaling is implicated.
  47. Thromboxane Synthase Inhibitor

    Imitrodast sodium is a potent thromboxane synthase inhibitor. This compound plays a significant role in research related to bronchoconstriction and its associated pathways. Its ability to inhibit thromboxane production offers insights into the mechanisms of allergic reactions and pulmonary function, making it valuable for studies focused on respiratory health and related conditions.
  48. Pain Reliever

    Nocistatin (human) is a peptide that acts as a potent pain reliever by blocking nociceptin-induced allodynia and hyperalgesia. Its ability to attenuate pain evoked by prostaglandin E2 positions Nocistatin as a valuable reagent for research in pain management and nociceptive signaling pathways. This compound is relevant for studies aimed at understanding pain mechanisms and developing therapeutic strategies for pain relief.
  49. Vasoconstrictor

    ent-8-iso Prostaglandin F2α is a potent vasoconstrictor primarily targeting porcine retinal and cerebral microvessels. It exhibits EC50 values of 30.6 nM and 53.5 nM, respectively, demonstrating its effectiveness in modulating vascular tone. This compound is useful for research applications involving vascular biology, neurovascular function, and studies of ocular physiology.
  50. EP2 Antagonist

    TG11-77 hydrochloride is a highly selective antagonist of the EP2 receptor, demonstrating potent inhibition with a KB value of 9.7 nM. This compound effectively blocks PGE2-induced activation of the human EP2 receptor, leading to significant anti-inflammatory effects. TG11-77 hydrochloride has also been shown to reduce delayed mortality and mitigate memory deficits, making it a valuable tool for research in neuroinflammation and related therapeutic areas.

Items 4501-4550 of 6966

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