GPCR/G Protein

Items 201-250 of 6977

Page
per page
Set Descending Direction
Catalog No.
Product Name
Application
Product Information
Citations
  1. dopamine D2-receptor agonist

    ent Naxagolide Hydrochloride is a dopamine D2-receptor agonist which is used for the treatment of extrapyramidal disorders. This compound is an antiparkinsonian drug.
  2. BLT2 receptors antagonist

    LY255283 is a LTB4 receptor (BLT2) antagonist, with an IC50 of ~100 nM for [3H]LTB4 binding to guinea pig lung membranes.
  3. 5-HT1A receptor antagonist

    NAD 299 hydrochloride (Robalzotan) is a selective, high affinity 5-HT1A receptor antagonist (Ki = 0.6 nM in vitro).
  4. CGRP receptor antagonist

    BMS-927711 is a potent, selective, competitive human calcitonin gene-related peptide (CGRP) receptor antagonist that has shown in vivo efficacy without vasoconstrictor effect.
  5. NK1 receptor antagonist

    Casopitant mesylate is the mesylate salt of a centrally-acting neurokinin 1 (NK1) receptor antagonist with antidepressant and antiemetic activities.
  6. tachykinin NK2 receptor antagonist

    Ibodutant is a tachykinin NK2 receptor antagonist for the treatment of Irritable Bowel Syndrome with diarrhoea (IBS-D)
  7. Oxytocin Receptor Antagonist

    Retosiban (GSK-221,149-A) is an oral drug which acts as a selective, sub-nanomolar (Ki = 0.65 nM) oxytocin receptor antagonist with >1400-fold selectivity[3] over the related vasopressin receptors
  8. mGlu2 receptor agonist

    LY 379268 is a highly selective group II mGlu receptor agonist (EC50 values are 2.69 and 4.48 nM for hmGlu2 and hmGlu3 respectively) that displays > 80-fold selectivity over group I and group III receptors.
  9. ultra-long-acting β??? adrenoreceptor agonist

    Vilanterol is a novel and selective agonist of Beta2-AR with a PEC50 value of 10.37??0.05.
  10. dopamine uptake inhibitor

    GBR 12783 dihydrochloride is a very potent and selective inhibitor of dopamine uptake (IC50 for inhibition of [3H]-dopamine uptake in rat striatal synaptosomes is 1.8 nM).
  11. D2 receptor antagonist

    Veralipride is a D2 receptor antagonist. It is an alternative antidopaminergic treatment for menopausal symptoms.
  12. 5-HT1B/1D receptors agonist

    Donitriptan is a potent, high efficacy agonist at 5-HT1B/1D receptors with pKis of 9.4 and 9.3, respectively.
  13. NK1R antagonist

    Befetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist.
  14. ETA receptor antagonist

    ZD-1611 is a potent, orally active, selective ETA receptor antagonist, used for the research of ischemic stroke.
  15. MK-447 is a free radical scavenger, also a nonsteroidal antiinflammatory agent, and enhances the formation of the endoperoxide, PGH2, and other prostaglandins.
  16. PAR2 agonist

    AC-264613 is a potent and selective protease-activated receptor 2 (PAR2) agonist (pEC50 = 7.5).
  17. CRTH2 receptor antagonist

    AZD1981, as a potent antagonist in a disease relevant cell system, inhibits DK-PGD2-induced CD11b expression in human eosinophils with IC50 of 10 nM.
  18. Sigma-1 antagonist

    BD-1047 2HBr is a selective functional antagonist of sigma receptors, shows antipsychotic activity in animal models predictive of efficacy in schizophrenia.
  19. endothelin receptor agonist

    RO462005 is an endothelin receptor selective agonist.
  20. β2 adrenergic antagonist

    ICI 118551 hydrochloride is a selective β2 adrenergic antagonist.
  21. mGlu5 receptor antagonist

    MPEP is a potent, highly selective non-competitive antagonist at the mGlu5a receptor subtype (IC50 = 36 nM) while having no agonist or antagonist activities at the mGlu1b receptor at concentrations up to 30 uM.
  22. prostaglandin (PG) antagonist

    Aligeron is a non-selective prostaglandin (PG) antagonist, and has vasodilatory properties.
  23. 5-HT2B receptor antagonist

    PRX-08066, a Novel 5-Hydroxytryptamine Receptor 2B Antagonist, reduced monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats.
  24. 5-HT Receptor antagonist

    Tandospirone is a partial agonist at 5HT1A receptors. It significantly reduces haloperidol-induced bradykinesia in a dose-dependent manner.
  25. Urotensin-II receptor antagonist

    Palosuran is a new potent and specific antagonist of the human UT receptor with an IC50 of 3.6??0.2 nM.
  26. A1 adenosine receptor agonist

    Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.
  27. S1P1 receptor modulator

    Ponesimod is an orally active, selective sphingosine-1-phosphate receptor 1 (S1P1) immunomodulator with EC50 of 5.7 nM.
  28. S1PR1 inhibitor

    KRP-203 is a selective Sphingosine-1-phosphate receptor agonist. It shows to reduce peripheral lymphocyte infiltration and to prolong survival in rat transplant models.
  29. Bamirastine inhibits ligand binding to recombinant human histamine H1 receptors (rhH1R) with an IC50 value of 17.3 nM.
  30. leukotriene biosynthesis inhibitor

    MK-886 is an inhibitor of leukotriene biosynthesis (IC50 = 3 nM in human polymorphonuclear leukocytes).
  31. guanylate cyclase activator

    (4-Acetamidocyclohexyl) nitrate (BM121307) is a guanylate cyclase activator that was in phase I development for the treatment of ischaemic heart disorders. The research has been discontinued.
  32. Thioridazine is a dopamine receptor antagonist that displays antipsychotic activity. Recently thioridazine is also reported to successfully kill human cancer stem cells.
  33. AT1 receptor antagonist

    Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure.
  34. mGluR2 modulator

    BINA is a selective positive allosteric modulator of mGlu2 (EC50 = 33.2 nM in CHO cells expressing human mGlu2).
  35. CaSR antagonist

    NPS-2143 is a selective Ca2+-sensing receptor antagonist, shown to block increases in cytoplasmic Ca2+ concentrations elicited by human Ca2+ receptors expressed in HEK293 cells with an IC50 of 43 nM.
  36. 5-HT1D receptor antagonist

    BRL-15572 is a selective h5-HT1D antagonist, displaying 60-fold selectivity over h5-HT1B, and exhibiting little or no affinity for a range of other receptor types.

  37. mGluR5 modulator

    ADX-47273 is a drug used in scientific research which acts as a positive allosteric modulator selective for the metabotropic glutamate receptor subtype mGluR5.

  38. FAAH Inhibitor

    PF-3845 is a potent, selective, and irreversible inhibitor of FAAH (Ki = 0.23 μM). It reduces inflammatory pain via a cannabinoid receptor-dependent mechanism.

  39. 5-HT1A agonist

    BMY 7378 is a 5-HT1A partial agonist and high affinity α1D adrenoceptor antagonist.
  40. Opioid Receptors agonist

    BRL 52537 hydrochloride is a highly selective and potent κ-opioid agonist (Ki = 0.24 nM).
  41. Dopamine D2 inhibitor

    Lurasidone is an atypical antipsychotic that alleviates positive symptoms (e.g., hallucinations, delusions) without inducing extrapyramidal side effects except for akathisia,despite its potent D2 antagonistic actions.
  42. PAFR inhibitor/H1 receptor inhibitor

    Rupatadine is an inhibitor of PAFR and histamine (H1) receptor with Ki of 550 and 102 nM, respectively.
  43. 5-HT3 antagonist

    Tropisetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting following chemotherapy.
  44. Metoprolol succinate is a cardioselective β-adrenergic receptor blocker with IC50 of 42 ng/mL.
  45. CB2 receptor agonist

    GW842166X is a selective non-cannabinoid CB2 receptor agonist, which is undergoing clinical development as a novel oral treatment for inflammatory pain
  46. CGRP receptor antagonist

    MK-0974 (Telcagepant) is a potent and selective antagonist of the human and rhesus CGRP receptors.
  47. Opioid antagonist

    Alvimopan behaves as a peripherally acting μ-opioid antagonist. Alvimopan competitively binds to mu-opioid receptor in the gastrointestinal tract.
  48. D2 receptor antagonist

    Adoprazine is part of the Antidepressant Agent group
  49. Endothelin antagonist

    Avosentan (SPP301) is a potent and highly selective ETA receptor blocker.
  50. Serotonin 5HT3-receptor antagonist

    Alosetron Hydrochloride(1:X) (GR 68755 Hydrochloride(1:X)) is a Serotonin 5HT3-receptor antagonist that is used in treatment of irritable bowel syndrome.

Items 201-250 of 6977

Page
per page
Set Descending Direction