GPCR/G Protein

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  1. 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.
  2. prostaglandin (PG) antagonist

    Aligeron is a non-selective prostaglandin (PG) antagonist, and has vasodilatory properties.
  3. 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.
  4. 5-HT Receptor antagonist

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

    Foropafant (SR27417) highly potent, competitive, selective and orally active antagonist of platelet-activating factor (PAF) receptor.
  7. Adrenoceptors antagonist

    BRL 44408 maleate is a high purity Adrenoceptors antagonist. It increases hippocampal noradrenalin release following systemic administration.
  8. Adrenergic α1 Receptor Antagonist

    HEAT hydrochloride is a very selective α1-AR adrenoceptor antagonist, precursor of the 3-[125I]-derivative. Adrenoreceptors (AR) or adrenergic receptors are G-protein coupled receptors involved in a variety of sympathetic nervous system processes.
  9. 5-HT1A receptor antagonist

    NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor.
  10. α2-adrenergic receptor antagonist

    Rauwolscine is a natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM).
  11. Adrenoceptors antagonist

    S-(-)-Atenolol is the active enantiomer of atenolol that is a cardioselective β-adrenergic blocker.
  12. Adrenoceptors antagonist

    (S)-Timolol maleate is a adrenergic receptor antagonist selective for β1-AR.
  13. Adrenoceptors antagonist

    SR 59230A hydrochloride is a β3-adrenoceptor antagonist.
  14. Histamine H4 receptor antagonist

    A 943931 2HCl is a potent and selective histamine H4 receptor antagonist (pKi values are 7.15 and 8.12 at human and rat receptors respectively).
  15. ETA/ETB antagonist

    PD-159020 is a non-selective ETA/ETB antagonist, with IC50s of 30 and 50 nM for hETA and hETB, respectively.
  16. Adenosine A2A receptor antagonist

    Preladenant is a potent and selective antagonist at the adenosine A2A receptor.
  17. Sigma2 antagonist

    UMB24 is a putative sigma2-preferring antagonist.
  18. CRF1 receptor antagonist

    R121919 is a potent small-molecule CRF1 receptor antagonist.
  19. Angiotensin AT1 receptor antagonist

    SL910102 is a nonpeptide angiotensin AT1 receptor antagonist.
  20. adrenergic receptor antagonist

    Celiprolol HCl is a b1 adrenergic receptor antagonist and a b2 adrenergic receptor partial agonist that has been shown to relax human arteries and veins with ED50 values of 40-50 M in vitro.
  21. ETBR antagonist

    IRL-2500 is a potent, selective ETBR antagonist. It shows some selectivity for ETB receptors (IC50 values are 1.3 and 94 nM for ETB and ETA receptors respectively).
  22. 5HT2A antagonist

    Ketanserin tartrate is a salt of Ketanserin. Ketanserin is reported to have a high affinity for multiple G protein-coupled receptors, such as serotonin receptors.
  23. CCK-2 receptor antagonist

    Z-360 is a selective, orally available, 1,5-benzodiazepine-derivative gastrin/cholecystokinin 2 (CCK-2) receptor antagonist with potential antineoplastic activity.
  24. G15

    GPER/GPR30 antagonist

    G15 is a high affinity and selective G-protein-coupled estrogen receptor (GPER/GPR30) antagonist with a Ki of 20 nM.
  25. dopamine D3 Receptor (DRD3) antagonist

    GSK598809 is a potent and selective dopamine D3 Receptor (DRD3) antagonist, with a pKi of 8.9.
  26. CCK antagonist

    Proglumide sodium salt is a non-selective cholecystokinin (CCK) antagonist. It inhibits CCK-stimulated amylase secretion and prevents CCK-induced 2-deoxyglucose uptake in mouse pancreatic acini.
  27. adenosine A2B receptors antagonist

    CVT-6883, a selective A2B adenosine antagonist, represents a novel potential approach to treating cardiopulmonary diseases.
  28. dual antagonist of TP/DP2

    BAY-u 3405 is an approved human medication for the treatment of allergic rhinitis that has documented activity as an antagonist of the thromboxane receptor (TP receptor).
  29. Oxytocin antagonist

    PF-3274167 is a high-affinity nonpeptide oxytocin receptor (OTR) antagonist, with Ki of 9.5 nM.
  30. mGluR antagonist

    SIB 1757 is a highly selective antagonist for the mGlu5 metabotropic glutamate receptor subtype.
  31. mGluR antagonist

    SIB 1893 is a highly selective non-competitive antagonist for the metabotropic glutamate mGlu5 receptor subtype.
  32. 5-HT4 Receptor Antagonist

    SDZ 205-557 is a potent, selective 5-HT4 serotonin receptor antagonist.
  33. 5-HT3 receptor antagonist

    Tropanserin acts as a potent and selective 5-HT3 receptor antagonist.
  34. OX1 Antagonist

    ACT-335827 is a selective orexin receptor 1 antagonist.
  35. ETA antagonist

    Atrasentan is an experimental drug that is being studied for the treatment of various types of cancer, including non-small cell lung cancer. It is an endothelin receptor antagonist selective for subtype A (ETA).
  36. mGluR-1 antagonist

    A 841720 is a potent, non-competitive mGluR-1 antagonist that displays 34-fold selectivity over mGluR-5 (IC50 values are 10 and 342 nM respectively).
  37. NK1 receptor antagonist

    GR203040 is a novel, potent and selective non-peptide tachykinin NK1 receptor antagonist.
  38. NPY Y5 receptor antagonist

    GW438014A is a potent and selective neuropeptide Y Y5 receptor antagonist.
  39. α2 adrenergic receptor antagonist

    Atipamezole HCl is a selective α2-adrenergic receptor antagonist (Ki values are 1.1, 1.0, 0.89, 1300 and 6500 nM for α2A, α2B, α2C, α1A and α1B receptors respectively). Has been shown to be a brain penetrant.
  40. A2A receptor antagonist

    Vipadenant, also known as BIIB014, CEB-4520, is a potent, selective and orally available adenosine A2A receptor antagonist under development for Parkinson's disease. Vipadenant demonstrates strong oral activity in commonly used models of Parkinson's disease.
  41. LPA1 receptor antagonist

    AM095 is a potent LPA1 receptor antagonist because it inhibited GTP??S binding to Chinese hamster ovary (CHO) cell membranes overexpressing recombinant human or mouse LPA1 with IC50 values of 0.98 and 0.73 μM, respectively, and exhibited no LPA1 agonism.
  42. I3 receptor Antagonist

    KU14R is an antagonist of the pancreatic β-cell atypical imidazoline binding site (putative I3 receptor). KU14R has also been shown to selectively block efaroxan-induced insulin secretion.
  43. 5-HT6 serotonin receptor antagonist

    SB 258585 hydrochloride has been found to be a selective and potent SR-6 antagonist. This compound displays more than a 160-fold selectivity over other serotonin receptor subtypes.
  44. CRF-1 antagonist

    Emicerfont, also known as GW876008, is a CRF-1 antagonist. Emicerfont blocks the CRH-1 receptor, and so reduces ACTH release.
  45. 5-HT6 receptor antagonist

    SB-742457 is a selective 5-HT6 receptor antagonist with cognition, memory, and learning-enhancing effects.
  46. 5-HT6 antagonist

    SB 399885 hydrochloride is a potent, brain penetrant, and orally active SR-6 antagonist. It displays > 200-fold selectivity for SR-6 over other serotonin receptors (pKi values are 9.11, 8.81 and 9.02 for human recombinant, native rat and native human SR-6 receptors, respectively).

  47. OX2 receptor antagonist

    JNJ-10397049 is a potent, selective, and bioavailable antagonist of the orexin-2 receptor (OX2R) (KB = 4.5 nM for OX2R versus 1.1 μM for OX1R).
  48. CRF1 receptor antagonist

    Pexacerfont is a selective corticotropin-releasing factor (CRF1) receptor antagonist with IC50 of 6.1??0.6 nM for human CRF1 receptor.
  49. angiotensin II receptor antagonist

    BIBS39 is a nonpeptide angiotensin II (AII) receptor antagonists that displaced [125I] AII from its specific binding sites with a K(i) value of 29 +/- 7 nM for the AII subtype I (AT1) receptor and a K(i) value of 480 +/- 110 nM for the AII subtype 2 (AT2) receptor.
  50. LPA1 Receptor antagonist

    AM095 is a novel, potent and orally bioavailable antagonist of lysophosphatidic acid type 1 receptor (LPA1) with IC50 values of 0.73 and 0.98 μM for mouse or recombinant human LPA1, respectively

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