GPCR/G Protein

Items 201-250 of 6977

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  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. PAF receptor antagonist

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

    BRL 44408 maleate is a high purity Adrenoceptors antagonist. It increases hippocampal noradrenalin release following systemic administration.
  34. β-adrenergic receptors agonist

    Cimaterol is a potent agonist of β-adrenergic receptors (pEC50 = 8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively).
  35. Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension.
  36. 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.
  37. α2- adrenoceptor antagonist / I2 imidazoline receptor agonist

    Idazoxan hydrochloride is an α2-AR adrenoceptor antagonist and potential I2 imidazoline receptor agonist. Also displays I1 imidazoline receptor antagonist activity. (pKi values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I1, I2, α 2A, α2B, and α 2C receptors respectively).
  38. imidazoline receptor 1 agonist

    Moxonidine hydrochloride is a centrally acting antihypertensive agent.
  39. 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.
  40. Octopamine hydrochloride is an invertebrate biogenic amine neurotransmitter, related to noradrenalin, that is an adrenoceptor agonist.
  41. α-Adrenergic blocker

    Phentolamine Hydrochloride is an AR (α-Adrenergic) blocker.
  42. Beta adrenergic receptor blocker

    Pindolol is a nonselective beta blocker with partial beta-adrenergic receptor agonist activity.
  43. norepinephrine (NE) transporter inhibitor

    Atomoxetine hydrochloride is a competitive and specific inhibitor of SLC6A2 while demonstrating weak ST and DAT inhibition as studied in synaptosomes of rat hypothalamus.
  44. α2-adrenergic receptor antagonist

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

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

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

    SR 59230A hydrochloride is a β3-adrenoceptor antagonist.
  48. Adrenergic Receptor agonist

    Tulobuterol is a beta-adrenergic receptor agonist that is related structurally to Terbutaline.
  49. Adrenoceptors agonist

    UK 14,304 tartrate is a water-soluble form UK 14,304. It is a full α2 adrenergic agonist.
  50. Adrenergic Receptor agonist

    Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR.

Items 201-250 of 6977

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