GPCR/G Protein

Items 301-350 of 6977

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  1. Trazodone is an antidepressant of the serotonin antagonist and reuptake inhibitor (SARI) class. It is a phenylpiperazine compound. Trazodone also has anti-anxiety (anxiolytic) and sleep-inducing (hypnotic) effects.
  2. Urapidil hydrochloride is an α1-adrenoceptor antagonist, 5-HT1A serotonin receptor partial agonist and anti-hypertensive.
  3. histamine receptor antagonist

    Cyproheptadine hydrochloride is a histamine receptor antagonist for 5-HT2 receptor with IC50 of 0.6 nM.
  4. NMDA receptor antagonist

    Orphenadrine citrate is a NMDA receptor antagonist with Ki of 6.0 +/- 0.7 μM, HERG potassium channel blocker.
  5. Beta1 receptor blocker

    Metoprolol is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.
  6. H2 receptor antagonist

    Lafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action.
  7. Duloxetine Hydrochloride is a dual serotonin and norepinephrine reuptake inhibitor (SNRI) that is used in the treatment of stress urinary incontinence, as well as depression.
  8. Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects.
  9. Fenoldopam is used as an antihypertensive agent postoperatively, and also intravenously (IV) to treat a hypertensive crisis.
  10. Betaxolol is a selective beta1 receptor blocker used in the treatment of hypertension and glaucoma. Being selective for beta1 receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta2 receptors) as timolol may. Betaxolol also shows greater affininty for beta1 receptors than metoprolol.
  11. Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H1 receptors.
  12. Formoterol is a long-acting β2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD).
  13. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.
  14. Phentolamine is a reversible nonselective alpha-adrenergic antagonist.
  15. Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of an enlarged prostate (BPH).
  16. Thromboxane A2 synthesis inhibitor

    Ozagrel is an antiplatelet agent working as a thromboxane A2 synthesis inhibitor.
  17. 5-HT antagonist

    Tegaserod functions as a motility stimulant, achieving its desired therapeutic effects through activation of the 5-HT4 receptors of the enteric nervous system in the gastrointestinal tract. It also stimulates gastrointestinal motility and the peristaltic reflex, and allegedly reduces abdominal pain. Additionally, tegaserod is a 5-HT2B receptor antagonist.
  18. mGluR5 PAM

    VU 0357121 is a positive allosteric modulator (PAM) of the metabotropic glutamate receptor 5 (mGlu5) with EC50 = 33 nM, 92% Glumax.
  19. neurokinin-1 receptor antagonist

    Fosaprepitant (MK-0517, L-758,298) is a water-soluble phosphoryl prodrug for Aprepitant which is a NK1 antagonist.
  20. Prostaglandin D2 receptor CRTH2 antagonist

    CAY10471 Racemate (TM30089 Racemate) is a potent and highly selective prostaglandin D2 receptor CRTH2 antagonist.
  21. CCK-A receptor antagonist

    Loxiglumide (CR1505) is a cholecystokinin antagonist
  22. NT Antagonist

    SR 48692 represents a new, potent, nonpeptide antagonist radioligand of the NT receptor that differentiates between agonist- and antagonist-receptor interactions.
  23. AT1 Receptor Blocker

    Azilsartan (TAK-536) is an angiotensin II receptor antagonist used in the treatment of hypertension.
  24. CB2 agonist

    JWH-133 is a potent selective CB2 receptor agonist, with a Ki of 3.4nM and selectivity of around 200x for CB2 over CB1 receptors.
  25. beta2-adrenergic receptor agonist

    Salmeterol is a long-acting beta2-adrenergic receptor agonist
  26. PGF2α/LTB4 production inhibitor

    Darbufelone mesylate (CI-1004 mesylate) is a dual inhibitor of cellular PGF2α and LTB4 production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 μM) but is much less potent with PGHS-1 (IC50= 20 μM).
  27. adrenergic agonist

    Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors.
  28. D2/5-HT2 receptor antagonist

    Blonanserin is a D2/5-HT2 receptor antagonist; atypical antipsychotic.
  29. β2-adrenergic receptor

    Carvedilol is a β1- and β2-adrenergic receptor (AR) agonist with antioxidant properties.
  30. alpha2-adrenoceptor agonist

    Dexmedetomidine hydrochloride is the active isomer of medetomide which acts a potent, highly selective alpha2-AR (alpha2-adrenoceptor) agonist.
  31. COX inhibitor/histamine H1 receptor agonist

    Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist
  32. Lamotrigine is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker.
  33. Prostaglandin Receptor Agonist

    Prostaglandin E2 is a hormone-like substance that participate in a wide range of body functions such as the contraction and relaxation of smooth muscle, the dilation and constriction of blood vessels, control of blood pressure, and modulation of inflammation.
  34. Procaterol is a short-acting β2-adrenergic receptor agonist with Kp of 8 nM, used for the treatment of asthma
  35. Leukotriene receptor antagonist

    Pranlukast is a selective cysteinyl leukotriene receptor antagonist.
  36. Ropinirole a selective dopamine D2 receptors inhibitor with IC5N/A of 29 nM.
  37. Ropinirole Hydrochloride is a dopamine receptor agonist.
  38. Roxatidine Acetate Hydrochloride is a histamine H2-receptor antagonist used in ulcer treatment. This compound has been found to inhibit platelet function in vitro.
  39. 5-HT7 receptor antagonist

    SB269970 is a potent and selective 5-HT7 receptor antagonist.
  40. CB2 receptor ligand

    BML-190 is a selective inverse agonist of the human cannabinoid CB2 receptor.
  41. CB2 agonist

    MDA 19 is a potent and selective agonist for the cannabinoid receptor CB2, with reasonable selectivity over the psychoactive CB1 receptor.
  42. CB1 antagonist

    CP 945598 is a potent and highly selective CB1 antagonist.
  43. CRTH2 antagonist

    OC 000459 is a potent, oral and selective CRTH2 (also known as DP2) antagonist.
  44. GPR40 Inhibitor

    GW 9508 is a cell-permeable aminophenylpropanoate that acts as a potent and selective agonist for the G-protein coupled receptor (GPCR) GRP40/FFA1 receptor (EC50 ?50 nM) with reduced activity towards family members GRP120 (EC50 ?3.5 μM), GRP41/GRP43 (EC50 >50 μM), as well as a panel of eight other free fatty acid (FFA) and prostaglandin receptors.
  45. LPA Receptor antagonist

    Ki16198 is a potent LPA receptor antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively.
  46. CTEP is a highly potent, selective and orally bioavailable allosteric antagonist of mGlu5 receptor with an IC50 of 2.2 nM.
  47. AR antagonist

    Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects.
  48. Rotundine (L-tetrahydropalmatine, L-THP) is a selective dopamine D1 receptor antagonist with IC50 of 166 nM.
  49. mGlu4 receptors modulator

    VU 0364770 is a positive allosteric modulator at mGlu4 receptors with EC50 value of 290 nM in mGlu4-expressing HEK 293 cells.

Items 301-350 of 6977

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