GPCR/G Protein

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  1. mGlu2 agonist

    LY2979165 is a mGlu2 agonist.
  2. CysLT1 receptor antagonist

    Montelukast (sodium) (MK0476) is a potent, selective CysLT1 receptor antagonist.
  3. Endothelin receptor antagonist

    Macitentan is an orally active, non-peptide dual endothelin ETA and ETB receptor antagonist for the potential treatment of idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).
  4. α2-adrenoceptor agonist

    Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively).
  5. GCGR inhibitor

    MK 0893 is glucagon receptor antagonist as antidiabetic agents.
  6. EP4 receptor antagonist

    MK-2894 is a highly potent and selective second generation EP4 antagonist.
  7. EP4 antagonist

    MK-2894 sodium salt is a highly potent and selective second generation EP4 antagonist.
  8. CaSR antagonist

    NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist.
  9. CGRP1 receptor

    Olcegepant is a potent and selective non-peptide antagonist of the calcitonin gene-related peptide 1 (CGRP1) receptor with IC50 of 0.03 nM and Ki of 14.4 pM for human CGRP.
  10. CB1 modulator?€?

    Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24).
  11. EP4 antagonist

    ONO-AE3-208 is an EP4 antagonist, and suppresses cell invasion, migration, and metastasis of prostate cancer.
  12. nonimidazole inverse agonist

    Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
  13. Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
  14. CB1 receptor inverse agonist

    Rimonabant hydrochloride is a CB1 receptor inverse agonist.
  15. sGC stimulator

    Riociguat (BAY 63-2521; BAY 632521) is a stimulator of soluble guanylate cyclase (sGC).
  16. Dopamine agonist

    Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.
  17. dopamine D3 receptor antagonist

    SB-277011 is a drug which acts as a potent and selective dopamine D3 receptor antagonist which is around 80-100x selective for D3 over D2 and lacks any partial agonist activity.
  18. A2a receptor antagonist

    SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders.
  19. ETA receptor antagonist

    Sitaxentan sodium (TBC-11251) is a selective endothelin receptor-A antagonist with IC50 and Ki of 1.4 nM and 0.43 nM, respectively.
  20. ETA receptor antagonist

    Sitaxsentan (IPI 1040; TBC-11251) is a selective endothelin A (ETA) receptor antagonist. Antihypertensive. Sitaxsentan is used in treatment of chronic heart failure.
  21. OX Receptor Antagonist

    SB-408124 is a selective non-peptide orexin OX1 receptor antagonist (Kb values are 21.7 and 1405 nM for human OX1 and OX2 receptors respectively). Blocks orexin-A induced grooming following oral administration in vivo.
  22. Dopamine receptor ligand

    ST-836 is a dopamine receptor ligand; Antiparkinsonian agent.
  23. 5-HT6 receptor antagonist

    SB271046 Hydrochloride is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 8.9.
  24. SIRT1 activator

    SRT3190 is a potent CXCR2 ligand.
  25. CB1 receptor inverse agonist

    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
  26. vasopressin receptor 2 antagonist

    Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28μM.
  27. serotonin transporter (SER) inhibitor

    Vilazodone Hydrochloride (EMD 68843 Hydrochloride) is a serotonin transporter (SER) inhibitor and 5-HT1A receptor partial agonist.
  28. LTD4 receptor antagonist

    Verlukast (MK-0679) is a potent leukotriene D4 antagonist
  29. DL-Adrenaline is a hormone and a neurotransmitter secreted by the medulla of the adrenal glands. DL-Adrenaline is found in small amounts in the body and is essential for maintaining cardiovascular homeostasis because of its ability to divert blood to tissues under stress.
  30. Noradrenaline bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.
  31. CaSR agonist

    Strontium ranelate is an antiosteoporotic agent which both increases bone formation and reduces bone resorption, resulting in a rebalance of bone turnover in favor of bone formation. This is similar to the effects of choline stabilized orthosilicic acid.
  32. Brompheniramine maleate is a first-generation antihistamine. Brompheniramine works by acting as an antagonist of histamine H1 receptors. It also functions as a moderately effective anticholinergic agent, and is likely an antimuscarinic agent similar to other common antihistamines such as diphenhydramine.

  33. Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic (to treat nausea and vomiting). Ondansetron reduces the activity of the vagus nerve, which deactivates the vomiting center in the medulla oblongata, and also blocks serotonin receptors in the chemoreceptor trigger zone.
  34. Mirtazapine is a noradrenergic and specific serotonergic antidepressant (NaSSA) . Structurally, mirtazapine can also be classified as a tetracyclic antidepressant (TeCA).
  35. 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.
  36. Urapidil hydrochloride is an α1-adrenoceptor antagonist, 5-HT1A serotonin receptor partial agonist and anti-hypertensive.
  37. histamine receptor antagonist

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

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

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

    Lafutidine is a second generation H2 receptor antagonist having multimodal mechanism of action.
  41. 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.
  42. Trimebutine is a drug with antimuscarinic and weak mu opioid agonist effects.
  43. Fenoldopam is used as an antihypertensive agent postoperatively, and also intravenously (IV) to treat a hypertensive crisis.
  44. 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.
  45. Mizolastine is a second generation antihistamine agent with high affinity and specificity for histamine H1 receptors.
  46. Formoterol is a long-acting β2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD).
  47. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.
  48. Phentolamine is a reversible nonselective alpha-adrenergic antagonist.
  49. Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of an enlarged prostate (BPH).

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