GPCR/G Protein

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  1. antihistamine

    Diphenylpyraline hydrochloride is a first-generation antihistamine with anticholinergic effects of the diphenylpiperidine class.
  2. alpha-adrenergic blocking agent

    Moxisylyte hydrochloride is an alpha-adrenergic blocking agent that is used in Raynaud's disease. It is also used locally in the eye to reverse the mydriasis caused by phenylephrine and other sympathomimetic agents.
  3. 5-HT3 receptor antagonist

    Dolasetron mesylate is a selective 5-HT3 receptor antagonist.
  4. Histamine 1 receptor antagonist

    Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.
  5. hemagglutinin (HA)-receptor antagonist

    Alimemazine hemitartrate is a phenothiazine derivative that is generally used as an antipruritic agent and also a hemagglutinin (HA)-receptor antagonist.
  6. Adrenergic alpha-1 agonist

    Midodrine hydrochloride is an ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of hypotension. It improves clinical outcome of chronic hypotension.
  7. adrenergic alpha-1 agonist

    Midodrine is an ethanolamine derivative that is an adrenergic alpha-1 agonist. It is used as a vasoconstrictor agent in the treatment of HYPOTENSION.
  8. Serotonin receptors agonist

    Dihydroergotamine Mesylate, also known as DHE or Migranal, is an ergot alkaloid used to treat migraines. It has similar actions to the triptans, acting as an agonist to the serotonin receptors and causing vasoconstriction of the intracranial blood vessels, but also interacts centrally with dopamine and adrenergic receptors.
  9. Beta 2 adrenergic agonist

    Fenoterol is a Beta 2 adrenergic agonist designed to open up the airways to the lungs. It is classed as sympathomimetic beta agonist and asthma medication.
  10. β-adrenergic blocker

    Esmolol is a short acting hyperselective β-adrenergic blocker effective in blunting adrenergic response to several perioperative stimuli and so it might interfere in the effect of the anesthetic drugs on the brain.
  11. α-1 adrenergic receptor blocker

    Doxazosin is an α-1 adrenergic receptor blocker that inhibits the binding of norepinephrine, which is released from sympathetic nerve terminals, to the α-1 receptors on the membrane of vascular smooth muscle cells. Blockages of the alpha-1 adrenergic action on the vascular smooth muscles lead to a decrease in vascular resistance and antihypertensive activity.
  12. LTR antagonist

    Montelukast (trade name Singulair) is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies.
  13. 5-HT1A receptor antagonist

    Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
  14. Tranilast is an inhibitor of the production of interleukin-6 in endothelial cells. It acts by reducing collagen synthesis in fibroblasts and inhibiting growth of neurofibroma cells.
  15. S1P antagonist

    Fingolimod is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.
  16. Serotonergic receptor antagonist

    (Z)-Thiothixene is an antagonist of serotonergic receptor extracted from patent US 20150141345 A1.
  17. α2-adrenergic receptor agonist

    Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
  18. Glucagon is a peptide hormone, produced by alpha cells of the pancreas. It works to raise the concentration of glucose in the bloodstream. Its effect is opposite that of insulin, which lowers the glucose.
  19. beta-adrenergic agonist

    Nylidrin hydrochloride is a beta-adrenergic agonist. Nylidrin hydrochloride is shown to be an effective inhibitor of IgE-mediated release of histamine from human basophils, and thus can be used as antiallergic agent.
  20. Lodoxamide Tromethamide is a mast-cell stabilizer, inhibiting type I immediate hypersensitivity reaction by preventing the antigen-stimulated calcium influx into mast cells and the release of slow-reacting substances of anaphylaxis (SRS-A).
  21. oxytocin receptor ligand

    Oxytocin (α-Hypophamine) is a mammalian neurohypophysial hormone; its actions are mediated by specific, high-affinity oxytocin receptors; ligand of oxytocin receptor.
  22. vasoconstrictor

    Terlipressin is a potent vasoconstrictor that acts via V1 receptors on arteriolar smooth muscle cells.
  23. Angiotensin II human is a vasoconstrictor that acts on the AT1 and the AT2 receptor.
  24. histamine H1-receptor antagonist

    Diazoline is a histamine H1-receptor antagonist.
  25. adrenergic receptor inhibitor

    Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
  26. histamine H1 antagonist

    Chlorcyclizine hydrochloride is a histamine H1 antagonist.
  27. dopamine D2 receptor agonist

    Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor.
  28. β-adrenergic receptor antagonist

    Metipranolol (hydrochloride) is a non-selective β-adrenergic receptor (β-AR) antagonist. Formulations containing metipranolol have been used in the treatment of elevated IOP in patients with ocular hypertension or glaucoma.
  29. Dopamine D2 antagonist

    Metoclopramide hydrochloride hydrate is a dopamine D2 antagonist that is used as an antiemetic.
  30. D2DR/D4DR inhibitor

    Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent.
  31. Bradykinin B2 receptors antagonist

    Icatibant (HOE-140) is a selective and specific antagonist of bradykinin B2 receptor with IC50 and Ki of 1.07 nM and 0.798 nM respectively.
  32. peripheral oxytocin receptors agonist

    Carbetocin (Lonactene; Duratocin) is an obstetric drug used to control postpartum hemorrhage and bleeding after giving birth; an agonist at peripheral oxytocin receptors.
  33. 5-HT receptor antagonist

    Pizotifen is a serotonin antagonist which acts mainly at the 5-HT1, 5-HT2A, and 5HT2C receptors with some antihistamine activity.
  34. DOPA decarboxylase inhibitor

    Methyldopa Sesquihydrate is a DOPA decarboxylase inhibitor and indirect α2-adrenergic receptor agonist used to treat hypertension.
  35. μ- opioid receptor agonist

    Trimebutine Maleate is a drug with antimuscarinic and weak mu opioid agonist effects. Trimebutine Maleate modulates the calcium and potassium channels, relieves abdominal pain in patients with irritable bowel syndrome.
  36. thromboxane A2 (TXA2) receptor (TP receptor) antagonist

    Seratrodast is a thromboxane A2 (TXA2) receptor (TP receptor) antagonist used primarily in the treatment of asthma.
  37. α2-receptor agonist

    Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.
  38. CCK antagonist

    Proglumide is a drug that exerts an inhibitory effect on gastric secretion and reduces gastrointestinal motility. IProglumide is a known cholecystokinin (CCK) antagonist.
  39. sigma-2 (σ2) receptor ligand

    Glycerol phenylbutyrate is a sigma-2 (ς2) receptor ligand, with a pKi of 8.02.
  40. Histamine H1 antagonist

    Mequitazine is a potent histamine H1 antagonist or antihistamine. It competes with histamine for the normal H1-receptor sites on effector cells of the gastrointestinal tract, blood vessels and respiratory tract.
  41. alpha-1 adrenergic receptors / mAChRs inhibitor

    Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
  42. Sodium deoxycholate is a bile acid formed by bacterial action from cholate. It is usually conjugated with glycine or taurine. Deoxycholic acid acts as a detergent to solubilize fats for intestinal absorption, is reabsorbed itself, and is used as a choleretic and detergent.
  43. β2-adrenergic receptor agonist

    Tulobuterol Hydrochloride is a long-acting beta2-adrenergic receptor agonist.
  44. Somatostatin Receptor agonist

    Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).
  45. Bromperidol, also known as Impromen and R-11333, is used as a means of long-term maintenance treatment of schizophrenia. Bromperidol is a close structural analogue of haloperidol. C3435T polymorphism is associated with some therapeutic response to bromperidol in schizophrenic patients, possibly by different drug concentration in the brain.
  46. 5-HT receptor /dopamine receptors antagonist

    Metergoline is a psychoactive drug of the ergoline chemical class which acts as a ligand for various serotonin and dopamine receptors.
  47. β-adrenergic receptor antagonist

    Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity.
  48. Levomepromazine, also known as methotrimeprazine, is a phenothiazine neuroleptic drug. Levomepromazine is used for the treatment of psychosis, particularly those of schizophrenia, and manic phases of bipolar disorder.
  49. Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3, and 5, increases Gi activity, and reduces intracellular cAMP production.
  50. Sincalide, also known as CCK-8, is a drug used to treat cholecystitis. Sincalide is an octapeptide hormone present in the intestine and brain. When secreted from the gastric mucosa, it stimulates the release of bile from the gallbladder and digestive enzymes from the pancreas.

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