GPCR/G Protein

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  1. 5-HT3 receptor antagonist

    Ondansetron hydrochloride is a serotonin 5-HT3 receptor antagonist.
  2. α1A-adrenoceptor antagonist

    Nicergoline is an ergot derivative used to treat senile dementia and other disorders with vascular origins. It has been found to increase mental agility and enhance clarity and perception. It decreases vascular resistance and increases arterial blood flow in the brain, improving the utilization of oxygen and glucose by brain cells. It has similar vasoactive properties in other areas of the body, particularly the lungs. Nicergoline is used for vascular disorders such as cerebral thrombosis and atherosclerosis, arterial blockages in the limbs, Raynaud's disease, vascular migraines, and retinopathy.
  3. Histamine H1 receptor antagonist

    Levocetirizine dihydrochloride is a L-isomer of cetirizine and histamine H1 receptor antagonist. It incrases levels of CD4+ CD25+ T cells and decreases levels of eosinophils, decreasing allergy symptoms.
  4. prostaglandin analogue

    Tafluprost, also known as MK2452 and AFP-168, is a prostaglandin analogue used topically (as eye drops) to control the progression of glaucoma and in the management of ocular hypertension.
  5. non-peptide angiotensin II receptor antagonist

    Fimasartan is a non-peptide angiotensin II receptor antagonist (ARB) used for the treatment of hypertension and heart failure. Through oral administration, fimasartan blocks angiotensin II receptor type 1 (AT1 receptors), reducing pro-hypertensive actions of angiotensin II, such as systemic vasoconstriction and water retention by the kidneys.
  6. beta Adrenergic Receptor blocker

    Nadolol is a non-selective beta blocker used in the treatment of high blood pressure and chest pain. Additionally, it is often prescribed in the treatment of atrial fibrillation, migraine headaches, and complications of cirrhosis.
  7. Dopamine D1/2 receptor antagonist

    Melitracen HCl ia potential dopamine D1/2 receptor antagonist used to treat depression. It is often co-administered with flupenthixol as a treatment for trigeminal neuralgia. It does not effect cardiovascular function.
  8. Prostaglandin Receptor inhibitor

    Benorilate, also known as Win-11450, is an ester of aspirin and paracetamol with analgesic, antipyretic, and anti-inflammatory activity used in the treatment of rheumatoid diseases. Benorilate has less severe side effects than aspirin.
  9. Prostaglandin Receptor inhibitor

    Dinoprost Tromethamine, also known as Dinoprost Trometamol, is a naturally occurring prostaglandin used in medicine to induce labor and as an abortifacient.
  10. Angiotensin II receptor antagonist

    Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
  11. Carbazochrome, also known as Adona and AC-17, is a hemostatic which increases capillary resistance and activates platelet factors.
  12. serotonin uptake inhibitor

    Paroxetine Mesylate is a serotonin uptake inhibitor that is effective in the treatment of depression.
  13. 5-HT3 receptor antagonist

    Dolasetron is a serotonin 5-HT3 receptor antagonist used to treat nausea and vomiting following chemotherapy. Its main effect is to reduce the activity of the vagus nerve, which is a nerve that activates the vomiting center in the medulla oblongata. It does not have much antiemetic effect when symptoms are due to motion sickness.
  14. 5-HT2 receptors inhibitor

    Nefazodone HCl is an inhibitor of 5-HT2 receptors, SERT, NET, and hERG K+ channels used to treat mood disorders. It decreases immobility time in the forced swim test.
  15. D2DR inhibitor

    Promazine Hydrochloride is a phenothiazine compound and D2DR inhibitor. Promazine Hydrochloride has been employed in studies investigating dopamine-stimulated glycosylation of brain proteins in vitro. It has actions similar to chlorpromazine but with less antipsychotic activity.
  16. MAO inhibitor

    Molindone HCl is a D2 dopamine receptor antagonist. It also acts as a MAO inhibitor.
  17. D2 receptor blocker

    Trimethobenzamide hydrochloride is a blocker of the D2 receptor. Trimethobenzamide is an antiemetic used to prevent nausea and vomiting.
  18. adrenoceptor antagonist

    Landiolol hydrochloride (ONO1101 hydrochloride) is a highly beta1 selective ultra-short acting beta-blocker (β1/β2 selectivity?=?255:1, a half-life of 4?min)?? acts as an adrenoceptor antagonist.
  19. histamine H1 receptor antagonist

    Emedastine Difumarate is the difumarate salt form of emedastine, a second generation, selective histamine H1 receptor antagonist with anti-allergic activity. This medication is an antihistamine, prescribed for allergic conjunctivitis.
  20. Histamine H1 receptor antagonist

    Hydroxyzine pamoate is an histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness.
  21. antihistamine

    Diphenylpyraline hydrochloride is a first-generation antihistamine with anticholinergic effects of the diphenylpiperidine class.
  22. Histamine H2-receptor antagonist

    Ranitidine is a potent, selective and orally active histamine H2-receptor antagonist with an IC50 of 3.3 μM that inhibits gastric secretion.
  23. 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.
  24. 5-HT3 receptor antagonist

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

    Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.
  26. 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.
  27. 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.
  28. 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.
  29. 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.
  30. 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.
  31. 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.
  32. 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.
  33. 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.
  34. 5-HT1A receptor antagonist

    Alprenolol (hydrochloride) is a non-selective beta blocker as well as 5-HT1A receptor antagonist.
  35. 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.
  36. 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.
  37. Serotonergic receptor antagonist

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

    Brimonidine (UK 14304) is a full α2-adrenergic receptor (α2-AR) agonist.
  39. 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.
  40. 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.
  41. 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).
  42. 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.
  43. vasoconstrictor

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

    Diazoline is a histamine H1-receptor antagonist.
  46. 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.
  47. histamine H1 antagonist

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

    Quinagolide hydrochloride is a selective dopamine D2 receptor agonist, also is a prolactin inhibitor.
  49. 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.
  50. Dopamine D2 antagonist

    Metoclopramide hydrochloride hydrate is a dopamine D2 antagonist that is used as an antiemetic.

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