GPCR/G Protein

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  1. GluR inhibitor

    (-)-Huperzine A is a naturally occurring sesquiterpene alkaloid compound found in the firmoss Huperzia serrata.
  2. 5-Hydroxytryptophan (5-HTP) is a naturally occurring amino acid and chemical precursor as well as a metabolic intermediate in the biosynthesis of the neurotransmitters serotonin and melatonin from tryptophan.
  3. Adenosine plays an important role in biochemical processes, such as energy transfer-as adenosine triphosphate (ATP) and adenosine diphosphate (ADP)-as well as in signal transduction as cyclic adenosine monophosphate, cAMP. It is also an inhibitory neurotransmitter.
  4. 5-HT Receptor antagonist

    Agomelatine is a melatonergic agonist (MT1 and MT2 receptors) and 5-HT2C antagonist.
  5. Alfuzosin (provided as the hydrochloride salt) is an α1 receptor antagonist used to treat benign prostatic hyperplasia (BPH). It works by relaxing the muscles in the prostate and bladder neck, making it easier to urinate.
  6. Amfebutamone (Bupropion) is an atypical antidepressant and smoking cessation aid.
  7. Adenosine receptor antagonist

    Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole.
  8. Dopamine Receptor antagonist

    Amisulpride is an atypical antipsychotic used to treat psychosis in schizophrenia and episodes of mania in bipolar disorder.
  9. neurokinin-1 receptor antagonist

    Aprepitant is classified as an NK1 antagonist. Aprepitant has been shown to inhibit both the acute and delayed emesis induced by cytotoxic chemotherapeutic drugs by blocking substance P landing on receptors in the brains neurons. It has also been shown to increase the activity of the 5-HT3 receptor antagonists ondansetron and the corticosteroid dexamethasone, which are also used to prevent nausea and vomiting caused by chemotherapy.

  10. H1 antagonist

    Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.
  11. Azelastine is a potent, second-generation, selective, histamine antagonist (histamine-H1-receptor antagonist).
  12. β1 adrenergic receptor blocker

    Bisoprolol is a drug belonging to the group of beta blockers, a class of drugs used primarily in cardiovascular diseases. More specifically, it is a selective type β1 adrenergic receptor blocker.
  13. Cetirizine is a second-generation antihistamine, a major metabolite of hydroxyzine, and a racemic selective H1 receptor inverse agonist used in the treatment of allergies, hay fever, angioedema, and urticaria.
  14. Chlorpheniramine maleate is a first-generation alkylamine antihistamine used in the prevention of the symptoms of allergic conditions such as rhinitis and urticaria.
  15. Chlorprothixene exerts strong antagonism at the following receptors: 5-HT2; D1, D2, D3; H1;mACh; α1-adrenergic.
  16. H2-receptor antagonist

    Cimetidine is a histamine H2-receptor antagonist that inhibits stomach acid production.
  17. CaSR activator

    AMG-073 HCl (Cinacalcet HCl) represents a new class of compounds for the treatment of hyperparathyroidism known as calcimimetics, which reduce parathyroid hormone (PTH) synthesis and secretion by increasing the sensitivity of the parathyroid calcium-sensing receptor (CaR) to extracellular calcium.
  18. Citalopram is a selective inhibitor of ST (5-hydroxytryptamine/serotonin transporter) and therefore is a potent and selective serotonin reuptake inhibitor.
  19. Histamine Receptor antagonis

    Clemastine is a selective histamine H1 antagonist. It binds to the histamine H1 receptor, thus blocking the action of endogenous histamine, which leads to temporary relief of the negative symptoms caused by histamine.
  20. 5-HT Receptor agonist

    Clomipramine is a blocker of the following transporters:Serotonin transporter (SERT) (Ki = 0.14 nM),Norepinephrine transporter (NET) (Ki = 54 nM),Dopamine transporter (DAT) (Ki = 3,020 nM),Glycine transporter (GlyT/LeuT).
  21. Alpha adrenergic agonist

    Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist.
  22. Clozapine displays a broad range of pharmacological actions; the antipsychotic effects are thought to be mediated principally by 5-HT2A/2C and dopamine receptor blockade.
  23. Dapoxetine works by inhibiting serotonin transporter, increasing serotonins action at the post synaptic cleft, and as a consequence promoting ejaculatory delay.
  24. Dehydroepiandrosterone is an important endogenous steroid hormone.
  25. Adrenergic Receptor agonist

    Detomidine is a sedative with analgesic properties. α2-adrenergic agonists produce dose-dependent sedative and analgesic effects, mediatated by activation of α2 catecholamine receptors, thus inducing a negative feedback response, reducing production of excitatory neurotransmitters.
  26. Adrenoceptors agonist

    Dobutamine is a direct-acting agent whose primary activity results from stimulation of the β1-adrenoceptors of the heart, increasing contractility and cardiac output.
  27. Domperidone blocks the action of dopamine. It has strong affinities for the D2 and D3 dopamine receptors, which are found in the chemoreceptor trigger zone, located just outside the blood brain barrier, which, among others, regulates nausea and vomiting (area postrema on the floor of the fourth ventricle and rhomboid fossa).
  28. Dopamine (abbreviated as DA), a simple organic chemical in the catecholamine family, is a monoamine neurotransmitter - a chemical released by nerve cells to send signals to other nerve cells.
  29. Doxazosin mesylate, a quinazoline compound, is an α1-selective alpha blocker used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).
  30. Adenosine receptor antagonist

    Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor.
  31. S1P Receptor antagonist

    FTY720 is a derivative of ISP-1 (myriocin), a fungal metabolite of the Chinese herb Iscaria sinclarii as well as a structural analog of sphingosine.
  32. PAFR antagonist

    Ginkgolide B (BN 52021) is a PAFR antagonist with IC50 of 3.6 μM.
  33. 5-HT3 receptor antagonist

    Granisetron HCl is a serotonin 5-HT3 receptor antagonist
  34. CYP2D6 inhibitor

    Haloperidol (Haldol) is an antipsychotic and butyrophenone.
  35. AT1 antagonist

    Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
  36. β adrenoceptor agonist

    Isoprenaline or isoproterenol is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.
  37. 5-HT2A serotonin receptor antagonist

    Ketanserin (Vulketan Gel) is specific 5-HT2A serotonin receptor antagonist with a Ki of 2.5 nM for rat and human 5-HT2A.
  38. LPA Receptor Antagonist

    Ki16425 is a LPA receptor antagonist with selectivity for LPA1 and LPA3 and exhibits Ki values of 0.34, 6.5, and 0.93 μM for the human LPA1, LPA2, and LPA3 receptors, respectively.
  39. Smo Antagonist

    LDE225 (NVP-LDE225) is a potent, selective and orally bioavailable Smoothened (SMO) antagonist that inhibits hedgehog (Hh) signaling pathway via antagonism of the Smoothened receptor (SMO).
  40. Loratadine is a non-sedative antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells. Loratadine is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.
  41. mGluR Agonist

    LY-404039 is a drug used in scientific research that acts as a selective agonist for the metabotropic glutamate receptor group II subtypes mGluR2 and mGluR3. It has anxiolytic and antipsychotic effects in animal studies, but without causing sedation. Early human trials using a prodrug form of LY-404,039 called LY-214,0023 have also given encouraging results.
  42. noradrenalin re-uptake inhibitor

    Maprotiline hydrochloride is a selective noradrenalin re-uptake inhibitor.
  43. NOP receptor agonist

    MCOPPB is a compound which acts as a potent and selective agonist for the nociceptin receptor, with a pKi of 10.07.
  44. MT1/MT2 agonist

    Melatonin is a endogenous hormone that acts as an agonist at melatonin receptors MT1 and MT2.
  45. 5-HT2/5-HT1 antagonist

    Mianserin hydrochloride is a 5-HT2/5-HT1 antagonist. Has moderate affinity for 5-ht6 Non-selective 5-HT2 receptor antagonist. Has moderate affinity for 5-HT6. Antidepressant.
  46. CGRP Receptor antagonist

    MK 3207 hydrochloride is a potent CGRP receptor antagonist with IC50 of 0.12 nM.
  47. 5-HT4-receptor agonist

    Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist.
  48. Naftopidil (Flivas) is a selective α1-adrenergic receptor antagonist or alpha blocker with a Ki of 58.3 nM.
  49. 5-HT1A and α1-adrenergic receptor antagonist

    Naftopidil 2HCl is a selective 5-HT1A and α1-adrenergic receptor antagonist with IC50 of 0.1 μM and 0.2 μM, respectively.
  50. 5-HT1 receptor

    Naratriptan is a selective 5-HT1 receptor subtype agonist.

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