GPCR/G Protein

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  1. Chlorprothixene exerts strong antagonism at the following receptors: 5-HT2; D1, D2, D3; H1;mACh; α1-adrenergic.
  2. 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.
  3. Citalopram is a selective inhibitor of ST (5-hydroxytryptamine/serotonin transporter) and therefore is a potent and selective serotonin reuptake inhibitor.
  4. 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.
  5. 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).
  6. Alpha adrenergic agonist

    Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist.
  7. Dapoxetine works by inhibiting serotonin transporter, increasing serotonins action at the post synaptic cleft, and as a consequence promoting ejaculatory delay.
  8. Dehydroepiandrosterone is an important endogenous steroid hormone.
  9. 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.
  10. 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.
  11. 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.
  12. Adenosine receptor antagonist

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

    Ginkgolide B (BN 52021) is a PAFR antagonist with IC50 of 3.6 μM.
  14. 5-HT3 receptor antagonist

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

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

    Irbesartan is an angiotensin II receptor antagonist used mainly for the treatment of hypertension.
  17. 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.
  18. 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.
  19. 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.
  20. noradrenalin re-uptake inhibitor

    Maprotiline hydrochloride is a selective noradrenalin re-uptake inhibitor.
  21. 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.
  22. MT1/MT2 agonist

    Melatonin is a endogenous hormone that acts as an agonist at melatonin receptors MT1 and MT2.
  23. 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.
  24. 5-HT4-receptor agonist

    Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist.
  25. Naftopidil (Flivas) is a selective α1-adrenergic receptor antagonist or alpha blocker with a Ki of 58.3 nM.
  26. 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.
  27. 5-HT1 receptor

    Naratriptan is a selective 5-HT1 receptor subtype agonist.
  28. dopamine beta-hydroxylase inhibitor

    Nepicastat is an inhibitor of dopamine beta-hydroxylase, an enzyme that catalyzes the conversion of dopamine to norepinephrine.
  29. 5-HT Receptors/D2 dopamine receptor antagonist

    Olanzapine(Zyprexa) is a high affinity for 5-HT2 serotonin and D2 dopamine receptor antagonist.
  30. Olopatadine hydrochloride is a dual acting histamine H1-receptor antagonist and mast cell stabilizer
  31. 5-HT Receptors antagonist

    Ondansetron is a serotonin 5-HT3 receptor antagonist used mainly as an antiemetic to treat nausea and vomiting, often following chemotherapy.
  32. alpha-1 adrenergic agonist

    Oxymetazoline is a selective alpha-1 agonist and partial alpha-2 agonist topical decongestant, used in the form of Oxymetazoline hydrochloride.
  33. α-adrenergic (AR) antagonist/CaM inhibitor

    Phenoxybenzamine is a cell-permeable, non-specific, irreversible α-adrenergic (AR) antagonist that also acts as an CaM inhibitor.
  34. Dopamine Receptor Agonist

    Pramipexole is a dopamine agonist of the non-ergoline class indicated for treating early-stage Parkinson's disease (PD) and restless legs syndrome (RLS).
  35. MT1/MT2-Receptor Agonist

    Ramelteon is a melatonin receptor agonist with both high affinity for melatonin MT1 (IC50 =28.5 ?? 8.55 pM)and MT2 (20.1 ?? 9.25 pM)receptors and selectivity over the MT3 receptor.
  36. α2 adrenergic agonist

    Rilmenidine is a second-generation imidazoline-α2 adrenergic agonist.
  37. Adrenergic Receptor agonist

    Salbutamol sulfate (Albuterol) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease.
  38. α1-adrenoceptor antagonist

    Silodosin(Rapaflo) is an α1-adrenoceptor antagonist with high uroselectivity. It causes practically no orthostatic hypotension (in contrast to other α1 blockers).
  39. DDP-4 inhibitor

    Sitagliptin phosphate is an anti-diabetic (antihyperglycemic) drug of the dipeptidyl peptidase-4 (DPP-4) class. Inhibition of the enzyme DPP-4 is thought to increase Glucagon-like peptide-1 (GLP-1) which inhibits glucagon release , stimulates the insulin release and lowers blood glucose.
  40. Adrenergic Receptor agonist

    Synephrine (Oxedrine) is an amine compound commonly used for weight loss.
  41. Angiotensin II receptor antagonist

    Tasosartan is an angiotensin II receptor antagonist.
  42. Tetrabenazine is a drug for the symptomatic treatment of hyperkinetic movement disorder.
  43. mast cell stabilizer

    Nedocromil is a medication considered as mast cell stabilizer which act to prevent wheezing, shortness of breath, and other breathing problems caused by asthma. It is administered by an inhaler under the brand name Tilade.
  44. D2 dopamine agonist

    U-95666E is a D2 selective dopamine agonist with an ED50 of about 46 nM, was investigated for its effect on rat striatal acetylcholine (ACh) concentration
  45. angiotensin II receptor antagonist

    Valsartan (CGP-48933) is an angiotensin II receptor antagonist for the treatment of high blood pressure and heart failure.
  46. LTD4 receptor antagonist

    Zafirlukast is a potent orally active leukotriene D4 (LTD4) receptor antagonist.
  47. 5-HT (serotonin) and dopamine receptor antagonist

    Ziprasidone hydrochloride monohydrate (CP 88059 hydrochloride monohydrate) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity.
  48. SMO Antagonist

    LY2940680 has been shown to affect a cancer cell signaling pathway initiated by the Hedgehog (Hh) protein.
  49. neurokinin-1 receptor antagonist

    Fosaprepitant is a selective neurokinin-1 (NK-1) receptor antagonist.
  50. Opioid Receptor agonist

    ADL5859 HCl is a highly potent and selective δ opioid receptor agonist with Ki value to be 0.84 nM and ED50 value to be 20 nM.

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