GPCR/G Protein

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  1. CB2 agonist

    Olorinab (APD 371) is a highly potent, selective and fully efficacious cannabinoid receptor type 2 (CB2) agonist, with an EC50 of 6.2 nM for hCB2.
  2. β2-adrenoceptor agonist

    Formoterol is a long-acting β2 agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD).
  3. μ-opioid receptor agonist

    Alvimopan dihydrate(LY 246736, ADL 8-2698) is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  4. μ-opioid receptor agonist

    Alvimopan monohydrate is a peripherally acting mu-opioid receptor (PAM-OR, IC50= 1.7 nM) antagonist for accelerating gastrointestinal recovery after surgery.
  5. α-adrenergic receptor agonist

    Brimonidine Tartrate is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension.
  6. dopamine agonist

    Dexpramipexole dihydrochloride is a neuroprotective agent and weak non-ergoline dopamine agonist.
  7. α2A-adrenoceptor agonist

    Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.
  8. 5HT1F agonist

    LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor.
  9. Nonimidazole inverse agonist

    Pitolisant hydrochloride is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
  10. Nonimidazole inverse agonist

    Pitolisant oxalate is a novel, potent, and selective nonimidazole inverse agonist at the recombinant human H3 receptor (Ki=0.16 nM).
  11. D2 receptor agonist

    rac-Rotigotine Hydrochloride is a high potency and selectivity agonist for D-2 receptor with Ki of 0.69 nM.
  12. LPA2 agonist

    GRI 977143, selective lysophosphatidic acid 2 (LPA2) receptor non-lipid agonist (EC50 = 3.3 uM).
  13. glutamate receptors agonist

    (S)-Glutamic acid acts as an excitatory transmitter and an agonist at all subtypes of glutamate receptors (metabotropic, kainate, NMDA, and AMPA).
  14. 5-HT1E/5-HT1F receptor agonist

    BRL 54443 is a 5-HT1E and 5-HT1F receptor agonist with pKi of 8.7 and 9.25, respectively, with a weak binding affinity for 5-HT1A, 5-HT1B, 5-HT1D receptors.
  15. Orexin 2 receptor agonist

    A potent and selective Orexin2 receptor agonist.
  16. β2-adrenergic receptor agonist

    Vilanterol is a long-acting beta-2 agonist drug, which in May 2013 was approved in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD).
  17. Adenosine A Receptor agonist

    2-Chloroadenosine is a metabolically stable analog of adenosine that behaves as an Adenosine A Receptor agonist (Ki values are 300, 80 and 1900 nM for Adenosine A1-R, Adenosine A2A-R and Adenosine A3-R, respectively).
  18. mGluR agonist

    (S)-3,5-DHPG is an agonist of the group I metabotropic glutamate receptors (mGluRs), binding both mGluR1a and mGluR5a (Ki = 0.9 and 3.9 uM, respectively) but not ionotropic glutamate receptors.
  19. GLP-1 receptor agonist

    Liraglutide is a long-acting glucagon-like peptide-1(GLP-1) receptor agonist.
  20. Histamine H1-receptor agonist

    Lidocaine hydrochloride is a local anesthetic and cardiac depressant used as an antiarrhythmia agent.
  21. REV-ERBα/β agonist

    SR9011 is the agonist for REV-ERB-α with IC50 of 670 nM and REV-ERB-β with IC50 of 800 nM.
  22. CB1/CB2 receptor agonist

    Bay 59-3074 is a novel, selective CB1/CB2 receptor partial agonist with Ki values of 48.3 and 45.5 nM at human CB1 and CB2 receptors respectively .
  23. CXCR4 agonist

    ATI-2341, pepducin targeting the C-X-C chemokine receptor type 4 (CXCR4) (EC50 = 194 nM, is an allosteric agonist activating the inhibitory heterotrimeric G protein (Gi) to promote inhibition of cAMP production and induce calcium mobilization.
  24. CB2 receptor agonist

    AM1241 is a selective cannabinoid CB2 receptor agonist with Ki of 3.4 nM, exhibits 82-fold selectivity over CB1 receptor.
  25. Adenosine A2 receptor agonist

    CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.
  26. β2-adrenergic receptor agonist

    Clorprenaline HCl is a β2-receptor agonist, it has a significant expansion of the bronchial effect.
  27. GPR35/CXCR8 agonist

    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
  28. β-adrenoceptor agonist

    Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist.
  29. β3-AR agonist

    L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM.
  30. adenosine A2B receptor agonist

    MRS1706 is a selective adenosine A2B receptor inverse agonist with Ki values of 1.39, 157, 112, and 230 nM for human A2B, A1, A2A, and A3 receptors, respectively.
  31. Endogenous galanin receptor agonist

    Galanin (1-30) (human) is an endogenous peptide with multiple endocrine, metabolic and behavioral effects
  32. 5-HT7 receptor agonist

    LP-211 is a a selective agonist of the serotonin 5-HT7 receptor with a Ki value of 0.58 nM at rat cloned 5-HT7 receptors, and >300-fold selectivity over the 5-HT1A receptor.
  33. KOR agonist

    Asimadoline is a potent κ-opioid receptor (KOR) agonist (IC50s = 5.6 and 1.2 nM for guinea pig and human receptors, respectively).
  34. NK3 receptor agonist

    Senktide is a potent, selective agonist of the neuromedin K3 (NK3) receptor (EC50 = 0.5-3 nM).
  35. Adenosine receptor agonist

    NECA is a high-affinity adenosine receptor agonist (Ki values are 6.2, 14, and 20 nM for human A3, A1 and A2A receptors respectively; EC50 = 2.4 μM for human A2B).
  36. CaSR agonist

    Evocalcet is a calcium-sensing receptor agonist. The calcium-sensing receptor (CaSR) is a Class C G-protein coupled receptor which senses extracellular levels of calcium ion.
  37. Dopamine Receptor Agonist?€?

    SKF38393 HCl is a D1 agonist with IC50 of 110 nM.
  38. EP2 Agonist

    C-544326 is a potent and selective prostaglandin E2 receptor agonist with EC50 value of 2.8 nM.
  39. Serotonin2A Receptor Inverse Agonist

    Pimavanserin is a potent and selective serotonin 5-HT2A inverse agonist with pIC50 of 8.73, used to treat psychosis associated with Parkinson?€?s disease.
  40. 5HT(1A) receptor agonist

    Eptapirone is a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
  41. 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).
  42. Alpha adrenergic agonist

    Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist.
  43. 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.
  44. 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.
  45. 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.
  46. 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.
  47. MT1/MT2 agonist

    Melatonin is a endogenous hormone that acts as an agonist at melatonin receptors MT1 and MT2.
  48. 5-HT4-receptor agonist

    Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist.
  49. 5-HT1 receptor

    Naratriptan is a selective 5-HT1 receptor subtype agonist.
  50. 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.

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