GPCR/G Protein

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  1. A1 adenosine receptor agonist

    Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.
  2. 5-HT1A agonist

    BMY 7378 is a 5-HT1A partial agonist and high affinity α1D adrenoceptor antagonist.
  3. Opioid Receptors agonist

    BRL 52537 hydrochloride is a highly selective and potent κ-opioid agonist (Ki = 0.24 nM).
  4. CB2 receptor agonist

    GW842166X is a selective non-cannabinoid CB2 receptor agonist, which is undergoing clinical development as a novel oral treatment for inflammatory pain
  5. D2 receptor agonist

    B-HT 920 is a dopamine agonist that has been proposed as an antiparkinsonian agent. It also has α1-adrenergic and α2-adrenergic agonist activity.
  6. adenosine A2A receptor agonist

    CGS 21680 is a selective adenosine A2A receptor agonist, with a Ki of 27 nM.
  7. mGlu2 agonist

    LY2979165 is a mGlu2 agonist.
  8. α2-adrenoceptor agonist

    Medetomidine(Domtor) is a potent, highly selective α2-adrenoceptor agonist (Ki values are 1.08 and 1750 nM for α2- and α1-adrenoceptors respectively).
  9. nonimidazole inverse agonist

    Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
  10. CB1 receptor inverse agonist

    Rimonabant hydrochloride is a CB1 receptor inverse agonist.
  11. Dopamine agonist

    Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.
  12. CB1 receptor inverse agonist

    Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
  13. CaSR agonist

    Strontium ranelate is an antiosteoporotic agent which both increases bone formation and reduces bone resorption, resulting in a rebalance of bone turnover in favor of bone formation. This is similar to the effects of choline stabilized orthosilicic acid.
  14. CB2 agonist

    JWH-133 is a potent selective CB2 receptor agonist, with a Ki of 3.4nM and selectivity of around 200x for CB2 over CB1 receptors.
  15. beta2-adrenergic receptor agonist

    Salmeterol is a long-acting beta2-adrenergic receptor agonist
  16. adrenergic agonist

    Adrenalone is an adrenergic agonist used as a topical vasoconstrictor and hemostatic, mainly acts on alpha-1 adrenergic receptors.
  17. β2-adrenergic receptor

    Carvedilol is a β1- and β2-adrenergic receptor (AR) agonist with antioxidant properties.
  18. alpha2-adrenoceptor agonist

    Dexmedetomidine hydrochloride is the active isomer of medetomide which acts a potent, highly selective alpha2-AR (alpha2-adrenoceptor) agonist.
  19. CB2 agonist

    MDA 19 is a potent and selective agonist for the cannabinoid receptor CB2, with reasonable selectivity over the psychoactive CB1 receptor.
  20. FFAR1/GPR40 agonist

    LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively.

  21. A3 adenosine receptor agonist

    AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.
  22. 5-HT2c receptor agonist

    PRX933 hydrochloride is a 5-HT2c receptor agonist extracted from patent WO 2014140631 A1.
  23. human 5-HT1A receptor agonist

    AP521 is an agonist of human 5-HT1A receptor with an IC50 of 94 nM.
  24. 5-HT2C receptor agonist

    YM348 is a potent and orally active 5-HT2C receptor agonist, which shows a high affinity for cloned human 5-HT2C receptor (Ki: 0.89 nM).
  25. β-adrenergic receptors agonist

    Cimaterol is a potent agonist of β-adrenergic receptors (pEC50 = 8.13, 8.78, and 6.62 for human β1, β2, and β3, respectively).
  26. α2- adrenoceptor antagonist / I2 imidazoline receptor agonist

    Idazoxan hydrochloride is an α2-AR adrenoceptor antagonist and potential I2 imidazoline receptor agonist. Also displays I1 imidazoline receptor antagonist activity. (pKi values are 5.90, 7.22, 8.01, 7.43, and 7.7 for I1, I2, α 2A, α2B, and α 2C receptors respectively).
  27. imidazoline receptor 1 agonist

    Moxonidine hydrochloride is a centrally acting antihypertensive agent.
  28. Adrenergic Receptor agonist

    Tulobuterol is a beta-adrenergic receptor agonist that is related structurally to Terbutaline.
  29. Adrenoceptors agonist

    UK 14,304 tartrate is a water-soluble form UK 14,304. It is a full α2 adrenergic agonist.
  30. Adrenergic Receptor agonist

    Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR.
  31. GPR40/FFA1 agonist

    AMG-837 calcium hydrate is a potent, orally bioavailable GPR40 agonist.
  32. δ opioid receptor agonist

    ADL5747 is a selective, nonpeptidic δ opioid receptor agonist.
  33. Kainate receptor agonist

    Kainate class of ionotropic glutamate receptor agonist. Has been shown to induce seizures and neurodegeneration in vivo and has also been used to induce experimental epilepsy in rodents and to examine excitation-induced neuronal apoptosis mechanisms.
  34. prostanoid DP-receptor (DP1) agonist

    BW 245C is a prostanoid DP-receptor (DP1) agonist, used to treat stroke.
  35. 5-HT2C agonist

    S 32212 hydrochloride is an inverse agonist of 5-HT2C receptors (pKi = 8.18 at human 5-HT2C INI receptors).
  36. D2 dopamine partial agonist

    Brexpiprazole is a novel D2 dopamine partial agonist investigational product currently in clinical trials for the treatment of depression, schizophrenia, and attention deficit hyperactivity disorder (ADHD).
  37. NTR1 agonist

    ML-314 is a brain penetrant nonpeptidic β-arrestin biased ggonist of the neurotensin NTR1 receptor, which exhibits full agonist behavior against NTR1 (EC50 = 2.0 μM) in the primary assay and selectivity against NTR2.
  38. 2A-AR adrenergic agonist

    Guanabenz acetate is an a2A-AR adrenergic agonist and IGRS (imidazoline I2 binding site) selective ligand.
  39. EDG-1 (S1P1) agonist

    CYM 5442 HCl is a potent and selective EDG-1 (S1P1) agonist in vitro (EC50 = 1.35 nM).
  40. histamine H3 receptor agonist

    Immethridine hydrobromide is a strong and highly selective histamine H3 receptor agonist (pEC50 = 9.74) that displays 300-fold selectivity over the H4 receptor (pKi values are 9.07 and 6.61 respectively).
  41. β3 adrenergic agonist

    CL 316243 disodium salt, a beta-3 adrenergic agonist, was developed as an anti-obesity and diabetes drug, and causes rapid decreases in blood glucose levels in mice.
  42. β3-adrenergic receptors agonist

    BRL-37344 is a b3-AR (b 3-adrenoceptor) selective agonist with lipolytic activity.
  43. opioid receptors agonist

    DPI-3290 (Org 41793) is a potent and specific opioid receptors agonist with Ki values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively.
  44. dopamine D2 receptor agonist

    Bromocriptine mesylate is a potent dopamine receptor agonist that binds the D2 receptor with highest affinity (Ki = 2.5 nM).1,2 As a result, it has found applications in combination therapy for Parkinsonism.
  45. GPR119 agonist

    AR-231453 is a potent and selective small molecule agonis of GPR119 that enhances glucose dependent insulin secretion and glucagon like peptide-1 (GLP-1) release.
  46. TGR5(GPCR19) agonist

    TGR5 Receptor Agonist is a potent TGR5(GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).
  47. adrenergic alpha-2 receptor agonist

    Medetomidine Hydrochloride is an adrenergic alpha-2 receptor agonist, which is used in veterinary medicine for its analgesic and sedative properties.
  48. GLP-1 receptor agonist

    BETP is a selective positive allosteric modulator and partial agonist of the glucagon-like peptide 1 (GLP-1) receptor.
  49. 5-HT1A/1B and 5-HT2C agonist

    RU 24969 succinate is a potent 5-HT1A/1B and moderate 5-HT2C agonist that may also release 5-HT.

  50. Dopamine receptor agonist

    Cabergoline, a lysergic acid amide derivative, is a potent dopamine D2 receptor agonist.

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