GPCR/G Protein

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  1. 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).
  2. Alpha adrenergic agonist

    Clonidine is classified as a centrally acting alpha adrenergic agonist.Clonidine acts centrally as an imidazoline receptor agonist.
  3. 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.
  4. 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.
  5. β adrenoceptor agonist

    Isoprenaline or isoproterenol is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.
  6. 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.
  7. 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.
  8. MT1/MT2 agonist

    Melatonin is a endogenous hormone that acts as an agonist at melatonin receptors MT1 and MT2.
  9. 5-HT4-receptor agonist

    Mosapride citrate acts as 5-HT4 receptor agonist and 5-HT3 receptor antagonist.
  10. 5-HT1 receptor

    Naratriptan is a selective 5-HT1 receptor subtype agonist.
  11. 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.
  12. 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).
  13. 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.
  14. α2 adrenergic agonist

    Rilmenidine is a second-generation imidazoline-α2 adrenergic agonist.
  15. 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.
  16. Adrenergic Receptor agonist

    Synephrine (Oxedrine) is an amine compound commonly used for weight loss.
  17. 5-HT Receptor agonist

    Tianeptine sodium is a selective serotonin reuptake enhancer (SSRE) in vitro and in vivo.
  18. 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
  19. GPR agonist

    TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.
  20. 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.
  21. Dopamine Receptor agonist

    Rotigotine hydrochloride is a dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.
  22. 5-HT1A agonist

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

    BRL 52537 hydrochloride is a highly selective and potent κ-opioid agonist (Ki = 0.24 nM).
  24. 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
  25. β1-selective adrenergic receptor agonist

    Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
  26. 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.
  27. adenosine A2A receptor agonist

    CGS 21680 is a selective adenosine A2A receptor agonist, with a Ki of 27 nM.
  28. 5-HT1B/1D receptor agonist

    Eletriptan hydrobromide is a selective SR-1B/SR-1D agonist.
  29. mGlu2 agonist

    LY2979165 is a mGlu2 agonist.
  30. 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).
  31. nonimidazole inverse agonist

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

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

    Rotigotine is dopamine D2 and D3 receptor agonist. Ki values are 13 and 0.71 nM for D2 and D3 respectively.
  34. 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.
  35. Adenosine A2A Receptor Agonist

    CGS 21680 is a specific adenosine A2A subtype receptor agonist.
  36. α1-adrenergic receptor agonist

    Phenylephrine is a selective α1-adrenergic receptor agonist used primarily as a decongestant, as an agent to dilate the pupil, and to increase blood pressure.
  37. 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.
  38. imidazoline receptor 1 agonist

    Moxonidine is a selective agonist at the imidazoline receptor subtype 1 (I1). Moxonidine causes a decrease in sympathetic nervous system activity and, therefore, a decrease in blood pressure.
  39. 5-HT Receptor agonist

    Prucalopride is a selective, high affinity 5-HT4 receptor agonist which targets the impaired motility associated with chronic constipation, thus normalising bowel movements.
  40. 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.
  41. beta2-adrenergic receptor agonist

    Salmeterol is a long-acting beta2-adrenergic receptor agonist
  42. 5-HT Receptor agonist

    Almotriptan malate (Axert) is a selective 5-hydroxytryptamine1B/1D (5-HT1B/1D) receptor agonist, used for the treatment of Migraine attacks in adults.
  43. 5-HT1A receptor agonist

    Aripiprazole is a human 5-HT1A receptor partial agonist with a Ki of 4.2 nM.
  44. adrenergic agonist

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

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

    Dexmedetomidine hydrochloride is the active isomer of medetomide which acts a potent, highly selective alpha2-AR (alpha2-adrenoceptor) agonist.
  47. COX inhibitor/histamine H1 receptor agonist

    Fexofenadine HCl is an antihistamine that inhibits Cox-1, Cox-2, and is a histamine H1 receptor agonist
  48. CB receptor agonist

    WIN 55,212-2 is a potent cannabinoid receptor agonist that has been found to be a potent analgesic in a rat model of neuropathic pain. It activates p42 and p44 MAP kinase via receptor-mediated signaling.
  49. CB2 agonist

    MDA 19 is a potent and selective agonist for the cannabinoid receptor CB2, with reasonable selectivity over the psychoactive CB1 receptor.
  50. 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.

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