Adenosine Receptors

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  1. 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.
  2. Adenosine receptor antagonist

    Aminophylline is a nonselective adenosine receptor antagonist and phosphodiesterase inhibitor capable of reversing ischemia-induced bradyasystole.
  3. Adenosine receptor antagonist

    Dyphylline is a xanthine derivative with bronchodilator and vasodilator effects. It acts as an adenosine receptor antagonist and phosphodiesterase inhibitor.
  4. adenosine A2A receptor agonist

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

    Istradefylline (KW-6002) is a selective antagonist at the A2A receptor. It has been found to be useful in the treatment of Parkinson's disease.
  6. A2a receptor antagonist

    SYN115 is an orally administered, potent and selective inhibitor of the adenosine 2a (A2a) receptor that is being developed initially for the treatment of Parkinson?€?s disease, but may also have utility in other CNS disorders.
  7. Adenosine A2A Receptor Agonist

    CGS 21680 is a specific adenosine A2A subtype receptor agonist.
  8. A3 adenosine receptor agonist

    AB-MECA is a high affinity A3 adenosine receptor agonist, has high affinity for recombinant A1 and A3 receptors.
  9. A2A adenosine agonist

    Regadenoson was selective agonist for the A2A adenosine receptor versus the A1, A2B, and A3 receptors in binding and functional studies. Regadenoson was also found to be a full and potent agonist to cause coronary vasodilation, a response that has a very large A2A receptor reserve?
  10. adenosine A2A/A1 receptor antagonist

    A2A receptor antagonist 1 (CPI-444 analog) is an antagonist of both adenosine A2A receptor and A1 receptor with Kis of 4 and 264 nM, respectively.
  11. Adenosine receptor inhibitor

    N-[(4-Aminophenyl)methyl]adenosine is a adenosine receptor inhibitor, with Ki of 29 nM for Rat ecto-5??-Nucleotidase. IC50 value: 29.0 ± 1.7 nM (Ki) Target: Adenosine Receptor
  12. A2A Receptor Antagonist

    SCH 442416 is a selective adenosine A2A receptor antagonist; binds to human and rat A2A receptors with high affinity (Ki values are 0.048 and 0.5 nM respectively). Displays > 23000-fold selectivity for hA2A over hA1 in vitro with minimal affinity for hA2B and hA3 receptors (IC50 > 10 μM).
  13. Tamsulosin hydrochloride is an antagonist of alpha1A adrenoceptors in the prostate.
  14. Adenosine A2A receptor antagonist

    ST3932 is a metabolite of ST1535, acts as an antagonist of adenosine A2A receptor, with Kis of 8 nM and 33 nM for A2A and A1 receptors, respectively.
  15. human A3 adenosine receptor antagonist /Aurora inhibitor

    Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.
  16. A1 adenosine receptor agonist

    Tecadenoson (CVT-510) is a selective A1 adenosine receptor agonist.
  17. Adenosine A2A receptor antagonist

    Preladenant is a potent and selective antagonist at the adenosine A2A receptor.
  18. Adenosine A2A antagonist

    ZM-241385 is a potent and highly selective Adenosine A2A-R antagonist, with a pA2 of 9.02 for Adenosine A2A-R in cardiac vasculature and selectivities of 1000, 91 and 500,000 over Adenosine A1-R, Adenosine A2B-R and Adenosine A3-R sites, respectively.
  19. human 5'-methylthioadenosine phosphorylase inhibitor

    MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
  20. adenosine A2B receptors antagonist

    CVT-6883, a selective A2B adenosine antagonist, represents a novel potential approach to treating cardiopulmonary diseases.
  21. Adenosine kinase inhibitor

    5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM.
  22. A2A receptor antagonist

    Vipadenant, also known as BIIB014, CEB-4520, is a potent, selective and orally available adenosine A2A receptor antagonist under development for Parkinson's disease. Vipadenant demonstrates strong oral activity in commonly used models of Parkinson's disease.
  23. Adenosine Receptor agonist

    Capadenoson is a selective agonist of adenosine-A1 receptor.
  24. Adenosine A Receptor antagonist

    CGS 15943 is a potent, non-selective Adenosine A Receptor antagonist. It is orally active in vivo.
  25. Adenosine A3-R agonist

    IB-MECA has been shown to act as a potent and selective Adenosine A3-R agonist with Ki values of 1.1, 54 and 56 nM for Adenosine A3-R, Adenosine A1-R and Adenosine A2A-R, respectively.
  26. Adenosine A3 receptor agonist

    CF-102 is an orally bioavailable, synthetic, highly selective adenosine A3 receptor (A3AR) agonist with potential antineoplastic activity.
  27. A2A adenosine receptor antagonist

    SCH58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.
  28. Adenosine A1-R antagonist

    DPCPX, a xanthine derivative, is a very potent and selective Adenosine A1-R antagonist. It displays very modest efficacy against Adenosine A2A-R, Adenosine A2B-R and Adenosine A3-R.
  29. 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).
  30. Adenosine A2 receptor agonist

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

    Alloxazine is an A2 receptor antagonist, which is approximately 10-fold more selective for the A2B receptor than for the A2A receptor.
  32. A2AR antagonist

    AZD-4635 (HTL1071) is an oral A2AR antagonist that binds to human A2AR with a Ki of 1.7 nM and with > 30-fold selectivity over other adenosine receptors.
  33. A1 adenosine receptors antagonist

    Proxyphylline is a derivative of theophylline which is used as a bronchodilator and for its cardiovascular properties. It selectively antagonizes A1 adenosine receptors (Ki = 82 nM for bovine brain) versus A2 adenosine receptors (Ki = 850 μM for platelets).
  34. Adenosine receptor antagonist

    Theophylline-7-acetic acid (Acefylline), acting as an adenosine receptor antagonist, is a stimulant drug of the xanthine chemical class.
  35. 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.
  36. Adenosine A3 receptor antagonist

    MRS1186 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 7.66 nM.
  37. Adenosine A3 receptor antagonist

    MRS1177 is a potent and selective human Adenosine A3 receptor (hA3AR) antagonist, with a Ki of 0.3 nM.
  38. 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).
  39. A2AR antagonist

    CPI-444 is a potent, oral and selective A2A receptor (A2AR) antagonist, which induces antitumor responses.
  40. Adenosine A1 receptor agonist

    N6-Cyclopentyladenosine (CPA) is a selective Adenosine A1 receptor agonist, with Ki values of 2.3 nM, 790 nM and 43 nM for human A1, A2A and A3 receptors, respectively.
  41. adenosine A3 receptor antagonist

    MRE3008F20 is a highly potent and selective antagonist of adenosine A3 receptor (AA3R), inhibits agonist-induced cAMP elevation in resting T lymphocytes with an IC50 of 5 nM.
  42. Adenosine receptor agonist

    N6-Ethyladenosine is an adenosine derivative, acts as a Adenosine receptor agonist, with Kis of 4.9 and 4.7 nM for hA1AR and hA3AR, respectively.
  43. A1 adenosine receptor agonist

    N6-(2-Phenylethyl)adenosine is a selective A1 adenosine receptor agonist.
  44. A2B adenosine receptor antagonist

    BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM.
  45. adenosine receptor antagonist

    Taminadenant is an antagonist of adenosine receptor.
  46. AA3R antagonist

    Adenosine antagonist-1 is an adenosine A3 receptor (AA3R) antagonist.
  47. A2A adenosine agonist

    PD 117519 (CI947) is an A2A adenosine agonist which has shown oral antihypertensive activity in pharmacological animal models.
  48. adenosine A1 receptor agonist

    GR79236 is a highly potent and selective adenosine A1 receptor agonist (Ki = 3.1 nM) that has analgesic and anti-inflammatory actions in humans and animals.
  49. A3 adenosine receptor agonist

    APNEA (N6-[2-(4-Aminophenyl)ethyl]adenosine) is a potent, non-selective A3 adenosine receptor agonist.
  50. A1 receptor agonist

    N6-Cyclohexyladenosine is a selective A1 receptor agonist (EC50 = 8.2 nM).

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