Adrenergic Receptors

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  1. β2-AR agonist

    Higenamine (Norcoclaurine), a β2-AR agonist, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries.
  2. Reboxetine is an antidepressant compound that selectively inhibits norepinephrine uptake (IC50s = 8.2 and 1,070 nM for norepinephrine and serotonin transporters, respectively). It displays greater than 1,000-fold affinity for binding rat norepinephrine receptors compared to serotonin, histamine, acetylcholine, or dopamine receptors (Kis = 1.1, 129, 1,400, 3,900, and >10,000 nM, respectively).
  3. Androgen Receptor inhibitor

    ARN-509 is an androgen receptor antagonist with potential antineoplastic activity. ARN-509 binds to AR in target tissues thereby preventing androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated to the nucleus. This prevents binding to and transcription of AR-responsive genes.
  4. Nebivolol hydrochloride is t a highly selective antagonist of the β1-adrenoceptor (Ki = 0.88 nM, β2-adrenoceptor Ki = 48 nM).
  5. β3 adrenergic receptor activator

    Mirabegron is a potent bladder relaxant and reagent for diabetes remedy.
  6. β-adrenergic blocker

    S(-)-Propranolol Hydrochloride is a nonselective β-adrenergic receptor (βAR) antagonist, has high affinity for the β1AR and β2AR with Ki values of 1.8 nM and 0.8 nM, respectively. Propranolol hydrochloride inhibits [3H]-DHA binding to rat brain membrane preparation with an IC50 of 12 nM.
  7. β1-selective adrenergic receptor agonist

    Norepinephrine (Levarterenol; L-Noradrenaline) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
  8. 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.
  9. β adrenoceptor agonist

    Isoprenaline or isoproterenol is a non-selective beta-adrenergic agonist and structurally similar to adrenaline.
  10. α2C antagonist

    JP 1302 2HCl is a potent and selective α2C antagonist.
  11. H1 antagonist

    Asenapine shows high affinity (pKi) for numerous receptors, including the serotonin 5-HT1A (8.6), 5-HT1B (8.4), 5-HT2A (10.2), 5-HT2B (9.8), 5-HT2C (10.5), 5-HT5A (8.8), 5-HT6 (9.5), and 5-HT7 (9.9) receptors, the adrenergic α1 (8.9), α2A (8.9), α2B (9.5), and α2C (8.9) receptors, the dopamine D1 (8.9), D2 (8.9), D3 (9.4), and D4 (9.0) receptors, and the histamine H1 (9.0) and H2 (8.2) receptors.
  12. Doxazosin mesylate, a quinazoline compound, is an α1-selective alpha blocker used to treat high blood pressure and urinary retention associated with benign prostatic hyperplasia (BPH).
  13. β2 adrenergic receptor antagonist

    ICI-118551 is a selective beta2 adrenergic receptor (adrenoreceptor) antagonist.
  14. alpha1/beta adrenergic receptors antagonist

    Labetalol HCl is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors.
  15. Prazosin HCl is an α1 and α2B-adrenoceptor antagonist. Also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 nM).
  16. Clenbuterol Hydrochloride is a sympathomimetic β2-adrenoceptor agonist that has been used as a bronchodilator in the treatment of pulmonary diseases such as asthma. At higher doses, clenbuterol acts as an anabolic steroid, favoring skeletal muscle protein synthesis at the expense of fat deposition.
  17. beta-adrenergic blocking agent

    Ancarolol is a beta-adrenergic blocking agent.
  18. alpha-1A/alpha-1B-adrenoceptor antagonist

    Tamsulosin is an alpha1a-selective alpha blocker used in the symptomatic treatment of benign prostatic hyperplasia (BPH).
  19. α2-adrenergic receptor angatonist

    OPC-28326 is a selective peripheral vasodilator and an angatonist of α2-adrenergic receptor, with Ki of 2040, 285, and 55?nM for α2A-, α2B- and α2C-adrenoceptors, respectively.
  20. β3-adrenergic receptor agonist

    β3-AR agonist 1 (compound 15) is a highly potent, selective, and orally available β3-adrenergic receptor (β3-AR) agonist (EC50=18 nM), being inactive to β1-, β2-, and α1A-AR (β1/β3, β2/β3, and α1A/β3>556-fold).
  21. beta2-adrenergic agonist

    Arformoterol tartrate is a beta2-adrenergic agonist
  22. α2 adrenergic agonist

    AGN 192836 is a potent and selective α2 adrenergic agonist with EC50s of 8.7, 41 and 6.6 nM for α2A, α2B and α2C receptor, respectively.
  23. Adrenergic Receptor agonist

    Tetrahydrozoline Hydrochloride is an alpha agonist which causes constriction of conjunctival blood vessels.
  24. ultra-long-acting β??? adrenoreceptor agonist

    Vilanterol is a novel and selective agonist of Beta2-AR with a PEC50 value of 10.37??0.05.
  25. β2 adrenergic antagonist

    ICI 118551 hydrochloride is a selective β2 adrenergic antagonist.
  26. Adrenoceptors antagonist

    BRL 44408 maleate is a high purity Adrenoceptors antagonist. It increases hippocampal noradrenalin release following systemic administration.
  27. 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).
  28. Bisoprolol is a cardioselective β1-adrenergic blocking agent used for secondary prevention of myocardial infarction (MI), heart failure, angina pectoris and mild to moderate hypertension.
  29. Adrenergic α1 Receptor Antagonist

    HEAT hydrochloride is a very selective α1-AR adrenoceptor antagonist, precursor of the 3-[125I]-derivative. Adrenoreceptors (AR) or adrenergic receptors are G-protein coupled receptors involved in a variety of sympathetic nervous system processes.
  30. 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).
  31. 5-HT1A receptor antagonist

    NAN-190 is a drug and research chemical widely used in scientific studies. It was previously believed to act as a selective 5-HT1A receptor antagonist, but a subsequent discovery showed that it also potently blocks the α2-adrenergic receptor.
  32. Octopamine hydrochloride is an invertebrate biogenic amine neurotransmitter, related to noradrenalin, that is an adrenoceptor agonist.
  33. α-Adrenergic blocker

    Phentolamine Hydrochloride is an AR (α-Adrenergic) blocker.
  34. Beta adrenergic receptor blocker

    Pindolol is a nonselective beta blocker with partial beta-adrenergic receptor agonist activity.
  35. α2-adrenergic receptor antagonist

    Rauwolscine is a natural alkaloid that acts as a selective and reversible α2-adrenergic receptor antagonist (Ki = 12 nM).
  36. Adrenoceptors antagonist

    S-(-)-Atenolol is the active enantiomer of atenolol that is a cardioselective β-adrenergic blocker.
  37. Adrenoceptors antagonist

    (S)-Timolol maleate is a adrenergic receptor antagonist selective for β1-AR.
  38. Adrenoceptors antagonist

    SR 59230A hydrochloride is a β3-adrenoceptor antagonist.
  39. Adrenergic Receptor agonist

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

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

    Xylazine hydrochloride is an activator of α2A-AR, α2B-AR and α2C-AR.
  42. adrenergic receptor antagonist

    Celiprolol HCl is a b1 adrenergic receptor antagonist and a b2 adrenergic receptor partial agonist that has been shown to relax human arteries and veins with ED50 values of 40-50 M in vitro.
  43. 2A-AR adrenergic agonist

    Guanabenz acetate is an a2A-AR adrenergic agonist and IGRS (imidazoline I2 binding site) selective ligand.
  44. 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.
  45. β3-adrenergic receptors agonist

    BRL-37344 is a b3-AR (b 3-adrenoceptor) selective agonist with lipolytic activity.
  46. Beta-1 adrenergic receptor blocker

    Nebivolol is a selective inhibits Beta-1 adrenergic receptor with IC50 of 0.8 nM
  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. α2 adrenergic receptor antagonist

    Atipamezole HCl is a selective α2-adrenergic receptor antagonist (Ki values are 1.1, 1.0, 0.89, 1300 and 6500 nM for α2A, α2B, α2C, α1A and α1B receptors respectively). Has been shown to be a brain penetrant.
  49. β2-adrenoceptor agonist

    Salmeterol Xinafoate is a long-acting β2-adrenergic receptor agonist with anti-inflammatory effect.
  50. β-adrenoceptor agonist

    Bambuterol HCl is a potent β-adrenoceptor agonist, used in the treatment of asthma.

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