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. Prazosin HCl is an α1 and α2B-adrenoceptor antagonist. Also a potent antagonist at the melatonin MT3 receptor (Ki = 10.2 nM).
  15. alpha1/beta adrenergic receptors antagonist

    Labetalol HCl is a dual antagonist for both selective alpha1-adrenergic and nonselective beta-adrenergic receptors.
  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. Metoprolol succinate is a cardioselective β-adrenergic receptor blocker with IC50 of 42 ng/mL.
  27. 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).
  28. Pardoprunox is an antiparkinsonian drug currently under development by Solvay for the treatment of Parkinson's disease.
  29. DL-Adrenaline is a hormone and a neurotransmitter secreted by the medulla of the adrenal glands. DL-Adrenaline is found in small amounts in the body and is essential for maintaining cardiovascular homeostasis because of its ability to divert blood to tissues under stress.
  30. Noradrenaline bitartrate monohydrate (Levophed) is a direct alpha-adrenergic receptors stimulator.
  31. Beta1 receptor blocker

    Metoprolol is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.
  32. Betaxolol is a selective beta1 receptor blocker used in the treatment of hypertension and glaucoma. Being selective for beta1 receptors, it typically has fewer systemic side effects than non-selective beta-blockers, for example, not causing bronchospasm (mediated by beta2 receptors) as timolol may. Betaxolol also shows greater affininty for beta1 receptors than metoprolol.
  33. Formoterol is a long-acting β2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD).
  34. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.
  35. Phentolamine is a reversible nonselective alpha-adrenergic antagonist.
  36. Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of an enlarged prostate (BPH).
  37. beta2-adrenergic receptor agonist

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

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

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

    Dexmedetomidine hydrochloride is the active isomer of medetomide which acts a potent, highly selective alpha2-AR (alpha2-adrenoceptor) agonist.
  41. Procaterol is a short-acting β2-adrenergic receptor agonist with Kp of 8 nM, used for the treatment of asthma
  42. AR antagonist

    Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects.
  43. Adrenoceptors antagonist

    BRL 44408 maleate is a high purity Adrenoceptors antagonist. It increases hippocampal noradrenalin release following systemic administration.
  44. 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).
  45. 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.
  46. 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.
  47. 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).
  48. 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.
  49. Octopamine hydrochloride is an invertebrate biogenic amine neurotransmitter, related to noradrenalin, that is an adrenoceptor agonist.
  50. α-Adrenergic blocker

    Phentolamine Hydrochloride is an AR (α-Adrenergic) blocker.

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