Adrenergic Receptors

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  1. beta-adrenergic agonist

    Nylidrin hydrochloride is a beta-adrenergic agonist. Nylidrin hydrochloride is shown to be an effective inhibitor of IgE-mediated release of histamine from human basophils, and thus can be used as antiallergic agent.
  2. adrenergic receptor inhibitor

    Asenapine(Org 5222) inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
  3. β-adrenergic receptor antagonist

    Metipranolol (hydrochloride) is a non-selective β-adrenergic receptor (β-AR) antagonist. Formulations containing metipranolol have been used in the treatment of elevated IOP in patients with ocular hypertension or glaucoma.
  4. DOPA decarboxylase inhibitor

    Methyldopa Sesquihydrate is a DOPA decarboxylase inhibitor and indirect α2-adrenergic receptor agonist used to treat hypertension.
  5. α2-receptor agonist

    Lofexidine is a selective α2-receptor agonist, commonly used to alleviate the physical symptoms of heroin and other types of opioid withdrawal.
  6. alpha-1 adrenergic receptors / mAChRs inhibitor

    Anisodamine is an inhibitor of alpha-1 adrenergic receptors and mAChRs isolated from Chinese solanacea plant.
  7. β2-adrenergic receptor agonist

    Tulobuterol Hydrochloride is a long-acting beta2-adrenergic receptor agonist.
  8. β-adrenergic receptor antagonist

    Levobunolol Hydrochloride is a non-cardioselective adrenergic beta-receptor antagonist with anti-glaucoma activity.
  9. α2 adrenoceptor antagonist

    Piperoxan hydrochloride is an α2 adrenoceptor antagonist.
  10. β2-adrenergic receptor agonist

    Vilanterol is a long-acting beta-2 agonist drug, which in May 2013 was approved in combination with fluticasone furoate for sale as Breo Ellipta by GlaxoSmithKline for the treatment of chronic obstructive pulmonary disease (COPD).
  11. α1D Adrenoceptor Antagonist

    TAK-259 is a Novel, Selective, and Orally Active α1D Adrenoceptor Antagonist (α1D, Ki = 1.1 nM) with Anti-urinary Frequency Effects and Reducing Human Ether-a-go-go-Related Gene (hERG) Liabilities.
  12. β-adrenergic receptors antagonist

    Acebutolol is a β-adrenergic receptors antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
  13. β2-adrenergic receptor agonist

    Clorprenaline HCl is a β2-receptor agonist, it has a significant expansion of the bronchial effect.
  14. β-adrenoceptor agonist

    Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist.
  15. β3-AR agonist

    L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM.
  16. α1A antagonist

    RS 17053 HCl is α1A-adrenoceptor antagonist, with very high affinity for α1A receptors (pKi and pA2 estimates of 9.1 - 9.9) and a 30 - 100 fold selectivity over the α1B and α1D subtypes (pKi and pA2 estimates 7.7 - 7.8).
  17. α1b adrenergic receptor antagonist

    L-765314 is a potent and selective α1b adrenergic receptor antagonist with Kis of 5.4 nM and 2.0 nM for rat and human α1b adrenergic receptor, respectively.
  18. β3-adrenergic receptor agonist

    Solabegron (GW 427353) is a selective β3-adrenergic receptor agonist, stimulating cAMP accumulation in Chinese hamster ovary cells expressing the human β3-AR, with an EC50 value of 22 nM.
  19. β2-adrenergic receptor agonist

    Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol.
  20. A2AR/ENT1 agonist

    A2AR-agonist-1 is a potent A2AR and ENT1 agonist with Ki of 4.39 and 3.47 for A2AR and ENT1.
  21. dual NE/DA transporter inhibitor

    Centanafadine is dual norepinephrine (NE)/dopamine (DA) transporter inhibitor, also inhibits serotonin transporter, with IC50s of 6 nM, 38 nM and 83 nM for human NE, DA and serotonin transporter , respectively.
  22. α2-adrenoceptor antagonist

    Atipamezole is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM.
  23. muscarinic receptor antagonist and β2-adrenoceptor agonist

    Batefenterol (GSK961081;TD-5959) is a novel muscarinic receptor antagonist and β2-adrenoceptor agonist; displays high affinity for hM2, hM3 muscarinic and hβ2-adrenoceptor with Ki values of 1.4, 1.3 and 3.7 nM, respectively.
  24. β1-adrenergic receptor blocker

    Bucindolol is a β1-adrenergic receptor blocker, with intrinsic sympathomimetic activity, used in the research of heart failure.
  25. β3-adrenoceptor agonist

    Amibegron hydrochloride is a selective β3-adrenoceptor agonist, with an EC50 of 3.5 nM for β-adrenoceptor in rat colon; Amibegron hydrochloride has anxiolytic and antidepressant activity.
  26. β-adrenoceptor antagonist

    Ko-3290 is an antagonist of β-adrenoceptor, with cardioselectivity and antilipolytic effects in animals.
  27. alpha-adrenergic agonist

    Indanidine is an alpha-adrenergic agonist.
  28. beta adrenergic receptor antagonist

    Ecastolol is a beta adrenergic receptor antagonist, with antianginal activities.
  29. α1 adrenergic receptor antagonist

    QF0301B is an α1 adrenergic receptor antagonist and a low α2 adrenoceptor, 5-HT2A, and histamine H1 receptor blocker.
  30. peripheral adrenoceptor antagonist

    Deriglidole is a peripheral adrenoceptor antagonist with a high affinity for α2-adrenoceptors.
  31. β adrenergic receptor antagonist

    Pargolol hydrochloride is a β adrenergic receptor antagonist.
  32. β adrenergic receptor antagonist

    Spirendolol is a β adrenergic receptor antagonist.
  33. 5-HT2A/α1-adrenergic receptor antagonist

    Lidanserin is a drug which acts as a combined 5-HT2A and α1-adrenergic receptor antagonist.
  34. ostsynaptic alpha adrenergic receptor antagonist

    Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist.
  35. β2 adrenergic receptor agonist

    BI-167107 is a high affinity, full agonist that binds to the β2 adrenergic receptor (β2AR) with a dissociation constant Kd of 84 pM.
  36. β-adrenergic agonist

    Imoxiterol (RP 58802B) is a β-adrenergic agonist.
  37. triple reuptake inhibitor/5-HT2A/5-HT2C/5-HT3/α1A-adrenergic receptor antagonis

    Tedatioxetine hydrobromide acts as a triple reuptake inhibitor and 5-HT2A, 5-HT2C, 5-HT3 and α1A-adrenergic receptor antagonist.
  38. β-adrenoceptor blocking agent

    (±)-Befunolol is a β-adrenoceptor blocking agent.
  39. α1 receptor antagonist

    Tamsulosin hydrochloride is a selective α1 receptor antagonist and a medicine which is used in benign prostatic hyperplasia.
  40. β2-adrenoceptor agonist

    Formoterol is a long-acting β2 agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD).
  41. adrenergic receptor/5-HT receptor inhibitor

    Asenapine hydrochloride inhibits adrenergic receptor (α1, α2A, α2B, α2C) with Ki of 0.25-1.2 nM and also inhibits 5-HT receptor (1A, 1B, 2A, 2B, 2C, 5A, 6, 7) with Ki of 0.03-4.0 nM.
  42. α-adrenergic receptor agonist

    Brimonidine Tartrate is a highly selective α-adrenergic receptor agonist with EC50 of 0.45 nM for the α2A adrenoreceptor, and used to treat open-angle glaucoma or ocular hypertension.
  43. α2A-adrenoceptor agonist

    Guanfacine hydrochloride, an anti-hypertensive agent, is a selective α2A-adrenoceptor agonist with Kd of 31 nM and displays 60-fold selectivity over α2B-adrenoceptors.
  44. Metabolites of tulobuterol

    HOKU-81, a new bronchodilator, is one of the metabolites of tulobuterol.
  45. serotonin (5-HT)/norepinephrine (NE) reuptake inhibitor

    Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
  46. NF-κB Expression Reducer, ERK 1/2 Activator, Beta-Adrenergic Receptor Modulator, Calcium Channel Inhibitor

    Eupatorin is a flavonoid that functions primarily as an NF-κB expression reducer and an ERK 1/2 activator, while also modulating beta-adrenergic receptors and inhibiting calcium channels. It demonstrates significant antiproliferative and vasodilatory effects, inducing apoptosis and causing G2/M phase cell cycle arrest, alongside reactive oxygen species (ROS) production. Eupatorin has been shown to impact inflammatory mediators and calcium signaling pathways, making it relevant for research in breast cancer, hypertension, and leukemia. Metabolized by CYP1A1 and other CYP1 enzymes, Eupatorin yields bioactive metabolites that maintain antiproliferative properties.
  47. Adrenergic Receptor Antagonist

    Aaptamine is an alkaloid derived from the marine sponge Aaptos suberitoides, functioning primarily as a competitive antagonist of the α-adrenergic receptor. This compound exhibits significant cytotoxicity against tumor cells, inducing apoptosis and cell cycle arrest while promoting p21 expression through a p53-independent mechanism. Aaptamine also demonstrates a variety of biological activities, including anti-tumor, antioxidant, antibacterial, and analgesic effects, making it a valuable tool for cancer research and therapeutic applications.
  48. α-1A Adrenergic Receptor Agonist

    Dabuzalgron is a selective α-1A adrenergic receptor agonist primarily utilized for the treatment of urinary incontinence. This compound exhibits key biological activity by enhancing bladder function, thereby mitigating symptoms associated with overactive bladder. Additionally, Dabuzalgron has been shown to provide protection against Doxorubicin-induced cardiotoxicity through the preservation of mitochondrial function, making it relevant in cardiovascular research.
  49. Stable Isotope

    N-(Phenylacetyl-d5)glycine is a deuterated form of phenylacetylglycine, functioning as a stable isotope. This compound serves as a gut microbial metabolite that can activate the beta-2 adrenergic receptor (β2AR). Its biological activity includes providing protective effects against cardiac injury induced by ischemia and reperfusion, making it valuable for research in cardiac health and metabolic studies.
  50. Stable Isotope

    D-Mannitol-13C6 is a stable isotope-labeled form of D-Mannitol, targeting metabolic pathways through its role as an osmotic agent. This compound is utilized in various research applications, including studies on calcium and magnesium absorption, cecal fermentation, and the modulation of insulin sensitivity. D-Mannitol has been shown to promote the browning of white adipose tissue by activating the β3-adrenergic receptor, which can lead to enhanced thermogenesis and potential reductions in blood glucose levels. Additionally, it is employed in plant cell culture to maintain osmotic balance and protect cellular integrity.

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