Adrenergic Receptors

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  1. Beta1 receptor blocker

    Metoprolol is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension.
  2. 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.
  3. Formoterol is a long-acting β2-agonist used in the management of asthma and/or chronic obstructive pulmonary disease (COPD).
  4. Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.
  5. Phentolamine is a reversible nonselective alpha-adrenergic antagonist.
  6. Terazosin is a selective alpha 1 antagonist used for treatment of symptoms of an enlarged prostate (BPH).
  7. beta2-adrenergic receptor agonist

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

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

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

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

    Diprophylline is a xanthine derivative with bronchodilator and vasodilator effects.
  13. β1-adrenergic receptor blocker

    Bucindolol is a β1-adrenergic receptor blocker, with intrinsic sympathomimetic activity, used in the research of heart failure.
  14. 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.
  15. β-adrenoceptor antagonist

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

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

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

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

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

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

    Spirendolol is a β adrenergic receptor antagonist.
  22. 5-HT2A/α1-adrenergic receptor antagonist

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

    Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist.
  24. 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.
  25. β-adrenergic agonist

    Imoxiterol (RP 58802B) is a β-adrenergic agonist.
  26. 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.
  27. β-adrenoceptor blocking agent

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

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

    Formoterol is a long-acting β2 agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD).
  30. 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.
  31. 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.
  32. 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.
  33. Metabolites of tulobuterol

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

    Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
  35. Metoprolol succinate is a cardioselective β-adrenergic receptor blocker with IC50 of 42 ng/mL.
  36. 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.
  37. 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.
  38. 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.
  39. Dopamine Receptors Blocker

    Trifluoperazine dimaleate is a potent dopamine receptor blocker, primarily indicated for research into antipsychotic mechanisms. This compound exhibits significant α1-adrenergic receptor antagonism and serves as an inhibitor of NUPR1, highlighting its potential anticancer properties. Additionally, trifluoperazine dimaleate functions as a calmodulin inhibitor and inhibits P-glycoprotein activity. Its versatile applications extend to studying schizophrenia and the reversible inhibition of influenza virus morphogenesis.
  40. Stable Isotope

    Carvedilol-d3 is a deuterium-labeled analogue of Carvedilol, functioning primarily as a non-selective β/α-1 adrenergic receptor blocker. It exhibits significant biological activity by inhibiting lipid peroxidation in a dose-dependent manner with an IC50 value of 5 μM. This compound serves as a versatile antihypertensive agent and has potential applications in the treatment of angina and congestive heart failure. Furthermore, Carvedilol-d3 promotes autophagy and is known to inhibit the NLRP3 inflammasome, making it valuable for research involving inflammatory processes.
  41. Stable Isotope

    Trifluoperazine-d3 dihydrochloride is a deuterated derivative of Trifluoperazine, primarily targeting dopamine receptors to exert its antipsychotic effects. This compound is a potent α1-adrenergic receptor antagonist and an effective inhibitor of NUPR1, showcasing anticancer properties. Additionally, it functions as a calmodulin inhibitor and can interfere with P-glycoprotein activity. Trifluoperazine-d3 dihydrochloride is valuable for research applications related to schizophrenia and serves as a reversible inhibitor of influenza virus morphogenesis.
  42. Stable Isotope

    Carvedilol-d5 is a deuterium-labeled analogue of Carvedilol, a non-selective β/α-1 adrenergic receptor blocker. It exhibits lipid peroxidation inhibition with an IC50 of 5 μM and serves as a versatile antihypertensive agent, showing potential in the treatment of angina and congestive heart failure. Additionally, Carvedilol functions as an autophagy inducer and inhibits the NLRP3 inflammasome, making it relevant for research in inflammatory pathways and cardiovascular health.
  43. Stable Isotope

    Dronedarone-d6 hydrochloride is a deuterium-labeled derivative of Dronedarone, serving as a stable isotope for research applications. This compound functions primarily as a class III antiarrhythmic agent, effective in the study of atrial fibrillation (AF) and atrial flutter. Dronedarone-d6 hydrochloride exhibits potent blockade of various ion currents, including potassium, sodium, and L-type calcium currents, and also demonstrates antiadrenergic activity through noncompetitive binding to β-adrenergic receptors. Additionally, it acts as a substrate and moderate inhibitor of the CYP3A4 enzyme, making it valuable for pharmacokinetic studies.
  44. Stable Isotope

    Dronedarone-d6 is a deuterium-labeled derivative of the antiarrhythmic agent Dronedarone, primarily targeting various ion channels, including potassium, sodium, and L-type calcium channels. This compound is vital for investigating the mechanisms underlying atrial fibrillation (AF) and atrial flutter, as well as for studying its antiadrenergic properties through its noncompetitive binding to β-adrenergic receptors. In addition, Dronedarone-d6 serves as a substrate and moderate inhibitor of CYP3A4, making it relevant for pharmacokinetic studies in cardiovascular research.
  45. Stable Isotope

    Salbutamol-d3 is a deuterium-labeled derivative of Salbutamol, a short-acting β2-adrenergic receptor agonist. This compound is primarily employed as a stable isotope for metabolic tracing and pharmacokinetic studies. Salbutamol exhibits significant therapeutic effects by relaxing bronchial smooth muscle, making it a valuable tool in research involving asthma and chronic obstructive pulmonary disease. Additionally, it has been identified to promote tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT pathway, highlighting its utility in oncology research.
  46. Stable Isotope

    Salbutamol-d9 acetate is a deuterium-labeled derivative of Salbutamol, a short-acting β2-adrenergic receptor agonist. This compound is primarily utilized as a stable isotope for research applications, specifically in studying its effects on bronchial smooth muscle relaxation and the β2-adrenergic receptor pathways. Salbutamol has also been implicated in promoting tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling cascade, making it relevant for cancer research as well as respiratory studies.
  47. Stable Isotope

    Salbutamol-d9 is a deuterium-labeled derivative of Salbutamol, a short-acting β2-adrenergic receptor agonist. It is primarily utilized as a stable isotope in biological research, allowing for the precise tracking of Salbutamol's pharmacokinetics and metabolism. Salbutamol is known for its ability to relax bronchial smooth muscle and is widely studied in the context of asthma and chronic obstructive pulmonary disease, as well as its role in promoting tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling pathway.
  48. Adrenergic Receptor Agonist

    Salbutamol adipate is an orally active short-acting β2-adrenergic receptor agonist. It is known to promote tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT pathway. Additionally, Salbutamol adipate is effective in relaxing bronchial smooth muscle, making it a valuable tool for researching bronchospasm associated with asthma and chronic obstructive pulmonary disease.
  49. Stable Isotope

    Salbutamol-d4 is a deuterated form of the beta-2 adrenergic receptor agonist Salbutamol, designed for stable isotope applications in biochemical research. This compound has been shown to promote tumorigenesis in gastric cancer cells via the β2-AR/ERK/EMT signaling pathway. In addition, Salbutamol-d4 is utilized in studies investigating bronchospasms associated with asthma and chronic obstructive pulmonary disease (COPD), allowing for precise tracking of biological processes and metabolic pathways.
  50. Stable Isotope

    Carvedilol-d4 is a deuterated derivative of Carvedilol, a non-selective β/α-1 adrenergic receptor antagonist. It exhibits dose-dependent inhibition of lipid peroxidation with an IC50 value of 5 μM. Carvedilol acts as a multifaceted antihypertensive agent, demonstrating potential therapeutic applications in managing conditions such as angina and congestive heart failure. Additionally, it has been identified as an autophagy inducer and a modulator of the NLRP3 inflammasome, making it a valuable tool for research into cardiovascular and inflammatory diseases.

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