Adrenergic Receptors

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  1. 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.
  2. β-adrenergic receptors antagonist

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

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

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

    L755507 is a potent, selective agonist of β3-AR with an IC50 of 35 nM.
  6. 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).
  7. Piribedil D8 is the deuterium labeled Piribedil, which is an antiparkinsonian agent.
  8. Droxidopa(L-DOPS), the mixture of Droxidopa (w/w80%) and Pharmaceutical starch (w/w20%), acts as a prodrug to the neurotransmitters norepinephrine (noradrenaline) and epinephrine (adrenaline).
  9. vasopressor/antihypotensive agent

    Midodrine D6 hydrochloride is deuterium labeled Midodrine, which is a vasopressor/antihypotensive agent.
  10. Indoramin D5 is deuterium labeled Indoramin, which is a piperidine antiadrenergic agent.
  11. β1-selective adrenergic receptor agonist

    Norepinephrine hydrochloride (Levarterenol hydrochloride; L-Noradrenaline hydrochloride) is a β1-selective adrenergic receptor agonist with EC50 of 5.37 μM.
  12. Bretylium (tosylate) is an inhibitor of the presynaptic release of vasoconstrictor neurotransmitters.
  13. β-adrenoceptor antagonist

    (+)-Penbutolol is a β-adrenoceptor antagonist, with an IC50 of 0.74 μM.
  14. beta-adrenoceptor agonist

    Bambuterol ((??)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
  15. β1 receptor antagonist

    Atenolol is a selective β1 receptor antagonist.
  16. β1-adrenergic receptor antagonist

    Practolol is a potent and selective β1-adrenergic receptor antagonist. Practolol can be used for the research of cardiac arrhythmias.
  17. β-adrenergic receptor (βAR) antagonist

    (R)-Propranolol hydrochloride is a less active enantiomer of the β-adrenoceptor antagonist propranolol. Propranolol 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.

  18. β2-adrenergic agonist

    Clenproperol is a β2-adrenergic agonist.
  19. 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.
  20. 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.
  21. β2-adrenergic receptor agonist

    Levosalbutamol tartrate(levalbuterol) is the R-enantiomer of the short-acting β2-adrenergic receptor agonist salbutamol.
  22. 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.
  23. 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.
  24. α2-adrenoceptor antagonist

    Atipamezole is a synthetic α2-adrenoceptor antagonist with a Ki of 1.6 nM.
  25. 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.
  26. β1-adrenergic receptor blocker

    Bucindolol is a β1-adrenergic receptor blocker, with intrinsic sympathomimetic activity, used in the research of heart failure.
  27. 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.
  28. β-adrenoceptor antagonist

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

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

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

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

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

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

    Spirendolol is a β adrenergic receptor antagonist.
  35. 5-HT2A/α1-adrenergic receptor antagonist

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

    Tiodazosin is a potent competitive postsynaptic alpha adrenergic receptor antagonist.
  37. 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.
  38. β-adrenergic agonist

    Imoxiterol (RP 58802B) is a β-adrenergic agonist.
  39. 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.
  40. β-adrenoceptor blocking agent

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

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

    Formoterol is a long-acting β2 agonist used in the management of asthma and chronic obstructive pulmonary disease (COPD).
  43. 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.
  44. 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.
  45. 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.
  46. Metabolites of tulobuterol

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

    Desvenlafaxine succinate hydrate is an antidepressant of the serotonin-norepinephrine reuptake inhibitor (SNRI).
  48. 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.
  49. 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.
  50. 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.

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