Catalog Number: 3517
Chemical Name: (±)-[2R*(1S*5S*(S*))]-α,α'-[Iminobis(methylene)bis(6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol)
Biological Activity
Highly selective β1-adrenoceptor antagonist (Ki values are 0.88, 20, 44, 700, 1160, 2400 and 4000 nM at β1, 5-HT1A, β2, 5-HT2, α1, H1 and D2 receptors respectively). Induces vasodilation via a nitric oxide- and cGMP-dependent mechanism (EC50 = 11.36 μM in renal arteries) and displays antihypertensive activity in vivo. GRK/β -arrestin biased agonist at the β2 adrenoceptor.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO and to 10 mM in ethanol
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. The �-blocker Nebivolol Is a GRK/�-arrestin biased agonist.
    Erickson et al.
    PLoS One, 2013;8:e71980
  2. The receptor binding profile of the new antihypertensive agent nebivolol and its stereoisomers compared with various β-adrenergic blockers.
    Pauwels et al.
    Mol.Pharmacol., 1988;34:843
  3. Nebivolol induces a hyperpolarizing effect on smooth muscle cells in the mouse renal artery by activation of beta-2-adrenoceptors.
    Georgescu et al.
    Pharmacology, 2008;81:110

The citations listed below are publications that use Tocris products. Selected citations for Nebivolol hydrochloride include:

Showing Results 1 - 1 of 1

  1. Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands.
    Authors: Littmann Et al.
    Brain Res
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