Nebivolol hydrochloride

Cat. No. 3517

Nebivolol hydrochloride C22H25F2NO4.HCl [152520-56-4]

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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:
441.9
Formula:
C22H25F2NO4.HCl
Solubility:
Soluble to 100 mM in DMSO and to 10 mM in ethanol
Purity:
>98 %
Storage:
Desiccate at RT
CAS No:
152520-56-4

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.

Certificate of Analysis / Product Datasheet / Safety Data Sheet

Erickson et al (2013) The -blocker Nebivolol Is a GRK/-arrestin biased agonist. PLoS One 8 e71980. PMID: 23977191.

Georgescu et al (2008) Nebivolol induces a hyperpolarizing effect on smooth muscle cells in the mouse renal artery by activation of beta-2-adrenoceptors. Pharmacology 81 110. PMID: 17952013.

Pauwels et al (1988) The receptor binding profile of the new antihypertensive agent nebivolol and its stereoisomers compared with various β-adrenergic blockers. Mol.Pharmacol. 34 843. PMID: 2462161.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products. Selected citations for Nebivolol hydrochloride include:

Littmann et al (2015) Recruitment of β-arrestin 1 and 2 to the β2-adrenoceptor: analysis of 65 ligands. Brain Res 355 183. PMID: 26306764.

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Keywords: Nebivolol hydrochloride, supplier, selective, α1-adrenoceptor, beta1-adrenoceptor, b1-adrenoceptor, b1-adrenergic, antagonists, β1-Adrenergic, beta1-Adrenergic, Receptors, Tocris Bioscience, Adrenergic β1 Receptor Antagonist products

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