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Submit ReviewNebivolol hydrochloride is a 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.
Nebivolol hydrochloride is also offered as part of the Tocriscreen FDA-Approved Drugs. 了解 Tocris 化合物库的更多信息。
分子量 | 441.9 |
公式 | C22H25F2NO4.HCl |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 152520-56-4 |
PubChem ID | 11812257 |
InChI Key | JWEXHQAEWHKGCW-VCVZPGOSSA-N |
Smiles | FC(C=C4)=CC3=C4O[C@@](CC3)([H])[C@H](O)CNC[C@@H](O)[C@]2([H])CCC1=CC(F)=CC=C1O2.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 44.19 | 100 | |
ethanol | 4.42 | 10 |
以下数据基于产品分子量 441.9。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.26 mL | 11.31 mL | 22.63 mL |
5 mM | 0.45 mL | 2.26 mL | 4.53 mL |
10 mM | 0.23 mL | 1.13 mL | 2.26 mL |
50 mM | 0.05 mL | 0.23 mL | 0.45 mL |
参考文献是支持产品生物活性的出版物。
Pauwels et al (1988) The receptor binding profile of the new antihypertensive agent nebi. and its stereoisomers compared with various β-adrenergic blockers. Mol.Pharmacol. 34 843 PMID: 2462161
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
Erickson et al (2013) The beta -blocker nebi. Is a GRK/ beta -arrestin biased agonist. PLoS One 8 e71980 PMID: 23977191
If you know of a relevant reference for Nebivolol hydrochloride, please let us know.
关键词: Nebivolol hydrochloride, Nebivolol hydrochloride supplier, selective, α1-adrenoceptor, beta1-adrenoceptor, b1-adrenoceptor, b1-adrenergic, antagonists, β1-Adrenergic, beta1-Adrenergic, Receptors, Adrenergic, Beta-1, 3517, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Nebivolol hydrochloride 的部分引用包括:
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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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.