152520-56-4 Usage
Description
Nebivolol hydrochloride is a highly selective β1-adrenoceptor antagonist, which is a white to off-white powder. It is known for its selective inhibition of the β1-adrenoceptor with an IC50 of 0.8 nM.
Uses
Used in Pharmaceutical Industry:
Nebivolol hydrochloride is used as a pharmaceutical agent for the treatment of hypertension and heart failure. Its selective action on the β1-adrenoceptor helps in reducing blood pressure and improving heart function without causing significant side effects on the β2-adrenoceptors, which are responsible for bronchodilation and vasodilation.
Used in Cardiovascular Applications:
Nebivolol hydrochloride is used as a cardiovascular agent for the management of various heart-related conditions, such as angina pectoris and arrhythmias. Its selective β1-adrenoceptor antagonism helps in reducing the workload on the heart and improving its efficiency.
Used in Research and Development:
Nebivolol hydrochloride is used as a research compound for studying the role of β1-adrenoceptors in various physiological and pathological processes. Its high selectivity makes it a valuable tool in understanding the mechanisms underlying cardiovascular diseases and developing new therapeutic strategies.
Biological Activity
Highly selective β 1 -adrenoceptor antagonist (K i values are 0.88, 20, 44, 700, 1160, 2400 and 4000 nM at β 1 , 5-HT 1A , β 2 , 5-HT 2 , α 1 , H 1 and D 2 receptors respectively). Induces vasodilation via a nitric oxide- and cGMP-dependent mechanism (EC 50 = 11.36 μ M in renal arteries) and displays antihypertensive activity in vivo .
Biochem/physiol Actions
Nebivolol hydrochloride (NEB) is used as a racemic mixture for clinical studies. It stabilizes membrane and possesses intrinsic sympathomimetic functionality. Nebivolol interaction with π-acceptors (2,3-dichloro-5,6-dicyano-1,4-benzoquinone (DDQ), 2,4-dinitrophenol (DNP) and 2,4,6-trinitrophenol (picric acid; PA)) is useful in the spectrophotometric detection methods.
Check Digit Verification of cas no
The CAS Registry Mumber 152520-56-4 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,5,2,5,2 and 0 respectively; the second part has 2 digits, 5 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 152520-56:
(8*1)+(7*5)+(6*2)+(5*5)+(4*2)+(3*0)+(2*5)+(1*6)=104
104 % 10 = 4
So 152520-56-4 is a valid CAS Registry Number.
InChI:InChI=1/C22H25F2NO4.ClH/c23-15-3-7-19-13(9-15)1-5-21(28-19)17(26)11-25-12-18(27)22-6-2-14-10-16(24)4-8-20(14)29-22;/h3-4,7-10,17-18,21-22,25-27H,1-2,5-6,11-12H2;1H
152520-56-4Relevant articles and documents
Synthesis of intermediate compound and [...] (by machine translation)
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Paragraph 0291, (2020/04/09)
Synthesis of intermediate compounds [a] and [...]. [Solution] a [...], asymmetric epoxidation, sulfonyl halide in the presence of base catalyst by sulfonation, alkylation of amines, such as synthesized by a series of cross-coupling reaction. [Effect] [...] important from the viewpoint of pharmacological value, high efficiency, low cost, and which meets the requirements of industrial, optical isomers may be prepared [...] and develop a method, which is very economical in social benefit. [Drawing] no (by machine translation)
Nebivolol synthetic method and intermediate compounds of the
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Paragraph 0505; 0506, (2018/10/04)
The present invention relates to a synthesis method and an intermediate compound of nebivolol. Specifically the invention relates to the method for synthesizing the nebivolol, the intermediate compound of the nebivolol, and a method for preparing the intermediate compound.
A kind of nebivolol hydrochloride synthetic method
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, (2017/03/28)
The invention discloses a synthetic method of nebivolol. The synthetic method comprises the following steps: by taking a 2-amino-1-(-6-fluoro-2-chromanyl) ethanol diastereomer mixture as an initial raw material, firstly, recrystallizing and separating the 2-amino-1-(-6-fluoro-2-chromanyl) ethanol diastereomer mixture to respectively obtain corresponding diastereomers A and B; carrying out reactions such as diazotization, halogenation and cyclization on the diastereomer B to synthesize an epoxy compound; and then, carrying out a reaction on the obtained epoxy compound and the diastereomer A to obtain nebivolol. The method disclosed by the invention is mild in reaction condition, simple and convenient to operate and short in synthetic line, and is suitable for industrialized batch production of nebivolol.
