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 SYNTHESIS METHOD AND INTERMEDIATE COMPOUND THEREOF
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, (2018/06/04)
The present invention relates to nebivolol synthesis method and intermediate compound thereof. Specifically, the present invention relates to a method for synthesizing nebivolol, intermediate compound thereof, and a method for preparing the intermediate compound.
PROCESS FOR PREPARATION OF NEBIVOLOL AND IT'S SALTS
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, (2016/12/07)
The present invention discloses a new process for preparation of Nebivolol or it's pharmaceutically acceptable salt. More particularly, the invention discloses an improved economical process for the preparation of intermediate, 6-fluoro-3,4- dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula – II, converting the 6- fluoro-3,4-dihydro-2H-1-benzopyran-2-carboxaldehyde of Formula – II into mixture of [R*(S*)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran and [R*(R*)]-6-fluoro-3,4-dihydro-2-oxiranyl-2H-1-benzopyran of Formula-V and separation of diastereomers of (R*)-6-Fluoro-3,4-dihydro-2-((S*)-oxiran-2-yl)- 2H-benzopran by forming azeotrope.