Delving into the Latest Updates on Nisoldipine with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

Nisoldipine (JAN/USAN/INN), isobutyl methyl 2,6-dimethyl-4-(2-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate

+ [14]

Target

Cav2.1

Action

inhibitors

Mechanism

Cav2.1 inhibitors(calcium voltage-gated channel subunit alpha1 A inhibitors)

Therapeutic Areas

Cardiovascular Diseases

Active Indication

Hypertension

Inactive Indication-

Originator Organization

Shionogi & Co., Ltd.

Active Organization

Covis Pharma Holdings BV

Inactive Organization-

Drug Highest PhaseApproved

First Approval Date

United States (02 Feb 1995),

Hypertension

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC20H24N2O6

InChIKeyVKQFCGNPDRICFG-UHFFFAOYSA-N

CAS Registry63675-72-9

Obesity and metabolic disorders are rising global health concerns, emphasizing the need for effective dietary interventions. High-viscosity dietary fibers such as bacterial cellulose (BC) and guar gum (GG) have unique properties that may complement each other in modulating gut microbiota and metabolic health. This study investigates their effects in high-fat diet-fed mice. BC and GG increase Bacteroides, which degrade polysaccharides and produce short-chain fatty acids (SCFAs), supporting metabolic health. BC enhances bile acid excretion and enriches Faecalibaculum, Duncaniella, and Paramuribaculum, promoting gut barrier integrity and reducing inflammation, potentially improving bile acid turnover and lipid metabolism. GG more effectively increases butyrate production by enhancing butyrate-producing bacteria, such as Clostridium XIVa and Kineothrix, and promotes Bifidobacterium, strengthening anti-inflammatory effects and gut barrier function. Both fibers upregulate bile acid biosynthesis, but BC's non-fermentable nature leads to higher bile acid excretion, while GG's fermentation causes lower excretion and broader liver metabolic changes. Both fibers reduce body weight, fat accumulation, and cholesterol levels, highlighting their potential in managing obesity and metabolic disorders. The complementary effects of BC and GG underscore the importance of fiber diversity for targeted dietary strategies to improve metabolic health.

13 Dec 2024·ACS Pharmacology & Translational Science

Repurposing Drugs and Synergistic Combinations as Potential Therapies for Inhibiting SARS-CoV-2 and Coronavirus Replication

Article

Author: Anton, Anaïs ; Farahani, Majid D. ; Ayotte, Yann ; Boulon, Richard ; Chatel-Chaix, Laurent ; LaPlante, Steven R. ; Lamarre, Alain ; Iddir, Mustapha ; Charpentier, Tania ; Broquière, Mathilde ; Woo, Simon ; Mazeaud, Clément

Drug repurposing can serve an important role in rapidly discovering medicament options for emerging microbial pandemics. In this study, a pragmatic approach is demonstrated for screening and testing drug combinations as potential broad-spectrum therapies against SARS-CoV-2 and other betacoronaviruses. Rapid cell-based phenotypic small molecule screens were executed using related common-cold-causing HCoV-OC43 betacoronavirus to identify replication inhibitors from a library of drugs approved by regulatory agencies for other indications. Given the best inhibitors, an expedient checkerboard strategy then served to identify synergistic drug combinations. These combinations were then validated using more challenging assays involving SARS-CoV-2 and variants. Promising drug combinations against multiple viral variants were discovered and involved Tilorone with Nelfinavir or Molnupiravir.

02 Sep 2024·Journal of The Electrochemical Society

The Electrochemistry of Nitro Compounds from a Bibliometric Approach

Author: La-Scalea, Mauro Aquiles ; La Scalea, Mauro Aquiles ; Brito, Charles de Lima ; Chiavassa, Luisa Donatto

The heterocyclic and aromatic nitro compounds are industrially and commercially important chemicals, used in drugs, explosives, pesticides, and dyes. Despite their economic importance, the advent of these chemicals also brought serious human health and environmental problems due to their toxic characteristics as contaminants and pollutants. The nitro group is catalyzed in vivo by nitroreductases promoting a six-electron reduction to form sequentially the nitro radical anion, nitroso-, N-hydroxylamino and amino-functional groups. These reactions can be electrochemically reproduced, involving the development of analytical methods and electrochemical sensors, degradation and removal of organic compounds in effluents, corrosion studies, and studies of action mechanism of drugs on DNA bases. In this sense, a bibliometric analysis has been performed based on the Web of Science Core Collection in conjunction with VOSviewer software for generating network visualizations. This research covered the database until 2023, describing the main research areas and the annual publication trends, the collaborations and contributions among countries and research institutions, in addition to identifying the most cited articles, hotspots, and the analysis of evolution and relevance of keywords. This investigation made it possible to recognize the main research focuses and what is under development, providing a comprehensive overview on electrochemistry of nitro compounds.

100 Deals associated with Nisoldipine

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
D00618	Nisoldipine	C08CA07	DB00401

R&D Status

10 top approved records.

Login

to view more data

Indication	Country/Location	Organization	Date
Hypertension	United States	Covis Pharma Holdings BV	02 Feb 1995

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT00311870 (Pubmed \| Diabetes Care)	Phase 4	Type 1 diabetes mellitus with established diabetic nephropathy	48	Nisoldipine	(luxilztyyy) = qznuzpulmn ufcyhvmzkd (pfriamprmz ) View more	-	01 Dec 2000
				Lisinopril	(luxilztyyy) = mwbfueorrk ufcyhvmzkd (pfriamprmz ) View more