A Review on Barnidipine: A Novel Calcium Antagonist

Sakai, Toshiharu; Teramura, Toshio; Okamiya, Hideaki; Inagaki, Osamu

doi:10.1111/j.1527-3466.1997.tb00336.x

Cited by 8 publications

(8 citation statements)

References 40 publications

(29 reference statements)

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“…For example, it was established that (−)-S-amlodipine [10], (+)-S-manidipine, and [11] (−)-S-nitrendipine [11,12] were more potent calcium channel blockers than the respective opposite enantiomers (Figure 2). The same occurrence was described for barnidipine, where the most active was (+)-S,S-isomer (Figure 1) [13]. The opposite effects on function of L-type channels were reported, for example, for derivative PN 202-791 and BAYK8644, where (−)-R-enantiomers of PN 202-791 and (+)-R-BAYK8644 were calcium channel blockers, while the corresponding (+)-S-PN 202-791 and (−)-S-BAYK8644 enantiomers were calcium channel agonists (Figure 3) [14][15][16].…”

Section: Introductionsupporting

confidence: 76%

Section: Introductionsupporting

confidence: 73%

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Recent Approaches to Chiral 1,4-Dihydropyridines and their Fused Analogues

et al. 2020

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The purpose of this review is to highlight recent developments in the synthesis of chiral 1,4-dihydropyridines and their fused analogues. 1,4-Dihydropyridines are among the most active calcium antagonists that are used for the treatment of hypertension. Enantiomers of unsymmetrical 1,4-dihydropyridines often show different biological activities and may have even an opposite action profile. Hantzsch synthesis usually produces racemic mixtures of unsymmetrical 1,4-dihydropyridines. Therefore, the development of stereoselective synthesis of 1,4-dihydropyridines is one of the priorities of medicinal chemistry. Over the years, numerous methodologies have been developed for the production of enantiopure 1,4-dihydropyridines, such as stereoselective synthesis using chiral auxiliaries and chiral cyclocondensation partners, chromatographical methods, resolution of diastereomeric 1,4-dihydropyridine salts, enzyme catalysed kinetic resolution, or asymmetrisation of ester groups of 1,4-dihydropyridines. These approaches have been studied in detail and are relatively well established. The catalytic asymmetric approach holds the greatest promise in delivering the most practical and widely applicable methods. Substantial progress has been made toward the development of enantioselective organocatalytic methods for the construction of the chiral dihydropyridines. However, most of them do not provide a convenient way to pharmacologically important 1,4-dihydropyridine-3,5-dicarboxylates. Organocatalytic enantioselective desymmetrisation of prochiral 1,4-dihydropyridine-3,5-dicarbaldehydes also has great promise in the synthesis of pharmacologically important 1,4-dihydropyridine-3,5-dicarboxylates.

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Section: Introductionsupporting

confidence: 76%

Section: Introductionsupporting

confidence: 73%

Recent Approaches to Chiral 1,4-Dihydropyridines and their Fused Analogues

et al. 2020

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“…The drug barnidipine, a calcium channel blocker and an antihypertensive agent was short listed because of its significant interaction with M pro ( 27 ). In the current study, it was a hit-drug can be screened for inhibiting replication of SARS-CoV-2 in COVID-19.…”

Section: Discussionmentioning

confidence: 99%

Targeting SARS-CoV-2 Main Protease: A Computational Drug Repurposing Study

Baby

Maity

Mehta

et al. 2021

Archives of Medical Research

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Background and Aims Severe Acute Respiratory Syndrome Coronavirus-2 (SARS-CoV-2) induced Novel Coronavirus Disease (COVID-19) has currently become pandemic worldwide. Though drugs like remdesivir, favipiravir, and dexamethasone found beneficial for COVID-19 management, they have limitations clinically, and vaccine development takes a long time. The researchers have reported key proteins which could act as druggable targets. Among them, the major protease M pro is first published, plays a prominent role in viral replication and an attractive drug-target for drug discovery. Hence, to target M pro and inhibit it, we accomplished the virtual screening of US-FDA approved drugs using well-known drug repurposing approach by computer-aided tools. Methods The protein M pro , PDB-ID 6LU7 was imported to Maestro graphical user interphase of Schrödinger software. The US-FDA approved drug structures are imported from DrugBank and docked after preliminary protein and ligand preparation. The drugs are shortlisted based on the docking scores in the Standard Precision method (SP-docking) and then based on the type of molecular interactions they are studied for molecular dynamics simulations. Results The docking and molecular interactions studies, five drugs emerged as potential hits by forming hydrophilic, hydrophobic, electrostatic interactions. The drugs such as arbutin, terbutaline, barnidipine, tipiracil and aprepitant identified as potential hits. Among the drugs, tipiracil and aprepitant interacted with the M pro consistently, and they turned out to be most promising. Conclusions This study shows the possible exploration for drug repurposing using computer-aided docking tools and the potential roles of tipiracil and aprepitant, which can be explored further in the treatment of COVID-19.

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“…The reduction in peripheral resistance brought about by barnidipine results in blood pressure lowering. When using barnidipine, the anti-hypertensive effect remains during the entire 24-hour dose interval 4 . Use of barnidipine in chronic treatment does not lead to an increase in basic heart frequency.…”

Section: Introductionmentioning

confidence: 99%

Simultaneous Estimation and Validation of Lc-MS Method for the Determination of Barnidipine in Human Plasma: Its Stability Indicating

Talari¹,

Kumar²

2019

RJC

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Various LC-MS/MS and RP-HPLC methods are reported in the literature for the estimation of barnidipine individually. According to the literature survey, there is no regulatory method reported for the estimation of barnidipine by LC-MS/MS in human plasma either in literature and pharmacopeia. Hence, in this study a Novel LC/MS/MS method was optimized and validated for simultaneous estimation and validation of barnidipine in human plasma in accordance with the USFDA, EMEA and other relevant regulatory guidelines. Bamidipine is an anti-hypertensive drug belonging to the dihydropyridine (DHP) group of calcium antagonists. It is available in a modified-release formulation which has a gradual onset of action and is effective in a single daily oral dose of 10 to 20 mg. Bamidipine has selective action against cardiovascular calcium antagonist receptors and its anti-hypertensive action is related to the reduction of peripheral vascular resistance secondary to its vasodilatory action. The clinical anti-hypertensive efficacy of barnidipine is similar to that of other DHP calcium antagonists such as nitrendipine and amlodipine, and anti-hypertensives belonging to other drug classes such as atenolol and enalapril. Barnidipine has been found to be as efficacious and well tolerated as hydrochlorothiazide in the management of hypertension in elderly patients. Barnidipine is generally well tolerated. As with other DHP calcium antagonists, vasodilator adverse events such as a headache, flushing and peripheral oedema account for most of the adverse events reported with its use and are usually transient. Oedema is less frequent than with amlodipine and nitrendipine. Its use is not associated with reflex tachycardia. The validated regulatory bioanalytical method for estimation of barnidipine by LC-MS/MS in human plasma is useful for analysis of subject samples to support generic ANDA applications for different regulatory authorities for introducing new generic drugs in affordable rates for the patients. Also the validated regulatory method would be used as supporting literature for developing and validating better method in CROs and clinical research organizations to support new generic drugs.

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A Review on Barnidipine: A Novel Calcium Antagonist

Cited by 8 publications

References 40 publications

Recent Approaches to Chiral 1,4-Dihydropyridines and their Fused Analogues

Recent Approaches to Chiral 1,4-Dihydropyridines and their Fused Analogues

Targeting SARS-CoV-2 Main Protease: A Computational Drug Repurposing Study

Simultaneous Estimation and Validation of Lc-MS Method for the Determination of Barnidipine in Human Plasma: Its Stability Indicating

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