Dihydropyridines as Calcium Channel Blockers: An Overview

Abstract

A heartfelt tribute to the memory of Professor AsimaChatterjee, the legendary scientist-teacher-humanitarian, on the occasion of her birth centenary . AbstractCardiovascular disease remains one of the leading causes of death in the United States. It is estimated that 1 in every 3 American adults suffer from high blood pressure. Hypertension, a precursor to most cardiovascular diseases, continues to grow at an alarming rate and is seldom managed carefully. Attempts have been made to manage hypertension and reduce the morbidity and mortality of the cardiovascular organ through methods including diets, increased amount of exercise, and medications. Many commercial drugs have been derived from dihydropyridine due to its antihypertensive property. Dihydropyridine derivatives work by acting as calcium channel blockers blocking the intake of calcium ions into the vascular smooth muscle and, to a lesser extent, cardiac muscles. Dihydropyridine moiety is well-known in pharmacology as L-type calcium channel blockers, which is extremely important since it treats hypertension in people who suffer from it. It is also highly important to understand the antagonists of calcium in the arterial hypertension. A brief overview is presented in this mini-review.

Opposing Responses of the Calcium Channel Blocker Nicardipine to Vascular Stiffness in the Elastic and Muscular Arteries in Rabbits

“…In this study, we observed a significant decrease in TPR, BP, and HR and a significant increase in CO during nicardipine infusion. These findings are almost consistent with those of other investigators, except that with regard to HR 22,24) . Satoh 26) also reported that a high dose of nicardipine inhibited tachycardia induced by sympathetic nerve stimulation mainly by suppressing slow inward Ca 2 currents.…”

“…Nicardipine, a calcium channel blocker, relaxes the VSMCs of the muscular arteries and arterioles by blocking L-type and T-type Ca 2+ channels 16,17) , which reduces peripheral vascular resistance, leading to a decrease in BP 22) . Nicardipine also dilates the coronary artery 23) , which results in an improved left ventricular function without producing any negative ionotropic effects 24) .…”

Synthesis and Crystal Structure of Benzyl 4-(2-fluoro-4-(trifluoromethyl)phenyl)- 2,6,6-trimethyl-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate and Its DFT Analysis Combined with Bond Order Modeling in Terms of The Bond Critical Point Quantities

“…Infrared spectra (IR) were recorded on Perkin Elmer Spectrum BX FT-IR (UK) equipped with MIRacle ATR accessory (PIKE Technologies, USA) and were reported in cm −1 . 1 H-NMR and 13 C-NMR spectra were taken in dimethyl sulfoxide (DMSO-d 6 ) solution on a Bruker Ultra Shield Spectrophotometer at 400 MHz using tetramethylsilane (TMS) as internal standard. Chemical shifts were reported in parts per million (ppm).…”

“…Calcium channel modulators operate calcium entry through cells and by that cause cardiological bene ts. As a result of this pharmacological action, they are widely used for the treatment and prevention of cardiovascular diseases [1,2]. Chronic in ammation plays an important role of development of several in ammatory diseases.…”

“…Many 1,4-DHP derivatives have in ammation supressing properties in different cell cultures [5][6][7][8][9][10][11]. Depending on these ndings we designed and synthesized an annulated 1,4-DHP compound, benzyl 4-(2-uoro-4-(tri uoromethyl)phenyl)-2,6,6-trimethyl-5-oxo-1,4,5,6,7,8-hexahydroquinoline-3-carboxylate, and elucidated structure of the compound by IR, 1 H-NMR, 13 C-NMR, HRMS and X-ray crystallography. In vitro studies showed that the compound has supressing activity on immunomodulator pathways, IL-1β, IL-6, TNF-α, NF-κB and TGF-β (Unpublished data).…”