scholarly journals Prenylflavanones as Novel T-Type Calcium Channel Blockers Useful for Pain Therapy

2019 ◽  
Vol 14 (9) ◽  
pp. 1934578X1987344
Author(s):  
Huy Du Nguyen ◽  
Takuya Okada ◽  
Fumiko Sekiguchi ◽  
Maho Tsubota ◽  
Hiroyuki Nishikawa ◽  
...  
Keyword(s):  
Side Effects ◽  
Calcium Channels ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Pain Therapy ◽  
Channel Blocker ◽  
Visceral Pain ◽  
Channel Blockers ◽  
Prenylated Flavonoids ◽  
Structure Activity

Prenylated flavonoids have attracted much attention due to their promising and diverse bioactivities on multitarget tissues. To the best of our knowledge, our recent studies demonstrated first that (2 S)-6-prenylnaringenin (6-PNG), a hop component, blocks Cav3.2 T-type calcium channels (T-channels) and alleviates neuropathic and visceral pain with little side effects; it also indicated first that other natural prenylflavanones (PFVNs), such as sophoraflavanone G and (2 S)-8-PNG, or synthetic 6-PFVNs including (2 R/S)-6-PNG and its derivatives are capable of blocking T-channels and useful for pain therapy. Through the structure-activity relationship studies on the synthetic 6-PFVNs, we identified 6-(3-ethylpent-2-enyl)-5,7-dihydroxy-2-(2-hydroxyphenyl)chroman-4-one (8j or KTt-45) as the most potent blocker of Cav3.2 T-channels. It is interesting to recognize a prenylated flavonoid, belonging to other sub-classes, as a novel T-channel blocker. Therefore, this article will review some of our recent studies to introduce a new branch to researchers studying on prenylated flavonoids.

Electroanalytical Methods for Determination of Calcium Channel Blockers

2019 ◽  
Vol 15 (3) ◽  
pp. 207-218 ◽  
Author(s):  
Fatma Ağın
Keyword(s):  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Channel Blocker ◽  
Heart Diseases ◽  
Dosage Forms ◽  
Channel Blockers ◽  
Electroanalytical Methods ◽  
Pharmaceutical Dosage Forms ◽  
Ischemic Heart Diseases

Background:Calcium Channel Blockers (CCBs) are widely used in the treatment of cardiovascular and ischemic heart diseases in recent years. They treat arrhythmias by reducing cardiac cycle contraction and also benefit ischemic heart diseases. Electroanalytical methods are very powerful analytical methods used in the pharmaceutical industry because of the determination of therapeutic agents and/or their metabolites in clinical samples at extremely low concentrations (10-50 ng/ml). The purpose of this review is to gather electroanalytical methods used for the determination of calcium channel blocker drugs in pharmaceutical dosage forms and biological media selected mainly from current articles.Methods:This review mainly includes recent determination studies of calcium channel blockers by electroanalytical methods from pharmaceutical dosage forms and biological samples. The studies of calcium channel blockers electroanalytical determination in the literature were reviewed and interpreted.Results:There are a lot of studies on amlodipine and nifedipine, but the number of studies on benidipine, cilnidipine, felodipine, isradipine, lercanidipine, lacidipine, levamlodipine, manidipine, nicardipine, nilvadipine, nimodipine, nisoldipine, nitrendipine, diltiazem, and verapamil are limited in the literature. In these studies, DPV and SWV are the most used methods. The other methods were used less for the determination of calcium channel blocker drugs.Conclusion:Electroanalytical methods especially voltammetric methods supply reproducible and reliable results for the analysis of the analyte. These methods are simple, more sensitive, rapid and inexpensive compared to the usually used spectroscopic and chromatographic methods.

scholarly journals Voltage-gated calcium channel blockers for psychiatric disorders: genomic reappraisal

2019 ◽  
Vol 216 (5) ◽  
pp. 250-253 ◽  
Author(s):  
Paul J. Harrison ◽  
Elizabeth M. Tunbridge ◽  
Annette C. Dolphin ◽  
Jeremy Hall
Keyword(s):  
Calcium Channels ◽  
Calcium Channel ◽  
Psychiatric Disorders ◽  
Calcium Channel Blockers ◽  
Channel Blockers ◽  
Risk Genes ◽  
Voltage Gated ◽  
Voltage Gated Calcium Channels ◽  
Voltage Gated Calcium Channel ◽  
Second Use

SummaryWe reappraise the psychiatric potential of calcium channel blockers (CCBs). First, voltage-gated calcium channels are risk genes for several disorders. Second, use of CCBs is associated with altered psychiatric risks and outcomes. Third, research shows there is an opportunity for brain-selective CCBs, which are better suited to psychiatric indications.

scholarly journals Dihydropyridine calcium channel blockers and peripheral side effects

2001 ◽  
Vol 15 (10) ◽  
pp. 745-746 ◽  
Author(s):  
A Sirker ◽  
CG Missouris ◽  
GA MacGregor
Keyword(s):  
Side Effects ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Channel Blockers

Structure–activity study of l-amino acid-based N-type calcium channel blockers

2003 ◽  
Vol 11 (8) ◽  
pp. 1901-1913 ◽  
Author(s):  
Takuya Seko ◽  
Masashi Kato ◽  
Hiroshi Kohno ◽  
Shizuka Ono ◽  
Kazuya Hashimura ◽  
...  
Keyword(s):  
Amino Acid ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Channel Blockers ◽  
Structure Activity

Benzazepinone calcium channel blockers. 3. Synthesis and structure-activity studies of 3-alkylbenzazepinones

1992 ◽  
Vol 35 (4) ◽  
pp. 773-780 ◽  
Author(s):  
Jagabandhu Das ◽  
David M. Floyd ◽  
S. David Kimball ◽  
Keith J. Duff ◽  
Michael W. Lago ◽  
...  
Keyword(s):  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Channel Blockers ◽  
Structure Activity

scholarly journals A Comparative study to assess the effectiveness and safety of cilnidipine versus amlodipine in patients with newly diagnosed essential hypertension: insights from a single centre prospective observational study

2017 ◽  
Vol 6 (3) ◽  
pp. 648
Author(s):  
Ramya Y. S. ◽  
Jayanthi C. R. ◽  
Raveendra K. R. ◽  
Pradeep Kumar B. T.
Keyword(s):  
Blood Pressure ◽  
Essential Hypertension ◽  
Side Effects ◽  
Calcium Channel ◽  
Calcium Channel Blockers ◽  
Channel Blockers ◽  
Newly Diagnosed ◽  
Open Label ◽  
Amlodipine Group ◽  
Pedal Edema

Background: Calcium channel blockers (CCBs) are proposed to play a pivotal role for the management and control of hypertension. Dihydropyridine-type calcium channel blockers (CCBs) like Amlodipine are frequently used because for their strong antihypertensive and minimal adverse side effects. However, it is commonly associated with the causation of pedal edema among the patients. Cilnidipine, which is a novel new generation calcium channel blocker, is presumed to cause lesser pedal edema with a satisfactory clinical control of hypertension along with negligible side effects. This study was carried out to compare clinical effectiveness and safety profile between Amlodipine and Cilnidipine.Methods: A prospective, randomized, open label study of 12 weeks’ duration was conducted amongst 60 patients with newly diagnosed essential hypertension. 30 patients of one group received Tab. Amlodipine 5 mg and 30 patients of same age groups received Tab. Cilnidipine 10mg.Results: There was a highly statistically significant decrease in the level of blood pressure in the Cilnidipine group compared to the Amlodipine group mainly at day 90 (P<0.001). Cilnidipine treated group had a fall in blood pressure of 23 ± 8 mmHg and the Amlodipine group had a decrease in the blood pressure of 12±7mmHg. Additionally, there was also significant reduction in pulse rate in the cilnidipine group. Only 4 patients in the Cilnidipine group developed ankle edema which completely disappeared at the end of 12 weeks of therapy compared to 9 patients in the Amlodipine group which persistently worsened at the completion of the study.Conclusions: Our study concluded that cilnidipine was a well-tolerated anti-hypertensive drug amongst patients with newly diagnosed essential hypertension and associated with minor adverse effects.

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