1.1. We investigated the effects of short- and long-term administration of efonidipine hydrochloride (NZ-105), 1,4-dihydropyridine derivative, in conscious spontaneously hypertensive rats (SHR).2.2. Oral administration of NZ-105 for 12 weeks caused diuretic and natriuretic effects, which were no...

1.We investigated the renal protective effect of efonidipine hydrochloride (efonidipine, NZ-105) in STZ-induced spontaneously hypertensive rats (SHRs, 8 weeks of age). Diabetic SHRs were treated with 15 mg/kg/day of efonidipine for 12 weeks.2.The dosage of efonidipine was chosen after preliminar...

The contribution of the T-type Ca2+ current to cardiac pacemaking was examined in isolated right atrial tissue from the mouse, guinea pig, and rabbit using a specific blocker, R(−)-efonidipine. At 10−6 M, R(-)-efonidipine produced negative chronotropy, which was prominent in the mouse and small ...

BackgroundAlthough several lines of recent studies fail to demonstrate the beneficial action of calcium antagonists, a novel dihydropyridine efonidipine, which possesses dilatory action of both afferent and efferent arterioles and, therefore, shares the renal microvascular action with angiotensi...

.Transforming growth factor beta-1 (TGF-β1) plays a critical role in progression of cardiac fibrosis, which may involve intracellular calcium change. We examined effects of efonidipine, a dual T-type and L-type calcium channel blocker (CCB), on TGF-β1–induced fibrotic changes in neonatal rat ...

The effect of S(+)-efonidipine on sinus node action potential and calcium channel α-subunits was examined. The slope of the phase 4 depolarization of isolated rabbit sinus node tissue was significantly reduced by S(+)-efonidipine (1 μM), slightly reduced by nifedipine (1 μM), but was not affe...

Although disturbance of cardiac Ca2+ regulation is involved in the pathophysiology of iron-overload cardiomyopathy, the obvious mechanisms involved in the dysregulation of iron-induced cardiac Ca2+ are unclear. Moreover, the roles of the iron chelator deferiprone and the T-type calcium channel b...

The effect of efonidipine, a commercially available antihypertensive drug and Ca2 + channel inhibitor, on voltage-dependent K+ (Kv) channels was studied in freshly isolated rabbit coronary arterial smooth muscle cells using the whole-cell patch clamp technique. The amplitude of Kv current was de...

Efonidipine hydrochloride is a new generation dihydropyridine Ca2+ channel blocker designed to inhibit both T-type and L-type Ca2+ channels. Efonidipine possesses a chiral carbon and is clinically administered as a racemate. In the present study, an enantioselective and sensitive LC–MS/MS metho...

Efonidipine hydrochloride is a new generation dihydropyridine calcium channel blocker designed to inhibit both T-type and L-type calcium channels. For the first time, a simple and robust LC–MS/MS method was developed for the determination of efonidipine in human plasma over the range of 0.100–...

The aim of this study was to improve the oral bioavailability of a practically insoluble drug, efonidipine hydrochloride (EFH), by agglomeration in acid solution/gastric fluid. The EFH nanosuspension was prepared by the wet-milling method with F68 as a dispersing agent, SDS as an auxiliary stabi...

Drug absorption into the body is known to be greatly affected by the solubility of the drug itself. The active pharmaceutical ingredient efonidipine hydrochloride ethanolate (NZ-105) is a novel 1,4-dihydropyridine calcium antagonist that has a very low solubility in water. It is classified as a ...

Efonidipine is a dual L-/T- type calcium channel blocker with a slow onset of action and a long lasting effect that exibihits antihypertensive and nephroprotective effects.differs from most other DHPs which can induce reflex tachycardia. Efonidipine reduces blood pressure without decreasing card...

T helper 9 (TH9) cells are considered as newly classified helper T cells that have an important role in the regulation of immune responses. Since these cells preferentially produce IL-9, these cells are termed TH9 cells. Recently, the role of TH9 and its signature cytokine (IL-9) has been invest...

Rat-liver mitochondria were incubated with cis-9,10-methylene hexadecanoic or cis-9,10-methylene octadecanoic acids. The mitochondria converted these longchain cyclopropane fatty acids to short-chain cyclopropane fatty acids. The methylene carbon of the cyclopropane ring of cis-9,10-methylene he...

The effects of fatty acids on oppositely charged polyelectrolyte–surfactant interactions are experimentally investigated. It was observed that dodecanoic (lauric) acid (LA) disrupts the well-established reported interaction between the anionic surfactant sodium dodecylethersulfate (SDES) and th...

In this study, a bio-based efficient plasticizer (acetylated-fatty acid methyl ester-citric acid ester, AC-FAME-CAE) for poly(vinyl chloride) (PVC) was synthesized by using waste cooking oil and citric acid as raw materials in very user-friendly approaches. Its structure was characterized by FTI...

RhoB, one of the upstream signaling proteins of the phosphatidylinositol-3-kinase (PI3K)/Akt pathway, is frequently mutated in human cancer. Based on a piperazine alkyl derivative that induced apoptosis via up-regulation of RhoB, we synthesized novel aliphatic amido/sulfonamido-quaternary ammoni...

High titer, productivity and yield are the main pre-requisites of an efficient lactic acid production process. However, the hyperosmotic stress inhibits cell metabolism in the later phase of fermentation. In this study, an osmotic-tolerant mutant named Lactobacillus paracasei NCBIO01-M2 was obta...

The organic modification of Na-montmorillonite (Na-MMT) clay by a reaction with the sodium salts of octadecanoic acid (SOD) and dodecanoic acid (SDD) was studied for the production of effectively intercalated and organophilic clays. The results of X-ray diffractometer (XRD) analysis reveal that ...