PURPOSE OF REVIEW To review goals of antihypertensive treatment in chronic kidney disease in the context of what role calcium antagonists play toward reducing progression of kidney disease. RECENT FINDINGS All recently published guidelines recommend a blood pressure goal of less than 130/80 mmHg in patients with chronic kidney disease. Use of calcium antagonists is not recommended as part of ...

reactions of 1 ,zdihydropyridines (la-c) and 1,4-dihydropyridines (2a-c) in the presence of benzyne (3) under thermal conditions, and in the case of (2c) under photochemical conditions, have been investigated. benzyne acts as an oxidizing agent to convert dihydropyridine (la) and (2a) to the corresponding pyridine (4) or adds as a dienophile to (lb-c).

Ca2+ channels are voltage-gated ion present in the membrane of most excitable cells. The nomenclature for Ca2+channels was proposed by [127] and approved NC-IUPHAR Subcommittee on [70]. Most form hetero-oligomeric complexes. α1 subunit is pore-forming provides binding site(s) practically all agonists antagonists. 10 cloned α1-subunits can be grouped into three families: (1) high-voltage activat...

Recent studies have indicated that 1, 4-dihydropyridine-3, 5-dicarboxamidederivativesshow significant anti-tubercular activity. In this research, new derivatives of 1, 4-dihydropyridine were designed and synthesized using Hantzsch condensation in which dicyclohexyl and different dicyclohexylcarbamoylwere substituted at C-3 and C-5 positions of the DHP ring.In addition, 4 (5)-chloro-2-methyl-5 (...

The concept of molecular hybridization led us to discover a novel series of coumarin-dihydropyridine hybrids that have potent osteoblastic bone formation in vitro and that prevent ovariectomy-induced bone loss in vivo. In this context, among all the compounds screened for alkaline phosphatase activity, four compounds 10, 14, 18, and 22 showed significant activity at picomolar concentrations. A ...

3-Amino-3-thioxopropanamide (1) reacted with ethyl acetoacetate to form 6-hydroxy-4-methyl-2-thioxo-2,3-dihydropyridine-3-carboxamide (2), which reacted with α-haloketones 3 to produce 2,3-disubstituted-8-hydroxy-6-methyl-2H,5H-pyrido[3,2-f]-[1,4]thiazepin-5-ones 4a-c. Benzoylation of 4c led to the formation of the dibenzoate derivative 9. Compounds 4a-c could be prepared stepwise through the f...

In smooth muscle, the gating of dihydropyridine-sensitive Ca(2+) channels may either be stochastic and voltage dependent or coordinated among channels and constitutively active. Each form of gating has been proposed to be largely responsible for Ca(2+) influx and determining the bulk average cytoplasmic Ca(2+) concentration. Here, the contribution of voltage-dependent and constitutively active ...

Leishmaniasis and Chagas disease are neglected parasitic diseases endemic in developing countries; efforts to find new therapies remain a priority. Calcium channel blockers (CCBs) are drugs in clinical use for hypertension and other heart pathologies. Based on previous reports about the antileishmanial activity of dihydropyridine-CCBs, this work aimed to investigate whether the in vitro anti-Le...

A pharmacologically active agent was easily extracted by aqueous or organic solvents from laboratory plastic tubes (Falcon Blue Max) and has been chemically identified as bis(2,2,6,6-tetramethyl-4-piperidyl) sebacate. This compound (approximately 12 micrograms per tube approximately 25 nmol) blocked 1,4-dihydropyridine-sensitive 45Ca2+ uptake into GH3 cells with an IC50 value of 3.6 microM, inh...