Voltage-gated calcium (Ca(V)) channels deliver Ca(2+) to trigger cellular functions ranging from cardiac muscle contraction to neurotransmitter release. The mechanism by which these channels select for Ca(2+) over other cations is thought to involve multiple Ca(2+)-binding sites within the pore. Although the Ca(2+) affinity and cation preference of these sites have been extensively investigated...

A series of N,N'-disubstituted-2-nitroethene-1,1-diamine and N,N'-disubstituted- N''-cyanoguanidine derivatives were prepared and evaluated for in vivo analgesic activity. The blood brain barrier (BBB) VolSurf model was used to predict the BBB permeation profiles of our synthesized compounds. Some compounds show both remarkable analgesic activity and good BBB permeation profiles, and these comp...

PURPOSE To evaluate porcine sclera as a model of human sclera for in vitro studies of transscleral drug delivery of both low and high molecular weight compounds. METHODS Human and porcine scleras were characterized for thickness and water content. The tissue surface was examined by scanning electron microscopy (SEM), and the histology was studied with hematoxylin-eosin staining. Comparative p...

comNode classification within Membrane Residue Curves (M-RCMs) currently hinges on Lyapunov’s Theorem and therefore the computation of mathematically complex eigenvalues. This paper presents an alternative criterion for the classification of nodes within M-RCMs based on the total membrane flux at node compositions. This paper demonstrates that for a system exhibiting simple permeation behaviour...

The effects of more than 300 kinds of food extracts on intestinal permeability were investigated in Caco-2 cells with the use of model compounds: Lucifer Yellow (LY) for the paracellular pathway, Fluorescein (FC) for the monocarboxylic acid transporter-mediated pathway, and Rhodamine 123 (RH) for the p-glycoprotein-mediated efflux pathway. With several extracts of increasing or decreasing LY pe...

Recently a cartilage growth finite element model (CGFEM) was developed to solve nonhomogeneous and time-dependent growth boundary-value problems (Davol et al., 2008, "A Nonlinear Finite Element Model of Cartilage Growth," Biomech. Model. Mechanobiol., 7, pp. 295-307). The CGFEM allows distinct stress constitutive equations and growth laws for the major components of the solid matrix, collagens ...

The potassium channel from Streptomyces lividans (KcsA) is an integral membrane protein with sequence similarity to all known potassium channels, particularly in the selectivity filter region. A recently proposed model for ion channels containing either n or (n-1) single-file ions in their selectivity filters [P. H. Nelson, J. Chem. Phys. 177, 11396 (2002)] is applied to published KcsA channel ...

Background The present work was conducted to prepare and evaluate transdermal patches with optimization of suitable polymeric blend of poly(meth) acrylates (Eudragit®) (Ammonio Methacrylate Copolymer Ph Eur) for sustained transdermal delivery of glimepiride. Method Polymeric matrix transdermal films were prepared by using Ammonio Methacrylate Copolymer Ph Eur RL 100 and Ammonio Methacrylate C...

objective(s):drug delivery through the skin can transfer therapeutic levels of drugs for pharmacological effects. analgesics such as nsaids have gastrointestinal side effects and topical dosage forms of these drugs are mainly preferred, especially for local pains. meloxicam is one of nsaids with no topical form in the market. in this research, we attempted to quantify the skin permeation of a m...

In the field of commercial manufacture, the permeation flaw detection is always used to inspect the surface quality of production. In conventional permeation flaw detection, the fluorescence or none fluorescence penetrant infiltrate the surface of the work and the developed image is used for flaw detection. The infiltration capacity of penetrant is very important to permeation flaw detection. I...