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At least 505 records · Page 28Linked to original sources
PubMed1980

Physical model evaluation of topical prodrug delivery--simultaneous transport and bioconversion of vidarabine-5'-valerate III: Permeability differences of vidarabine and n-pentanol in components of hairless mouse skin.

The permeation behavior of 3H-vidarabine (3H-9-beta-D-ara-binofuranosyladenine) and 14C-n-pentanol through different strata of hairless mouse skin was studied using a diffusion cell at 37 degrees under steady-state conditions. Partition coefficients for the skin components verus 0.9% aqueous NaCl solution also were obtained. Various skin preparations including full-thickness skin, cellophane-stripped skin, and dermis membranes of different thicknesses were employed. The dermis membranes were considered to be diffusionally homogenous, and the product of the permeability coefficient and the thickness was taken as the apparent diffusivity. The apparent diffusivities for both compounds investigated were independent of thickness. Therefore, it was concluded that the molecular diffusivity is constant throughout the dermis. Comparisons of permeability coefficients in various strata of the skin revealed that, while the stratum corneum is the major diffusional barrier, the epidermis appears to be significantly less permeable than the dermis.

Administration, Topical↗
PubMed1985

Threshold effects of N-methyl D-aspartate (NMDA) and 2-amino 5-phosphono valeric acid (2APV) on the spontaneous activity of neocortical single neurones in the urethane anaesthetised rat.

Spontaneous activity of single neurones in neocortex was sampled using pairs of microelectrodes in rats anaesthetised with urethane. In confirmation of previous studies, many cells recorded from middle layers characteristically fired in bursts, the onset times of which were synchronous both unilaterally and bilaterally. Iontophoresis of 2APV onto such cells either caused an abolition of bursts or a reduction in spikes per burst. In the latter case action potentials which occurred later in the burst were preferentially abolished. Iontophoresis of NMDA onto the same cells caused a prolongation of bursts with minimal effect on intraburst interspike interval. In interactive trials with the two drugs the effect of NMDA could be abolished by 2APV, and NMDA counteracted the effect of 2APV. It is concluded that spontaneous burst generation in neocortex during urethane anaesthesia is generated through a cortical NMDA/2APV-sensitive receptor mechanism.

Action Potentials↗