Search results for "farmakologia"
showing 4 items of 4 documents
Pharmacological activity of C10-substituted analogs of the high-affinity kainate receptor agonist dysiherbaine
2010
Kainate receptor antagonists have potential as therapeutic agents in a number of neuropathologies. Synthetic modification of the convulsant marine toxin neodysiherbaine A (NDH) previously yielded molecules with a diverse set of pharmacological actions on kainate receptors. Here we characterize three new synthetic analogs of NDH that contain substituents at the C10 position in the pyran ring of the marine toxin. The analogs exhibited high-affinity binding to the GluK1 (GluR5) subunit and lower affinity binding to GluK2 (GluR6) and GluK3 (GluR7) subunits in radioligand displacement assays with recombinant kainate and AMPA receptors. As well, the natural toxin NDH exhibited ∼100-fold selectivi…
Exploring kainate receptor pharmacology using molecular dynamics simulations
2010
Ionotropic glutamate receptors (iGluRs) are enticing targets for pharmaceutical research; however, the search for selective ligands is a laborious experimental process. Here we introduce a purely computational procedure as an approach to evaluate ligand–iGluR pharmacology. The ligands are docked into the closed ligand-binding domain and during the molecular dynamics (MD) simulation the bi-lobed interface either opens (partial agonist/antagonist) or stays closed (agonist) according to the properties of the ligand. The procedure is tested with closely related set of analogs of the marine toxin dysiherbaine bound to GluK1 kainate receptor. The modeling is set against the abundant binding data …
Sappihappojen aminohappo- ja oligopeptidikonjugaatit
2012
Kirjallisen osion tarkoituksena on esitellä sappihappojen aminohappo- ja oligopeptidikonjugaatteja ja niiden synteettistä valmistusta sekä perehtyä niiden erilaisiin käyttömahdollisuuksiin. Sappihappojen aminohappo- ja oligopeptidikonjugaateista valmistetut makrosykliset rakenteet voivat toimia mm. rakenneosina lääkekehityksessä, materiaalikemiassa ja supramolekyylikemiassa. Sappihappo- ja aminohappokonjugaatteja on tutkittu myös ionikuljettimina, reseptoreina ja gelaattoreina.Tutkielman kokeellisen osion tarkoituksena oli valmistaa sappihappojen aminoetyy-liamidien ja L-proliinin konjugaatteja sekä tutkia niiden geelinmuodostusominaisuuksia eri liuottimissa.
Time is the key – Music and Altered States of Consciusness
2011
Introduction: In this chapter, I will summarize the literature on how music and altered states of consciousness (ASC) are connected. Essential aspects include induction and expression of emotions and rhythmic body movements to music and how an altered experience of music is connected to states of altered temporality. Winkelman (2000) stressed the human capacity for experiencing ASC as a fundamental biological function. Studies on brain functions of altered music experience and temporality (Fachner, 2006b, 2009; Shanon, 2001) convey the natural bases of these phenomena, which have been utilized in shamanistic practice for ages. As Rouget suggested: To shamanize, in other words to sing and da…