Search results for "relationship"

Differential effect of the enantiomers of phenprocoumon and warfarin on the vitamin K1-epoxide/vitamin K1 ratio in rat plasma.

1979

Toxicokinetics of xenobiotics in zebrafish—Comparison between tap and river water

1991

Abstract 1. 1. Uptake and elimination of lindane, 3,4-dichloroaniline, phenol and 4-nitrophenol by the zebrafish Brachydanio rerio were investigated in tap water and in water of the river Rhine. 2. 2. The differences in bioconcentration of chemicals between the two water types did not exceed a factor of 2.5. 3. 3. Elimination kinetics were comparable in tap and river water. 4. 4. It can be concluded that water of the river Rhine does not influence the kinetics of the investigated xenobiotics.

Blockage of collagen binding to integrin α2β1: structure–activity relationship of protein–protein interaction inhibitors

2011

The interaction between the α2β1 integrin and collagen plays a crucial role in the development of pathological conditions, such as thrombus formation and cancer cell metastasis. Accordingly, the α2β1 integrin is a promising target for the development of new drug molecules to treat these diseases. Here, we have designed, synthesized, and measured in vitro a set of novel drug-like compounds that block the protein–protein interactions between α2β1 integrin and collagen. The obtained structure–activity relationship reveals the key features that are required for successful inhibition of this integrin–collagen interaction.

Synthesis of hexahydrocyclopenta[ij]isoquinolines as a new class of dopaminergic agents.

2014

In this study, we have described the synthesis of the tricyclic 1,2,3,7,8,8a-hexahydrocyclopenta [ij]isoquinoline (HCPIQ). Herein, six differently substituted 5,6-dioxygenated-7-phenyl-HCPIQs have been synthesized using a new methodology via (E)-1-styryl-THIQ by Friedel-Crafts cyclization with Eaton's reagent. Results showed that HCPIQs (3, 3a-e) displayed a moderate affinity for D1 dopamine receptors (DR) in the micromolar range, furthermore the catecholic HCPIQs 3a (NH), 3c (NCH3) and 3e (NCH2CHCH2) exhibited outstanding affinity and high selectivity towards D2 DR. Indeed, 3a, 3c and 3e showed Ki values of 29 nM, 13 nM and 18 nM, respectively, and HCPIQs 3a (NH) and 3c (NCH3) displayed a …

Antiasthmatic acetophenones - an in vivo study on structure activity relationship.

1994

The recently isolated acetophenone glucoside androsin, as the major antiasthmatic principle of Picrorhiza kurroa Royle ex Benth. (Scrophulariaceae), was used as a lead compound for detailed structure-activity relationship studies. More than 25 synthesized or commercially available acetophenones with modified substitution patterns were screened in the Plethysmographic guinea pig model using PAF and/or ovalbumin as challenging agents for the generation of bronchial constriction. Whereas the aglycones in most cases were more effective than the corresponding glycosides, substitution patterns in position 3 and 4 of the phenyl ring and the keto function attached to the phenyl ring were found to b…

Number of nitrate groups determines reactivity and potency of organic nitrates: a proof of concept study in ALDH-2−/− mice

2007

Background and purpose: Mitochondrial aldehyde dehydrogenase (ALDH-2) has been shown to provide a pathway for bioactivation of organic nitrates and to be prone to desensitization in response to highly potent, but not to less potent, nitrates. We therefore sought to support the hypothesis that bioactivation by ALDH-2 critically depends on the number of nitrate groups within the nitrovasodilator. Experimental approach: Nitrates with one (PEMN), two (PEDN; GDN), three (PETriN; glyceryl trinitrate, GTN) and four (pentaerithrityl tetranitrate, PETN) nitrate groups were investigated. Vasodilatory potency was measured in isometric tension studies using isolated aortic segments of wild type (WT) an…

8-NH2-Boldine, an Antagonist of α1Aand α1BAdrenoceptors without Affinity for the α1DSubtype: Structural Requirements for Aporphines at α1-Adrenocepto…

2005

Structure-activity analysis of 21 aporphine derivatives was performed by examining their affinities for cloned human alpha (1A), alpha (1B) and alpha (1D) adrenoceptors (AR) using membranes prepared from rat-1 fibroblasts stably expressing each alpha (1)-AR subtype. All the compounds tested competed for [ (125)I]-HEAT binding with steep and monophasic curves. The most interesting compound was 8-NH (2)-boldine, which retains the selective affinity for alpha(1A)-AR (pKi = 6.37 +/- 0.21) vs. alpha(1B)-AR (pKi = 5.53 +/- 0.11) exhibited by 1,2,9,10-tetraoxygenated aporphines, but shows low affinity for alpha(1D)-AR (pKi < 2.5). Binding studies on native adrenoceptors present in rat cerebral cor…

P1 and P2 receptors in the rat duodenal smooth muscle

1989

Sugar-induced stabilization of the monoolein Pn3m bicontinuous cubic phase during dehydration

2001

To explore the molecular mechanism of the protective function of sugars on cubic lipidic systems, the mesomorphic properties of the monoolein-water system, dehydrated in the presence of a series of sugars, have been studied by osmotic stress experiments. Two bicontinuous inverse cubic structures $(Pn3m$ and $\mathrm{Ia}3d)$ and a lamellar ${L}_{\ensuremath{\alpha}}$ phase form under dehydration in pure water. In sugar solutions, the $\mathrm{Pn}3m$ phase shows an extraordinary stability: as a function of sugar concentration, the lattice parameter decreases to very low values, but no phase transitions occur. Instead, the $\mathrm{Pn}3m$ to $\mathrm{Ia}3d$ phase transition is obtained by equi…

Embedding bullying related learning in the curriculum for initial teacher education: a possible approach

2021

Teachers are key players in preventing and combating the phenomenon of bullying in schools. To actively and constructively assume this role, they need bullying training during their initial and continuous teacher education. This study explores opportunities to engage pre-service teachers in learning about school bullying within the curriculum for initial teacher education in Romania. More competencies were identified as necessary for future teachers for being able to manage the problems related to bullying in school. Suggestions for bullying-related learning activities within the curriculum of four psycho-pedagogical disciplines are provided from the perspective of an infusion approach. Thi…