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61.
    
We present a highly sensitive, rapid method for the determination of ruthenium originating from the investigational anti-cancer drug NAMI-A in human plasma ultrafiltrate, plasma, and urine. The method is based on the quantification of ruthenium by inductively coupled plasma mass spectrometry and allows quantification of 30 ng L(-1) ruthenium in plasma ultrafiltrate and urine, and 75 ng L(-1) ruthenium in human plasma, in 150 microL of matrix. The sample pretreatment procedure is straightforward and only involves dilution with appropriate diluents. The performance of the method, in terms of accuracy and precision, fulfilled the most recent FDA guidelines for bioanalytical method validation. Validated ranges of quantification were 30.0 to 1 x 10(4) ng L(-1) for ruthenium in plasma ultrafiltrate and urine and 75.0 to 1 x 10(4) ng L(-1) for ruthenium in plasma. The applicability of the method and its superiority to atomic-absorption spectrometry were demonstrated in two patients who were treated with intravenous NAMI-A in a phase I trial. The assay is now successfully used to support pharmacokinetic studies in cancer patients treated with NAMI-A.  相似文献   
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A new simple and efficient method for the detection of incomplete coupling reactions during solid-phase peptide synthesis is decribed. Using p-nitrophenyl ester 1 (NF31), free amino groups can be visually detected on the resin by direct coloring of the beads. A specific feature of the assay resides in the possibility of detection of sterically hindered primary amines.  相似文献   
63.
The wound-healing properties of Plantago major L. (plantain) were evaluated using an ex-vivo porcine wound-healing model. Ethanol- and water-based extracts were prepared from greenhouse-grown and freeze-dried leaves of P. major. Both types of extracts stimulated wound healing in porcine skin, but the ethanol-based extracts had a somewhat stronger effect. A concentration of 1.0 mg/mL (on dry weight basis) produced the best results for both types of extracts.  相似文献   
64.
Telechelic polyacetals have been synthesized by endcapping of bifunctionally living polyacetals with tertiary amines. Bifunctionally living poly-(1, 3-dioxolane) (poly-DXL) was obtained by polymerization of the cyclic acetal initiated with terephthaloyl-bis-triflate. Attempts to prepare well defined bifunctionally growing poly-DXL with trifluoro-methane sulfonic acid anhydride failed. Low molecular weight dialkyl formals containing functional groups were used as transfer agents for the polymerization of cyclic acetals to control the molecular weight of the polymer and to introduce functional endgroups. Polytelechelic hydroxy-terminated poly-DXL was synthesized by copolymerization of DXL and glycidol. The latter monomer reacts as comonomer through its epoxy ring and as transfer agent by its hydroxyl group.  相似文献   
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Nanotechnology is an emerging technology particularly vulnerable to societal unrest, which may hinder its further development. With the increasing convergence of several technological domains in the field of nanotechnology, so too could convergence of social science methods help to anticipate societal response. This paper systematically reviews the current state of convergence in societal response research by first sketching the predominant approaches to previous new technologies, followed by an analysis of current research into societal response to nanotechnology. A set of 107 papers on previous new technologies shows that rational actor models have played an important role in the study of societal response to technology, in particular in the field of information technology and the geographic region of Asia. Biotechnology and nuclear power have, in contrast, more often been investigated through risk perception and other affective determinants, particularly in Europe and the USA. A set of 42 papers on societal response to nanotechnology shows similarities to research in biotechnology, as it also builds on affective variables such as risk perception. Although there is a tendency to extend the rational models with affective variables, convergence in social science approaches to response to new technologies still has a long way to go. The challenge for researchers of societal response to technologies is to converge to some shared principles by taking up the best parts from the rational actor models dominant in information technology, whilst integrating non-rational constructs from biotechnology research. The introduction of nanotechnology gives a unique opportunity to do so.  相似文献   
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It has been suggested that sex judgments of male-to-female transsexuals based on the voice may be influenced by the physical appearance of the clients. To explore this hypothesis, a listener experiment was designed in which a panel of 22 laypersons and 22 students in speech-language pathology rated the “femaleness” of fourteen male-to-female transsexuals from video-recorded speech samples in three modes of presentation: auditory-only presentation, visual-only presentation, and audiovisual presentation. Results indicate that appearance and voice are indeed interacting factors. Ratings from the auditory-only presentation were significantly lower than ratings from the audiovisual presentation and ratings from the visual-only presentation were significantly higher than those from the audiovisual presentation. It follows that the success of voice training in male-to-female transsexuals is not solely dependent on vocal characteristics and that speech pathologists should consider incorporating physical appearance as a treatment and outcome variable in the voice training of male-to-female transsexuals.  相似文献   
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Carvedilol (CAR), a racemic lipophilic aryloxy propanolamine, acts as a selective α1-adrenoreceptor antagonist and a nonselective β-adrenoreceptor antagonist. CAR metabolism mainly produces three active metabolites: desmethyl carvedilol (DMC), 4′-hydroxy carvedilol (4′OHC) and 5′-hydroxy carvedilol (5′OHC). The oxidative S-(-)-metabolites contribute to the β-antagonistic effect, yet not to the α-antagonistic effect to be observed after drug dosage. Therefore, the three β-adrenoceptor blocking metabolites, which are structurally closely related to the parent CAR, are included into the development of a bioanalytical quantitative method for all major active species relevant with respect to adrenoceptor-blockade. Because of the given pharmacological profile, resolution of the enantiomers of carvedilol, of 4′- and 5′-hydroxy carvedilol as well as of DMC, is mandatory. The current study aims to determine the response surface for the enantiomer separation of the parent CAR as well as the major metabolites on a suitable chiral stationary phase. Design of experiment approach (DoE) was utilized in an initial screening phase followed by central-composite design for delimitation of the response surface for resolution of the four enantiomeric pairs in least run time. The impact of chromatographic variables (composition and percentage of organic modifier(s), buffer type, buffer pH, flow rate) on critical peaks resolution and adjusted retention time was evaluated, in order to select the most significant critical quality attributes. On this basis, a robust UHPLC-UV method was developed and optimized for the simultaneous, enantioselective determination of CAR along with its major active metabolites (4′OHC, 5′OHC, and DMC) on Chiralpak IBN-5. The optimized UHPLC-UV method (which includes metoprolol as the internal standard) was validated according to the ICH M10 guidelines for bioanalytical methods and proven to be linear, precise, accurate, and robust. The validated assay was applied to plasma samples from cardiovascular patients treated with rac-CAR (blood randomly drawn at different times after oral CAR intake). In order to provide more insight into the mechanism of the enantiomer separation of CAR and its metabolites on the CSP, docking experiments were performed. Molecular simulation studies suggest the chiral recognition to be mainly due to different binding poses of enantiomers of the same compound.  相似文献   
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