No abstract

Use of base-labile N-fluorenylmethoxycarbonylamino-acids, t-butyl based side chain protecting groups, and a p-alkoxybenzyl ester resin linkage provides a simple, rapid, and exceptionally mild strategy in solid phase peptide synthesis.

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1. 14C-Flocoumafen, administered to Japanese quail as a single oral or i.p. dose, was rapidly and extensively eliminated in excreta; most was eliminated within 24 h. Extensive metabolism of the rodenticide was seen, with at least 8 metabolites detected; unchanged flocoumafen comprised 9% dose. The elimination kinetics and metabolic profiles were qualitatively similar after oral and i.p. dosing. 2. The major metabolites (60% dose) were labile to beta-glucuronidase, liberating aglycones with identical chromatographic mobilities to those of the unchanged flocoumafen isomers. 3. Radioactivity was retained mostly in the liver; largely as unchanged flocoumafen associated with the mitochondrial and microsomal fractions. Elimination of radioactivity from most tissues was biphasic with an initially rapid depletion (5 days) followed by a slow terminal elimination phase. The elimination half life from liver was greater than 100 days. 4. Livers of quail receiving extended dietary exposure to flocoumafen at 5, 15 and 50 ppm had concentrations of flocoumafen (1.0 nmol/g) that were independent of dose, indicating a capacity-limited binding site. These hepatic concentrations were similar to those after a single oral dose and were also similar to those in rats. The data indicate the presence in quail liver of a saturable high affinity flocoumafin binding site with similar characteristics and capacity to that in the rat. 5. The selective toxicity of flocoumafen to rats (highly toxic) and quail (moderately toxic) appears to arise from differences in metabolism rather than from anticoagulant binding in the liver. When hepatic binding sites of rats are saturated anticoagulant action becomes lethal, whereas quail are able to survive and extensively metabolize the compound.

No abstract

Delirium and agitation are commonly encountered after administration of electroconvulsive therapy (ECT). Management is generally fairly straightforward, although some patients may have a severe, prolonged, or refractory course. We recently cared for a 65-year-old man who consistently developed severe and very prolonged post-ECT delirium that did not respond to typical pharmacological agents; the duration of delirium was dramatically shortened by the addition of donepezil. Cholinesterase inhibitors may have a place in mitigating severe and prolonged post-ECT delirium.

Die Verwendung von basenlabilen, mit der Fmoc‐Gruppe (I) N‐geschützten Aminosäuren in Verbindung mit säurelabilen tert.‐Butyl‐ oder p‐A1koxybenzyl‐Schutzgruppen (für Seitenketten oder terminale Carboxygruppen), die gleichzeitig die Verknüpfung zum Polymerharz herstellen, ermöglicht die Durchführung von Festphasenpeptidsynthesen unter außergewöhnlich milden Reaktionsbedingungen.

SUMMARYTwo methods of inoculating tubers, one by dipping them in an aqueous suspension of Erwinia carotovora subsp. atroseptica, the other by inserting the end of a wooden toothpick charged with undiluted bacteria into the rose‐end near a sprout, were compared over two years for their ability to produce black leg and for their effect on plant growth and yield on a number of cultivars chosen because of expected differences in susceptibility. Although both methods produced a similar rank order for cultivar reaction, the more consistent results were obtained using the toothpick method, clear differences in black leg incidence and yield being evident between the susceptible cultivars Ulster Sceptre and Maris Bard and the more resistant Pentland cultivars. As some cultivars appear more tolerant to black leg than others, yield may be as important a criterion as disease incidence when assessing overall cultivar performance.The inoculation of the base and middle of stems and the infiltration of the bacterium into tubers were also investigated as alternative methods for assessing cultivar susceptibility.