Evaluation of the ability of intact platelets to accumulate acridine orange

A new approach to the evaluation of the uptake of fluorescent probes by intact cells is described. Acridine orange (AO) was used because it can be selectively accumulated by serotonin-containing granules of platelets. Analysis of the fluorescence signal allows the estimation of the relative volume of the granules and the equilibrium coefficients for AO transport across the cytoplasm and granule membranes. The following results were obtained for human and rabbit platelets: the relative volumes of the granules were 14 +/- 1% and 29 +/- 2%, the ratios of intragranular-extracellular probe concentration were 2260 +/- 382 and 30,000 +/- 5550, and the cytoplasm-extracellular medium concentration ratios were 375 +/- 60 and 225 +/- 60, respectively.     

Über die tuberkulostatische Aktivität von 2,5-Bis-(aminooxymethyl)-3,6-diketopiperazin,eines Umwandlungsproduktes des Cycloserins

Summary It has been ascertained that racemic 2,5-bis-(aminooxymethyl)-3,6-diketopiperazine, being a transformation product ofD,L-cycloserine, possesses the same effect againstMycobacterium tuberculosis asD,L-cycloserine itself.     

Derivate des 6,11-Dihydrodibenz(b,e)thiepins,eine neue Gruppe von psychotropen Substanzen

Summary Reactions of phthalide and 6-chlorophthalide with sodium salts of thiophenols gaveo-(phenylmercaptomethyl)benzoic acids (III), which were cyclized by the action of polyphosphoric acid to 6, 11-dihydrodibenz(b,e)-thiepin-11-ones (1). These ketones were treated with 3-di-methylaminopropylmagnesium chloride and other basic Grignard reagents and the products (IV) dehydrated to a series of 11-(aminoalkylidene)-6,11-dihydrodibenz(b,e)-thiepins (V), the hydrochlorides of which show psychotropic activity.

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6. Mitt. Synthetische Ataractica, 5. Mitt. siehe eskoslov. farm.11, im Druck (1962).     

Biological indicators of cadmium exposure and toxicity

The increasing environmental and occupational exposure of populations to cadmium creates the need for biological indicators of cadmium exposure and toxicity. The advantages and disadvantages of monitoring blood cadmium, urinary, fecal, hair, and tissue cadmium, serum creatinine, beta 2-microglobulin, alpha 1-antitrypsin and other proteins, and urinary amino acids, enzymes, total proteins, glucose, beta 2-microglobulin, retinol-binding protein, lysozyme, and metallothionein are discussed. It is concluded that urinary cadmium, metallothionein and beta 2-microglobulin may be used together to assess cadmium exposure and toxicity.     

Hormone and forskolin-stimulated cyclic AMP accumulation in human lymphocytes: reliability of longitudinal time measurements

Summary Reliability of measurement of lymphocyte cyclic AMP synthesis in intact cells was estimated by taking 3 successive blood samples during a one-month period from 11 healthy volunteers. Isoproterenol and prostaglandin E₁-stimulated cyclic AMP accumulation were used to evaluate the activity of these two receptor activities in human lymphocytes. Forskolin-stimulated cyclic AMP accumulation was used to evaluate the activity of the Ns/catalytic subunit. Only for forskolin was significant reliability observed. For isoproterenol and prostaglandin E₁ significant reliability was observed only for male subjects.Acknowledgment. This work was supported in part by the following organizations: Chief Scientist's Office, Israel Ministry of Health; Herman Goldman Foundation, New York; United Jewish Endowment Fund of Greater Washington-Pollinger Foundation.     

Polymethylcyclohexylamine — neue,hypotensiv wirksame substanzen

Summary A series of cyclohexylamine derivatives methylated both on nitrogen atom and in position 1, 2 and 6 of the cyclohexane ring have been prepared. Some of them showed considerable hypotensive and ganglioplegic activity. The most interesting compound is N,N,1,2,2-pentamethylcyclohexylamine (‘penhexamine’) whose activity compares favourably with mecamylamine or dimecamine.

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9. MitteilungGanglioplegica, 8. Mitteilung siehe Českoslov. farm:8 (1959), im Druck.     

Effect of penicillin on ribonucleic acid synthesis in lymphocytes of sensitized individuals

Zusammenfassung Es wird gefunden, dass Penicillin zur RNS-Synthese während der ersten 4 h der Kultur stimuliert und 7–13% der Blutlymphozyten bei Menschen eine Sensibilisierung gegen dieses Antibioticum aufweisen. Der ermittelte Prozentsatz gleicht dem der unter Penicillineinfluss transformierenden Lymphozyten bei ein und derselben Person. Ein Einfluss von Penicillin auf die RNS-Synthese der Lymphozyten bei nicht sensibilisierten Personen wurde nicht gefunden.     

Ein Beitrag über die Art der Wirkung einiger Antituberkulotika

Summary The direct effect of any antituberculotics on pancreatic lipase was studied by the modified method ofWillstätter. The antituberculotics were found to activate the pancreatic lipase in the presence of Ca⁺⁺. Any cations, especially copper, decreases the lipase activity. Increasing antituberculotics concentration is accompanied by an increasing effect on the lipolytic action of lipase.