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J Lengyel

Publications and source records attributed to J Lengyel.

36 records · Page 2Linked to original sources

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History of Pharmacy↗

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History of Pharmacy↗

hnRNA size and processing as related to different DNA content in two dipterans: Drosophila and Aedes.

The size of hnRNA transcripts and the fraction of hnRNA that is converted to mRNA in cell lines of Drosophila melanogaster and Aedes albopictus are compared. Both insects belong to the order Diptera, but Aedes has a 5-6 fold larger genome than does Drosophila. The Aedes line produces significantly (2-2.5 fold) larger hnRNA than does the Drosophila line, even though the two cell lines grow under similar conditions and produce mRNA of the same size and sequence complexity. These data suggest that within a given taxonomic order, the size of hnRNA increases with increasing genome size. The fraction of hnRNA converted to mRNA [cytoplasmic poly(A)+ RNA] has been measured for the two cell types by comparing initial rates of labeling of hnRNA with initial rates of appearance of labeled mRNA in the cytoplasm. While 20of the Drosophila hnRNA is converted to mRNA, only 3.3% of the Aedes hn %RNA is converted to mrRNA. The poly(A) content of the hnRNA from the two species is also different; Drosophila hnRNA has approximately three times as much poly(A) as does Aedes hnRNA. The data show-at least for these two species-that the average amount of hnRNA transcribed relative to the amount of mRNA formed increases as genome size increases. The data are consistent with the interpretation that more DNA is transcribed into hnRNA in Aedes, the organism with the larger genome, than in Drosophila.

Adenine Nucleotides↗

Distribution of deramciclane (EGIS-3886) in rat brain regions.

The time related distribution and pharmacokinetics of double-labelled EGIS-3886 (EGIS-3886-phenyl-14C and -ethyl-3H) were studied in the plasma, hypophysis and 14 cerebral regions, including the spinal cord of the rat after a single oral treatment (acute experiments) and after repeated administration of one dose daily for six days (subacute experiments). The tissue levels of EGIS-3886 (deramciclane) were calculated from the simultaneously determined dpm values and the specific activities of the two radioisomers present in the dose administered. EGIS-3886 was rapidly absorbed from the gastrointestinal tract (t(max)=1.0 h). The concentration-time curves in the tissues can be described by a two compartment open model. The 3H-activity could be measured during the whole period of the acute experiment (96 h), whereas 14C-radioactivity fell below the detection limit within 24 h. The AUC(0-96) values for 3H were 10 to 15 times higher than that for 14C. In all samples examined, on the concentration time curves a peak characteristic of enterohepatic cycle can be seen at 12 h. The studies indicated that intact molecules entered brain tissues from the circulation. The results of the subacute experiments indicate that the 14C-labelled EGIS-3886, or its metabolite(s) carrying the tracer, reach an equilibrium as early as on the second to third day, whilst the level of 3H-radioactivity continually increases during the six days of repeated administration. In the subacute experiments the peak concentrations were reached at 0.5 h after the final treatment. However, their values for 3H were higher than in acute experiments. The last tendency was not observed in the case of 14C-tracer. The AUC values of 3H-labelled EGIS-3886 determined in subacute experiments predominated over 14C; the ratios were 50 to 60 in all brain regions. The enterohepatic cycle, seen after a single dose, also operated after repeated dosage. The time related concentrations of EGIS-3886 in the hypophysis were at least two times higher than that in the plasma and the brain tissues. No significant difference was seen in the concentrations of EGIS-3886 in the symmetrical (left and right) regions of the brain.

Animals↗

In vitro metabolic study of EGYT-3615 using rat liver microsomes.

In vitro metabolism of EGYT-3615, a prospective new antidepressant was studied by using rat liver microsomes. The metabolite (M) found in earlier in vivo studies was unanimously found to be the product of a microsomal enzymatic process. The Michaelis-Menten constant of the reaction was calculated.

Animals↗