Arzneimittel Forsch
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Arzneimittel Forsch · Jan 1983
2-Acetylpyridine thiosemicarbazones. 6.2-Acetylpyridine and 2-butyrylpyridine thiosemicarbazones as antileukemic agents.
N4-Monosubstituted and N4,N4-disubstituted thiosemicarbazones derived from 2-acetylpyridine, 2-acetyl-6-methylpyridine and 2-butyrylpyridine, and N4,N4-disubstituted selenosemicarbazones derived from 2-acetylpyridine were evaluated against leukemia P388 in the mouse. Significant antitumor activity (T/C greater than 125%) was observed for members of each class. Enhancement of antitumor activity resulted from increasing the size of the N4-substituent of the thiosemicarbazone moiety. Selenosemicarbazones were less active than the corresponding thiosemicarbazones.
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Arzneimittel Forsch · Jan 1981
Influence of biological fluids on the release of 125I from povidone-iodine.
A study on the influence of vaginal smear, blood cells and human plasma on the release of 125I from povidone-iodine was conducted. The total amounts of iodine released from povidone-iodine in presence of saliva and vaginal smear are 9.51% and 5.99%, respectively, as compared to 5.9 in normal saline solution. Blood cells and plasma were found to take up 54.2 and 80.1% of iodine released from povidone-iodine. The possible effect of these fluids on the antimicrobial activity of povidone-iodine is discussed.
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Arzneimittel Forsch · Jan 1981
The pharmacology of a new short-acting, non-depolarising muscle relaxant steroid (RGH-4201).
The actions of a new steroid 3alpha-pyrrolidino-17alpha-methyl-17alpha-aza-D-homo-5alpha-androstane-dimethobromide (RGH-4201) have been studied on the skeletal muscle, autonomic and cardiovascular systems in the conscious dog and in the anaesthetized cat and dog. In the cat and dog RGH-4201 exhibited a potent, non-depolarizing neuromuscular blocking action that was rapid in onset and of short duration. RGH-4201 was equipotent with suxamethonium and chandonium as a neuromuscular blocking agent in the conscious dog but was 2-3 times less active in the anaesthetized cat. ⋯ In open-chest dog, neuromuscular paralysing dose of RGH-4201 did not cause haemodynamic changes. Duration of action of a medium-term neuromuscular blocking agent (pipecurium bromide) was not affected by a preliminary dose of RGH-4201. Pathological alterations were not found in conscious beagle dogs treated daily for 14 days with 100 and 500 microgram . kg-1 of RGH-4201, however, a transient elevation on heart rate occurred during the paralysis.