GENERAL PHARMACOLOGICAL STUDY OF BRL 28500

General pharmacological properties of BRL 28500 and its components CVA-K and TIPC were studied by administering these compounds intravenously. With regard to the central nervous system, gross observations on mice and rats revealed no abnormal findings other than a slight and transient effect on the...

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Published in:CHEMOTHERAPY Vol. 34; no. Supplement4; pp. 168 - 186
Main Authors: NISHIOKA, YOSHITAKA, KITAMURA, YUTAKA, ISHII, RYUTARO, KOSHIMA, YOSHINOBU, NISHIMORI, TSUKAO, KOBAYASHI, FUMIO, NISHIMURA, TAKAHARU, TSUCHIYAMA, MICHIO, MORINO, KYUYA, FLACK, JOHN D.
Format: Journal Article
Language:English
Japanese
Published: Japanese Society of Chemotherapy 1986
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Summary:General pharmacological properties of BRL 28500 and its components CVA-K and TIPC were studied by administering these compounds intravenously. With regard to the central nervous system, gross observations on mice and rats revealed no abnormal findings other than a slight and transient effect on the respiratory system of rats at 120 mg/kg of CVAK. Prolongation of thiopental hypnosis was noted in animals treated with TIPC at 1, 800 mg/kg and CVA-K at 120 mg/kg, but not with BRL 28500. Otherwise, no effects on the central nervous system were noted. Studies on the respiratory and cardiovascular systems of cats showed that BRL 28500 at 480 mg/kg and above tended to reduce mildly the respiratory rate and depressed the T-wave in some animals, and at 960 mg/kg and above caused a decrease in blood pressure, though no effects were observed on the blood pressure responses to sympathetic and parasympathetic agents. No effects were observed on the isolated heart nor on the peripheral blood vessel circulation. With regard to the smooth muscle and the autonomic nervous system, slight acceleration of the spontaneous movement of uterus in situ was noted with BRL 28500 at 960 mg/kg and above and TIPC at 900 mg/kg and above. A small decrease of the contraction of the nictitating membrane was noted with BRL 28500 at 1, 920 mg/kg and TIPC at 1, 800 mg/kg. Otherwise, no effects were observed. In the tests on the peripheral nervous system, all three compounds showed no effects. With regard to the digestive system, mild acceleration of the spontaneous gastric motility was noted with BRL 28500 at 480 mg/kg and above and TIPC at 450 mg/kg and above, though the charcoal propulsive movement was unaffected. Inhibition of gastric secretion was noted with BRL 28500 at 1, 920 mg/kg and TIPC at 1, 800 mg/kg, while biliary secretion was enhanced with BRL 28500 at 480 mg/kg and above and TIPC at 450 mg/kg and above. In the ICG test, an inhibitory effect on clearance of ICG was noted with BRL 28500 at 120 mg/kg and above, TIPC at 112. 5 mg/kg and above and CVA-K at 30 mg/kg and above. The enhanced biliary secretion and the inhibition of ICG excretion seem to have been due to TIPC being excreted into bile. With regard to blood, slight prolongation of PT was noted with BRL 28500 at 1, 920 mg/kg and mild hemolysis was noted in 200 mg/ml solutions of BRL 28500 and TIPC. Otherwise, no effects were observed. With regard to the renal functions, increases in the urine volume and urinary electrolytes were noted with BRL 28500 at 960 mg/kg and above, TIPC at 900 mg/kg and above and CVA-K at 120 mg/kg. All these changes seem to have been due to sodium and potassium salt contained in the test compounds. Serum glucose, FFA, TG and the sensory organs were not affected by the test compounds.
ISSN:0009-3165
1884-5894
DOI:10.11250/chemotherapy1953.34.Supplement4_168