GENERAL PHARMACOLOGY OF DL-8280

DOI

Bibliographic Information

Other Title
  • DL-8280の一般薬理作用

Abstract

General pharmacological properties of DL-8280 were studied in various animals by using standard tests.<BR>1. Central nervous system; DL-8280 at doses above 300mg/kg, p. o. suppressed general behavior and spontaneous motor activity in mice. It also produced an EEG slowing in curarized cats at 3mg/kg, i. v. and more, a mild analgesia in mice at doses of 100-1, 000 mg/kg, p. o. as well as a prolongation of hexobarbital-induced sleeping time in mice and an antiinflammatory effect in rats at a dose of 1, 000mg/kg, p. o. DL-8280, however, had no effect on electro-and chemo-convulsions in mice, conditioned avoidance response in rats, body temperature in rabbits and spinal reflex in anesthetized cats.<BR>2. Respiratory and cardiovascular system ; The antibacterial drug showed no effect on systolic blood pressure and heart rate in conscious rats even at a dose as high as 1, 000 mg/kg, p. o. However, in anesthetized dogs, it increased respiratory rate and decreased respiratory depth, blood pressure, heart rate, left ventricular pressure and femoral arterial resistance without affecting cardiac contractility at doses of 10 mg/kg, i. v. and more.<BR>3. Autonomic nervous system; DL-8280 was without effect on pupillary size in rabbits but at 10-30mg/kg, i. v. inhibited both norepinephrine-induced pressor and acetylcholine-induced depressor responses in anesthetized dogs. Itexerted no ganglion-blocking effect in anesthetized cats.<BR>4. Smooth muscles; DL-8280 had little effect on the contractile response of the isolated guinea-pig ileum to various spasmogens, while it slightly enhanced norepinephrine-induced contraction of the guinea-pig was deferens and spontaneous motility of the isolated nonpregnant rat uterus only at a concentration of 10-3g/ml. The drug failed to affect the spontaneous motility of the isolated pregnant rat uterus atconcentrations up to 10-4g/ml, gastrointestinal propulsion in mice and gastric mucosa in rats at 1, 000 mg/kg, p. o. However, it inhibited gastrointestinal motility in anesthetized dogs at 3 mg/kg, i. v. and more. Gastric emptying rate and gastric secretion in rats were inhibited at doses of 300 mg/kg, p. o. and 300 mg/kg, i. p., respectively.<BR>5. Miscellaneous; DL-8280 at a dose of 30 mg/kg, i. v. slightly enhanced twitch response of the anterior tibial muscle in anesthetized rabbits. It decreased urine volume and excretion of urinary electrolytes in rats at doses above 300 mg/kg, p.o. No local anesthetic effect was observed in the guinea-pig cornea after topical application of DL-8280 (1.0%).<BR>Since these pharmacological effects of DL-8280 were observed at dose much greater than those in clinical use (approximately 4 mg/kg, p. o.), it is likely that, this drug may be relatively free of undesirable effects in clinical practice.

Journal

  • CHEMOTHERAPY

    CHEMOTHERAPY 32 (Supplement1), 1148-1161, 1984

    Japanese Society of Chemotherapy

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