Tone H, Kiyosaki T, Nishimori T, Kobayashi F, Nishimura K, Morino H, Tsuchiyama M
Jpn J Antibiot. 1986 Feb;39(2):526-46.
General pharmacology of (2"R)-4'-O-tetrahydropyranyladriamycin hydrochloride (THP) was studied in experimental animals. Intravenous administration of THP showed no significant effect on the respiratory and cardiovascular systems, such as blood pressure, heart rate, ECG and respiration in anesthetized rabbits and dogs. But in rats and cats, THP produced a transient decrease in blood pressure resulted from vasodilation. The hypotension was not inhibited by antihistaminics. Contraction of isolated guinea-pig atria was stimulated by THP at high concentrations (10(-4) g/ml). THP inhibited the spontaneous movement of isolated rabbit ileum and rat uterus (virgin and pregnant) at high concentrations (10(-4) g/ml). In some isolated guinea-pig ileum preparations, THP partially (6 approximately 36%) antagonized the contraction inducing by acetylcholine, histamine, serotonin and barium chloride. Urine volume and urinary excretion of electrolytes were increased by intravenous injection of 5.0 mg/kg THP. Vascular permeability was progressed when administered intracutaneously. Hemolytic effect was shown at high concentrations (10(-4) g/ml) but no effect on the coagulation was found. No significant effect of THP was observed on the general behavior and central nervous system, autonomic nervous and peripheral nervous systems. Also, THP had no significant effect on gastrointestinal propulsion in mice, the mucous membranes of the stomach and duodenum of rats, or gastric acid and bile secretion in rats.
研究了盐酸（2“R）-4'-O-四氢吡喃阿霉素（THP）在实验动物中的一般药理学。静脉注射THP对麻醉兔和犬的呼吸和心血管系统（如血压、心率、心电图和呼吸）无显著影响。但在大鼠和猫中，THP因血管扩张导致血压短暂下降。抗组胺药不能抑制这种低血压。高浓度（10（-4）g/ml）的THP刺激离体豚鼠心房收缩。高浓度（10（-4）g/ml）的THP抑制离体兔回肠和大鼠子宫（未孕和孕）的自发运动。在一些离体豚鼠回肠制剂中，THP部分（约6%至36%）拮抗乙酰胆碱、组胺、5-羟色胺和氯化钡诱导的收缩。静脉注射5.0mg/kg THP可增加尿量和电解质的尿排泄量。皮内给药时血管通透性增加。高浓度（10（-4）g/ml）时显示溶血作用，但未发现对凝血有影响。未观察到THP对一般行为、中枢神经系统、自主神经系统和周围神经系统有显著影响。此外，THP对小鼠胃肠道推进、大鼠胃和十二指肠黏膜或大鼠胃酸和胆汁分泌均无显著影响。
