Agarwal N, Agrawal V K, Sharma S, Srivastava V M
Division of Biochemistry, Central Drug Research Institute, Lucknow, India.
Pharmazie. 1987 May;42(5):332-4.
The metabolic disposition of [2-14C]-centperazine (1; 3-ethyl-8-methyl-1,3,8-triazabicyclo[4.4.0]decan-2-one) following an injection of 5 mg/kg dose was studied in male albino rats. During the initial period of 45-60 min, a very rapid fall in blood level of radioactivity was noticed. Thereafter the rate of fall of blood radiocarbon went on decreasing but did not attain linearity even upto 24 h. The drug was found to be fairly distributed in all the tissues attaining highest concentration in most of them within 30 min. In 24 h, about 83.5% of the administered drug was eliminated from the body, of which 21.3% was recovered from the faeces and 61.1% from the urine. The 14CO2 accountes for only 1% of the total dose. The drug exhibited significant binding with all the tissues examined. The brain and muscle showed highest and lowest activity, respectively.
在雄性白化病大鼠中研究了注射5mg/kg剂量的[2-¹⁴C]-氯氮平（1；3-乙基-8-甲基-1,3,8-三氮杂双环[4.4.0]癸烷-2-酮）后的代谢情况。在最初的45-60分钟内，观察到放射性血液水平迅速下降。此后，血液中放射性碳的下降速率持续降低，但直至24小时仍未达到线性。发现该药物在所有组织中分布相当均匀，在30分钟内大多数组织中达到最高浓度。在24小时内，约83.5%的给药药物从体内消除，其中21.3%从粪便中回收，61.1%从尿液中回收。¹⁴CO₂仅占总剂量的1%。该药物与所有检测的组织均表现出显著结合。脑和肌肉分别显示出最高和最低活性。
