Hu C Y, Choudhuri M S, Berg I E, Rao N G, Chaturvedi A K
Toxicol Appl Pharmacol. 1984 Dec;76(3):403-13. doi: 10.1016/0041-008x(84)90344-2.
The toxicity of 1-phenylcyclohexene (PC), a pyrolysis product of phencyclidine (PCP), and its interaction with PCP were evaluated. The ip LD50 of PC in Swiss male mice was 22 mmol/kg. Treatment of mice with PC at 2.2 mmol/kg/day, ip, for up to 7 days increased the liver/body weight ratio, which returned to normal within 7 days after PC withdrawal. Increases of 32% in serum glutamic-oxalacetic transaminase (SGOT) and 94% in serum glutamic-pyruvic transaminase (SGPT) were observed within 4 hr following the initial (Day 1) dose of PC. Smaller increases in the SGOT activity continued following Day 2 and 3 PC administrations. The SGPT activity remained elevated after these treatments. Activities of both enzymes, however, returned to normal within 24 hr following daily PC injections. No pathologic changes were observed in liver, brain, spleen, kidneys, and lungs with light microscopy. PC treatment for 4 days at 2.2 or 4.4 mmol/kg produced proliferation along with dilatation and fragmentation of the endoplasmic reticulum in liver. Scattering of ribosomes in the cytoplasm and dilatation of rough-surfaced cisternae were prominent at the higher dosage. Pretreatment of animals for 4 days with PC (1.1, 2.2, and 4.4 mmol/kg, ip) decreased pentobarbital- (60 mg/kg) induced sleeping time by 27, 64, and 80% and lowered PCP- (16.4 mumol/kg) stimulated locomotor activity by 18, 28, and 41%, respectively. Pretreatment of animals with PC for 1 hr inhibited (ED50: 2.3 mmol/kg) the PCP-induced locomotion. These results indicate that the PC treatment during a 7-day period produces some undesirable effects on liver function, which are reversible on its discontinuation. However, PC also weakens toxic effects of PCP.
对苯环利定（PCP）的热解产物1-苯基环己烯（PC）的毒性及其与PCP的相互作用进行了评估。PC在瑞士雄性小鼠中的腹腔注射半数致死剂量（LD50）为22 mmol/kg。以2.2 mmol/kg/天的剂量腹腔注射PC处理小鼠，持续7天，会增加肝脏/体重比，在停止注射PC后7天内该比值恢复正常。在首次（第1天）注射PC后的4小时内，血清谷草转氨酶（SGOT）升高了32%，血清谷丙转氨酶（SGPT）升高了94%。在第2天和第3天注射PC后，SGOT活性仍有较小幅度的升高。这些处理后SGPT活性仍保持升高。然而，每天注射PC后，两种酶的活性在24小时内恢复正常。光学显微镜检查未发现肝脏、脑、脾、肾和肺有病理变化。以2.2或4.4 mmol/kg的剂量用PC处理4天，会导致肝脏内质网增生、扩张和断裂。在较高剂量下，细胞质中核糖体的分散和粗面内质网池的扩张较为明显。用PC（1.1、2.2和4.4 mmol/kg，腹腔注射）对动物进行4天预处理，可使戊巴比妥（60 mg/kg）诱导的睡眠时间分别减少27%、64%和80%，并使PCP（16.4 μmol/kg）刺激的自发活动分别降低18%、28%和41%。用PC对动物预处理1小时可抑制（半数有效剂量：2.3 mmol/kg）PCP诱导的自发活动。这些结果表明，7天的PC处理对肝功能产生了一些不良影响，停药后这些影响是可逆的。然而，PC也会减弱PCP的毒性作用。
