Nishikawa M, Yoshida K, Okamoto M, Itoh Y, Kohsaka M
Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., Ibaraki, Japan.
J Antibiot (Tokyo). 1991 Apr;44(4):441-4. doi: 10.7164/antibiotics.44.441.
Pharmacokinetic properties of WF-3681 and FR-62765 in rats were examined. FR-62765 showed higher peak concentrations in the plasma and higher concentrations in the sciatic nerve than WF-3681 when each compound was administered orally to rats. We therefore evaluated FR-62765 in rats with diabetic neuropathy. As a result, FR-62765 at 32 mg/kg/day administered for 3 weeks to streptozotocin-induced diabetic rats significantly prevented the accumulation of sorbitol in the sciatic nerve and the reduction of motor nerve conduction velocity in the tail. From these results it was concluded that the aldose reductase inhibitor FR-62765 might be a useful drug for diabetic neuropathy.
研究了WF - 3681和FR - 62765在大鼠体内的药代动力学特性。当分别给大鼠口服这两种化合物时，FR - 62765在血浆中的峰值浓度高于WF - 3681，在坐骨神经中的浓度也高于WF - 3681。因此，我们在患有糖尿病性神经病变的大鼠中对FR - 62765进行了评估。结果，给链脲佐菌素诱导的糖尿病大鼠连续3周每天服用32 mg/kg的FR - 62765，可显著防止坐骨神经中山梨醇的蓄积以及尾部运动神经传导速度的降低。从这些结果得出结论，醛糖还原酶抑制剂FR - 62765可能是一种治疗糖尿病性神经病变的有效药物。
