Yamamoto I, Kuze J, Kimura T, Watanabe K, Kondo S, Ho I K
Faculty of Pharmaceutical Sciences, Hokuriku University, Kanazawa, Japan.
Biol Pharm Bull. 1994 Apr;17(4):514-6. doi: 10.1248/bpb.17.514.
The hypnotic activity of N3-phenacyluridine in 2.0 mumol/mouse by intracerebroventricular (i.c.v.) injection was 20 times stronger than that of known N3-benzyluridine. In 0.5 mumol/mouse, i.c.v., this compound strongly potentiated both pentobarbital- and diazepam-induced sleep as compared to N3-substituted uridines, including N3-benzyluridine. Furthermore, the compound caused motor incoordination as well as decreasing spontaneous activity in the same dose. These results indicate that among the N3-substituted uridines and related compounds previously reported, N3-phenacyluridine possesses potent depressant effects.
通过脑室内(i.c.v.)注射给予小鼠2.0微摩尔/只的N3-苯甲酰基尿苷的催眠活性比已知的N3-苄基尿苷强20倍。在脑室内注射0.5微摩尔/只的剂量下,与包括N3-苄基尿苷在内的N3-取代尿苷相比,该化合物能强烈增强戊巴比妥和地西泮诱导的睡眠。此外,该化合物在相同剂量下会导致运动不协调并降低自发活动。这些结果表明,在先前报道的N3-取代尿苷和相关化合物中,N3-苯甲酰基尿苷具有强大的抑制作用。