Mori N, Fukatsu T
Department of Neuropsychiatry, Fukushima Medical College, Japan.
Epilepsia. 1992 Nov-Dec;33(6):994-1000. doi: 10.1111/j.1528-1157.1992.tb01749.x.
The effects of gamma-butyrolactone-gamma-carbonyl-L-histidyl-L-propionamide citrate (DN-1417), a derivative of thyrotropin-releasing hormone, and liposome-entrapped DN-1417 (DN-L) were examined in amygdaloid-kindled rats. The animals were tested 2 h after intraperitoneal (i.p.) drug administration and then again every 24 h without further drug treatment. DN-1417 did not suppress the kindled seizure at 2 h but did beginning 1-6 days after injection. DN-L suppressed the kindled seizure at 2 h and had a more prolonged anticonvulsant effect than DN-1417. After liposomes were given i.p. once daily for 2 weeks, there was no morphologic evidence that liposomes damaged brain neurons. These results, together with previously published data, suggest that as drug delivery vehicles, liposomes can enhance the effectiveness of drugs in the CNS without producing overt brain damage.
在杏仁核点燃大鼠中检测了促甲状腺激素释放激素的衍生物γ-丁内酯-γ-羰基-L-组氨酰-L-丙氨酰胺柠檬酸盐（DN-1417）以及脂质体包裹的DN-1417（DN-L）的作用。在腹腔注射药物2小时后对动物进行测试，然后在不进行进一步药物治疗的情况下每24小时测试一次。DN-1417在2小时时并未抑制点燃性癫痫发作，但在注射后1 - 6天开始起作用。DN-L在2小时时抑制了点燃性癫痫发作，并且其抗惊厥作用比DN-1417更持久。在每天腹腔注射脂质体，持续2周后，没有形态学证据表明脂质体损害脑神经元。这些结果与先前发表的数据一起表明，作为药物递送载体，脂质体可以增强药物在中枢神经系统中的有效性，而不会产生明显的脑损伤。
