Zhang A Z, Yang H Y, Costa E
Neuropharmacology. 1982 Jul;21(7):625-30. doi: 10.1016/0028-3908(82)90004-1.
Thiorphan (60 micrograms intracerebrally) increased the met5-enkephalin content of mouse striatum by 30% in 30 min. This increase was no longer evident at 1 hr. If the dipeptidyl carboxypeptidase, inhibited by thiorphan, were located extraneuronally as suggested by De La Baume, Patey and Schwartz (1981), the met5-enkephalin accumulation represents the rate at which the pentapeptide is released extraneuronally. The increase in met5-enkephalin content was accompanied by an inhibition, greater than 80%, of the dipeptidyl carboxypeptidase that degrades striatal met5-enkephalin. Such an inhibition lasted longer then 2 hr. Thiorphan, given to mice intracerebrally, prolonged the latency time to jump off a 54 degree plate. The effects of thiorphan on brain met5-enkephalin content and hot plate latencies were significantly potentiated by bestatin, which inhibits aminopeptidase B and leucine aminopeptidase.
硫喷妥（脑内注射60微克）在30分钟内使小鼠纹状体中蛋氨酸脑啡肽含量增加了30%。1小时时这种增加不再明显。如果如德拉博姆、帕蒂和施瓦茨（1981年）所指出的，被硫喷妥抑制的二肽基羧肽酶位于神经元外，那么蛋氨酸脑啡肽的积累代表了五肽从神经元外释放的速率。蛋氨酸脑啡肽含量的增加伴随着对降解纹状体蛋氨酸脑啡肽的二肽基羧肽酶超过80%的抑制。这种抑制持续超过2小时。给小鼠脑内注射硫喷妥可延长其从54度平板上跳下的潜伏期。抑制氨肽酶B和亮氨酸氨肽酶的贝司他汀可显著增强硫喷妥对脑内蛋氨酸脑啡肽含量和热板潜伏期的作用。
