Inhibition of enkepha,in metabolism by, and antinociceptive activity of, bestatin, an aminopeptidase inhibitor
作者： Pierre Chaillet , Hélène Marçais-Collado , Jean Costentin , Ching-Cheng Yi , Sophie De La Baume
DOI: 10.1016/0014-2999(83)90181-4
关键词: Endogeny 、 In vivo 、 Thiorphan 、 Aminopeptidase 、 Internal medicine 、 Enkephalinase 、 Chemistry 、 Endocrinology 、 Puromycin 、 IC50 、 Enkephalin
摘要: In the presence of thiorphan an 'enkephalinase' inhibitor, bestatin aminopeptidase inhibitor bacterial origin potently inhibited hydrolysis [3H][Leu5]enkephalin by slices from rat striatum with IC50 value about 0.2 microM whereas puromycin was approximately 1000 times less potent on this preparation. vivo or (but not puromycin) significantly protected [3H][Met5]enkephalin administered intracerebroventricularly to mice and co-administration these two peptidase inhibitors resulted in a strong reduction appearance products brain. parallel fashion antinociceptive activity [Met5]enkephalin mouse hot-plate test additively potentiated but puromycin. Finally both themselves displayed properties either jump phenyl-benzo-quinone writhing test. It is concluded that bestatin-sensitive together plays critical role inactivation exogenous endogenous enkephalins.
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