[Inhibition of the evoked liberation of (Met5)enkephalin from slices of globus pallidus in the presence of thiorphan and bestatin].

B Giros, S de la Baume, C Gros, J C Schwartz
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Abstract

(Met5) enkephalin released from slices of Rat globus pallidus by 30 mM or 50 mM K+ is hydrolysed to the extent of 85% before reaching the incubation medium. When thiorphan and bestatin, two peptidase inhibitors, are added, this inactivation process is completely prevented but the peptide release from tissues is significantly diminished. The latter effect being reversed in the presence of an opioid antagonist, naloxone, in moderate concentration, the existence of an auto-inhibition process regulating enkephalin release is suggested.

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[硫索芬和贝司他汀对苍白球脑组织(Met5)脑啡肽释放的抑制作用]。
大鼠苍白球切片经30 mM或50 mM K+释放的(Met5)脑啡肽在到达培养液前水解至85%。当添加两种肽酶抑制剂硫索芬和贝司他汀时,这种失活过程被完全阻止,但从组织中释放的肽明显减少。后一种效应在阿片类拮抗剂纳洛酮的存在下被逆转,在中等浓度下,存在调节脑啡肽释放的自抑制过程。
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