van Ree J M, de Wied D
Life Sci. 1982;31(20-21):2383-6. doi: 10.1016/0024-3205(82)90162-x.
The non-opiate beta-endorphin (beta E) fragment des-Tyr-alpha-endorphin (beta E 2-16) delays extinction of pole jumping avoidance behavior and potentiates apomorphine-induced stereotyped sniffing. Structure-activity relationship studies revealed that the active moiety mediating these psychostimulant effects resides in the sequence beta E 2-9. The interaction between beta E 2-9 and apomorphine was also present following intrastriatal injection of both substances. These data provide evidence for a selective interference of the fragment beta E 2-9 with brain mechanisms, which can be distinguished from the opiate- and neuroleptic-like activity of beta-endorphin fragments. This further demonstrates the importance of beta-endorphin and its fragments for modulation of behavioral processes.
非阿片类β-内啡肽(βE)片段去酪氨酸-α-内啡肽(βE 2-16)可延迟跳杆回避行为的消退,并增强阿扑吗啡诱导的刻板嗅探。构效关系研究表明,介导这些精神兴奋作用的活性部分位于βE 2-9序列中。在纹状体内注射这两种物质后,βE 2-9与阿扑吗啡之间也存在相互作用。这些数据为βE 2-9片段对脑机制的选择性干扰提供了证据,这与β-内啡肽片段的阿片样和抗精神病样活性不同。这进一步证明了β-内啡肽及其片段对行为过程调节的重要性。