SNC80和[D-青霉胺（2），D-青霉胺（5）]脑啡肽对人δ阿片受体的差异性下调

Differential down-regulation of the human delta-opioid receptor by SNC80 and [D-Pen(2),D-Pen(5)]enkephalin.

作者信息

Okura T, Cowell S M, Varga E, Burkey T H, Roeske W R, Hruby V J, Yamamura H I

机构信息

Departments of Pharmacology, Biochemistry, Medicine, Psychiatry, and the Program in Neuroscience, College of Medicine, University of Arizona Health Sciences Center, Tucson, AZ 85724, USA.

出版信息

Eur J Pharmacol. 2000 Jan 10;387(2):R11-3. doi: 10.1016/s0014-2999(99)00761-x.

DOI:10.1016/s0014-2999(99)00761-x

PMID:10650167

Abstract

We examined the contribution of the human delta-opioid receptor carboxyl terminal tail to (+)-4-[(alphaR)-alpha-((2S,5R)-4-allyl-2, 5-dimethyl-1-piperazinyl)-3-methoxybenzyl]-N,N-diethylbenzamide (SNC80)- and cyclic[D-Pen(2),D-Pen(5)]enkephalin (DPDPE)-mediated receptor down-regulation. Both SNC80 and DPDPE mediated down-regulation of an epitope tagged human delta-opioid receptor. Truncation of the human delta-opioid receptor after Gly(338) blocked DPDPE-mediated down-regulation. However, SNC80 mediated significant down-regulation of the truncated receptor. These findings suggest that SNC80-mediated down-regulation involves receptor domains in addition to the carboxyl terminal tail.

摘要

我们研究了人δ-阿片受体羧基末端尾巴对(+)-4-[(αR)-α-((2S,5R)-4-烯丙基-2,5-二甲基-1-哌嗪基)-3-甲氧基苄基]-N,N-二乙基苯甲酰胺(SNC80)和环[D-青霉胺(2),D-青霉胺(5)]脑啡肽(DPDPE)介导的受体下调的作用。SNC80和DPDPE均介导了表位标记的人δ-阿片受体的下调。在Gly(338)之后截断人δ-阿片受体可阻断DPDPE介导的下调。然而，SNC80介导了截短受体的显著下调。这些发现表明，SNC80介导的下调除羧基末端尾巴外还涉及受体结构域。