Differential signaling signatures evoked by DOI versus lisuride stimulation of the 5-HT2A receptor

被引：21

作者：

Banerjee, Antara A. ^{[1
]}

Vaidya, Vidita A. ^{[1
]}

机构：

[1] Tata Inst Fundamental Res, Dept Biol Sci, Homi Bhabha Rd, Mumbai 400005, Maharashtra, India

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 2020年 / 531卷 / 04期

关键词：

5-HT(2A)receptor; G protein-coupled receptor; Hallucinogen; Psychedelic; SEROTONIN 2A RECEPTOR; LSD; PHOSPHORYLATION; IDENTIFICATION; TRAFFICKING; MECHANISM; SITE; RAT;

D O I：

10.1016/j.bbrc.2020.08.022

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The 5-HT2A receptor is a target for hallucinogenic and non-hallucinogenic ligands that evoke unique behavioral, electrophysiological and molecular consequences. Here, we explored the differential effects of distinct 5-HT2A receptor ligands on signaling pathways downstream to the 5-HT2A receptor. The hallucinogenic 5-HT2A receptor agonist DOI evoked an enhanced signaling response compared to the non-hallucinogenic 5-HT2A receptor agonist lisuride in human/rat 5-HT2AR-EGFP receptor expressing HEK293 cell lines and cortical neuronal cultures. We noted higher levels of phospho-PLC, pPKC, pERK, pCaMKII, pCREB, as well as higher levels of IP3 and DAG production following 5-HT2A receptor stimulation with DOI. Our study reveals distinct signaling signatures, differing in magnitude and kinetics at the 5-HT2A receptor in response to DOI versus lisuride. (C) 2020 Elsevier Inc. All rights reserved.

引用

页码：609 / 614

页数：6

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