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

Abstract:

: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.

authors

Banerjee AA,Vaidya VA

doi

10.1016/j.bbrc.2020.08.022

subject

Has Abstract

pub_date

2020-10-22 00:00:00

pages

609-614

issue

4

eissn

0006-291X

issn

1090-2104

pii

S0006-291X(20)31567-9

journal_volume

531

pub_type

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