Antagonist-mediated down-regulation of 5-hydroxytryptamine type 2 receptor gene expression: Modulation of transcription

Miklos Toth, Thomas Shenk

Research output: Contribution to journalArticle

47 Scopus citations

Abstract

Prolonged exposure to an agonist results in a progressive loss of most G protein-coupled receptors, whereas exposure to an antagonist causes increased receptor response. The 5-hydroxytryptamine (5-HT)2 receptor is down- regulated by agonists but, paradoxically, antagonists can also elicit a decrease in receptor density. Here we show that long term treatment with serotonin or mianserin, an antagonist and antidepressant, results in reduced levels of both the 5-HT2 receptor and its RNA. Antagonist-induced down- regulation requires the presence of the 5-HT2 receptor, it occurs at the level of transcription, and it is mediated by a drug response sequence in the 5' flanking region of the 5-HT2 receptor gene. The effect of mianserin might result, at least in part, from its ability to modulate transcription.

Original languageEnglish (US)
Pages (from-to)1095-1100
Number of pages6
JournalMolecular Pharmacology
Volume45
Issue number6
StatePublished - Jun 1 1994

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Pharmacology

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