Polyamines may modulate both G protein-coupled receptors and G proteins

Gabriella Marucci, Francesca Novi, Rita Banzi, Maria L. Bolognesi, Michela Buccioni, Anna Minarini, Michela Rosini, Piero Angeli, Roberto Maggio, Carlo Melchiorre

Research output: Contribution to journalArticlepeer-review

Abstract

Polyamines pipertramine (PIP) and pipertramine amide (PIPAM), unlike prototype methoctramine, displayed a potent inotropic effect in guinea pig atria. While the inotropic effect of PIP may be rationalized, as previously suggested, through a direct activation of a Gi/o protein, PIPAM effects were possibly the result of multiple interactions. Besides a direct Gi/o protein activation, PIPAM activated also muscarinic M 2 receptors by interacting most likely with an allosteric site. Binding experiments in CHO cells, expressing human cloned muscarinic M 2 receptors, confirmed that both compounds were effective muscarinic ligands.

Original languageEnglish
Pages (from-to)63-73
Number of pages11
JournalMedicinal Chemistry Research
Volume13
Issue number1-2
DOIs
Publication statusPublished - 2004

ASJC Scopus subject areas

  • Drug Discovery
  • Organic Chemistry

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