Effects of newly-developed benzodiazepine ligands on noise-induced mitochondrial damage in the rat

Marco Gesi, Antonio Pellegrini, Paola Lenzi, Federico Da Settimo, Claudia Martini, Francesca Salvetti, Sabrina Taliani, Francesco Fornai

Research output: Contribution to journalArticlepeer-review

Abstract

In this study we measured the ability of three newly-synthesized N-arylalkylindol-3-ylglyoxylylamide derivatives, which have recently been characterized as partial agonists at central benzodiazepine binding sites, to prevent the rat cardiac mitochondrial alterations resulting from acute loud noise exposure. In particular, we evaluated the effects of these new compounds on the ultrastructural damage induced by noise stress on the right atrium and ventricle after 6 and 12 hr of loud noise exposure. In parallel experiments, we measured the affinity of these compounds for peripheral benzodiazepine binding sites. Following a single injection of the test products, we observed a cardioprotective effect which was more marked after 6 hr compared with 12 hr of noise exposure. Confirming our recent data showing that full agonists at benzodiazepine receptors produce cardioprotection, we demonstrate in this study that partial agonists, like indolylglyoxylylamides, can also produce a cardioprotective effect. Based on their greater affinity in binding studies, the protective activity seems to be related more to their action at central than at peripheral benzodiazepine receptors.

Original languageEnglish
Pages (from-to)311-318
Number of pages8
JournalAnnals of Anatomy
Volume182
Issue number4
Publication statusPublished - 2000

Keywords

  • Benzodiazepine ligands
  • Heart
  • Mitochondria
  • N-arylalkylindol-3-ylglyoxylylamide derivatives
  • Noise stress
  • Rat
  • Transmission electron microscopy

ASJC Scopus subject areas

  • Agricultural and Biological Sciences (miscellaneous)
  • Anatomy

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