Synthesis and neuromuscular blocking activity of 16-(2- and 3-pyridylmethylene) dehydroepiandrosterone derivatives

Sonal Dubey, Amit K. Sharma, D. P. Jindal, Alan Harvey, Randhir Singh, S. L. Bodhankar

Research output: Contribution to journalArticle

6 Citations (Scopus)

Abstract

The interonium distance plays a major role in neuromuscular blocking activity of bis-quaternary ammonium compounds. In this study we tried to alter the distance between two quaternary nitrogens in some of the steroidal derivatives synthesized and evaluated them for neuromuscular blocking activity using in vivo (in chicks) and in vitro models (rectus abdominus and chick biventer cervis muscle) for their mechanism of action. All the synthesized compounds have shown to possess good depolarizing, competitive neuromuscular blocking activity, particularly the 17-acetoxy derivative and the increase in the distance between two quaternary nitrogens decreased the activity.

Original languageEnglish
Pages (from-to)323-329
Number of pages7
JournalSteroids
Volume75
Issue number4-5
DOIs
Publication statusPublished - 1 Apr 2010

Keywords

  • depolarizing competitive antagonism
  • in vitro and in vivo models
  • neuromuscular blockers
  • quaternary ammonium compounds
  • intubating conditions
  • neuromuscular blocking agents
  • controlled study
  • drug dose comparison

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