2-iminobiotin, a selective inhibitor of nitric oxide synthase, improves memory and learning in a rat model after four vessel occlusion, mimicking cardiac arrest

PLoS One. 2023 Sep 25;18(9):e0291915. doi: 10.1371/journal.pone.0291915. eCollection 2023.

Abstract

Survivors of out-of-hospital cardiac arrest (OHCA) experience between 30% and 50% cognitive deficits several years post-discharge. Especially spatial memory is affected due to ischemia-induced neuronal damage in the hippocampus. Aim of this study was to investigate the potential neuroprotective effect of 2-iminobiotin (2-IB), a biotin analogue, on memory and learning in a four-vessel occlusion model of global ischemia using the Water Maze test. Sprague-Dawley rats were randomly assigned to either sham operation (n = 6), vehicle treatment (n = 20), 1.1 (n = 15), 3.3 (n = 14), 10 (n = 14), or 30 mg/kg/dose 2-IB treatment (n = 15). Treatment was subcutaneously (s.c.) administered immediately upon reperfusion, at 12h, and at 24h after reperfusion. Memory function on day 32 was significantly preserved in all doses of 2-IB rats compared to vehicle, as was the learning curve in the 1.1, 3.3 and 30 mg/kg dose group. Adult rats treated s.c. with 3 gifts of 2-IB every 12 h in a dose range of 1.1-30 mg/kg/dose directly upon reperfusion showed significant improved memory and learning after four vessel occlusion compared to vehicle-treated rats. Since 2-IB has already shown to be safe in a phase 1 clinical trial in adult human volunteers, it is a suitable candidate for translation to a human phase 2 study after OHCA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Aftercare
  • Animals
  • Biotin
  • Excipients
  • Humans
  • Learning Curve
  • Nitric Oxide Synthase
  • Out-of-Hospital Cardiac Arrest*
  • Patient Discharge
  • Rats
  • Rats, Sprague-Dawley
  • Vascular Diseases*

Substances

  • 2-iminobiotin
  • Biotin
  • Nitric Oxide Synthase
  • Excipients

Grants and funding

This study was sponsored by Neurophyxia B.V., ‘s Hertogenbosch, the Netherlands. CPS is a consultant for and stockholder of Neurophyxia and has received honoraria from Neurophyxia for consultancy work; SM and YB are employees of MD Biosciences Ltd., Israel, which is a contract research organization which received funding from Neurophyxia to perform the experiments described herein.