Therapeutic time window for conivaptan treatment against stroke-evoked brain edema and blood-brain barrier disruption in mice

PLoS One. 2017 Aug 30;12(8):e0183985. doi: 10.1371/journal.pone.0183985. eCollection 2017.

Abstract

Background: Ischemic stroke is often complicated by brain edema, disruption of blood-brain barrier (BBB), and uncontrolled release of arginine-vasopressin (AVP). Conivaptan, a V1a and V2 receptor antagonist, reduces brain edema and minimizes damage to the blood-brain barrier after stroke. Most stroke patients do not receive treatment immediately after the onset of brain ischemia. Delays in therapy initiation may worsen stroke outcomes. Therefore, we designed a translational study to explore the therapeutic time window for conivaptan administration.

Methods: Mice were treated with conivaptan beginning 3, 5, or 20 hours after 60-minute focal middle cerebral artery occlusion. Treatments were administered by continuous IV infusion for a total of 48 hours. Brain edema and blood-brain barrier (BBB) disruption were evaluated at endpoint.

Results: Conivaptan therapy initiated at 3 hours following ischemia reduced edema in the ipsilateral hemisphere, which corresponded with improvements in neurological deficits. Stroke-triggered BBB disruption was also reduced in mice when conivaptan treatments were initiated at 3 hours of reperfusion. However, 5 and 20-hour delays of conivaptan administration failed to reduce edema or protect BBB.

Conclusion: Timing of conivaptan administration is important for successful reduction of brain edema and BBB disruption. Our experimental data open new possibilities to repurpose conivaptan, and make an important "bench-to-bedside translation" of the results into clinical practice.

MeSH terms

  • Animals
  • Antidiuretic Hormone Receptor Antagonists / therapeutic use*
  • Benzazepines / therapeutic use*
  • Blood-Brain Barrier / drug effects*
  • Blood-Brain Barrier / pathology
  • Brain Edema / drug therapy*
  • Brain Edema / etiology*
  • Brain Edema / pathology
  • Infarction, Middle Cerebral Artery / complications*
  • Infarction, Middle Cerebral Artery / pathology
  • Male
  • Mice
  • Mice, Inbred C57BL

Substances

  • Antidiuretic Hormone Receptor Antagonists
  • Benzazepines
  • conivaptan

Grants and funding

This research was supported by a grant from Swedish Medical center to Dr. J. Paul Elliott.