Intranasal guanosine administration presents a wide therapeutic time window to reduce brain damage induced by permanent ischemia in rats

Purinergic Signal. 2016 Mar;12(1):149-59. doi: 10.1007/s11302-015-9489-9. Epub 2015 Dec 23.

Abstract

In addition to its intracellular roles, the nucleoside guanosine (GUO) also has extracellular effects that identify it as a putative neuromodulator signaling molecule in the central nervous system. Indeed, GUO can modulate glutamatergic neurotransmission, and it can promote neuroprotective effects in animal models involving glutamate neurotoxicity, which is the case in brain ischemia. In the present study, we aimed to investigate a new in vivo GUO administration route (intranasal, IN) to determine putative improvement of GUO neuroprotective effects against an experimental model of permanent focal cerebral ischemia. Initially, we demonstrated that IN [(3)H] GUO administration reached the brain in a dose-dependent and saturable pattern in as few as 5 min, presenting a higher cerebrospinal GUO level compared with systemic administration. IN GUO treatment started immediately or even 3 h after ischemia onset prevented behavior impairment. The behavior recovery was not correlated to decreased brain infarct volume, but it was correlated to reduced mitochondrial dysfunction in the penumbra area. Therefore, we showed that the IN route is an efficient way to promptly deliver GUO to the CNS and that IN GUO treatment prevented behavioral and brain impairment caused by ischemia in a therapeutically wide time window.

Keywords: Guanosine; Intranasal; Ischemia; Neuroprotection; Purines.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Intranasal
  • Animals
  • Behavior, Animal
  • Brain Ischemia / drug therapy*
  • Brain Ischemia / psychology
  • Cerebral Infarction / pathology
  • Cerebral Infarction / prevention & control
  • Dose-Response Relationship, Drug
  • Exploratory Behavior / drug effects
  • Guanosine / administration & dosage*
  • Guanosine / cerebrospinal fluid
  • Guanosine / pharmacokinetics
  • Guanosine / therapeutic use*
  • Male
  • Mitochondria / drug effects
  • Neuroprotective Agents / administration & dosage*
  • Neuroprotective Agents / cerebrospinal fluid
  • Neuroprotective Agents / pharmacokinetics
  • Neuroprotective Agents / therapeutic use*
  • Rats
  • Rats, Wistar
  • Stroke / drug therapy*
  • Stroke / psychology

Substances

  • Neuroprotective Agents
  • Guanosine