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Pharmaceuticals 2013, 6(10), 1287-1303; doi:10.3390/ph6101287

Glibenclamide for the Treatment of Acute CNS Injury

1
Department of Neurosurgery, University of Maryland School of Medicine, Baltimore, MD 21201, USA
2
Department of Pathology, University of Maryland School of Medicine, Baltimore, MD 21201, USA
3
Department of Physiology, University of Maryland School of Medicine, Baltimore, MD 21201, USA
*
Author to whom correspondence should be addressed.
Received: 16 July 2013 / Revised: 17 September 2013 / Accepted: 23 September 2013 / Published: 11 October 2013
(This article belongs to the Special Issue CNS-Drugs and Therapy)
View Full-Text   |   Download PDF [144 KB, uploaded 11 October 2013]

Abstract

First introduced into clinical practice in 1969, glibenclamide (US adopted name, glyburide) is known best for its use in the treatment of diabetes mellitus type 2, where it is used to promote the release of insulin by blocking pancreatic KATP [sulfonylurea receptor 1 (Sur1)-Kir6.2] channels. During the last decade, glibenclamide has received renewed attention due to its pleiotropic protective effects in acute CNS injury. Acting via inhibition of the recently characterized Sur1-Trpm4 channel (formerly, the Sur1-regulated NCCa-ATP channel) and, in some cases, via brain KATP channels, glibenclamide has been shown to be beneficial in several clinically relevant rodent models of ischemic and hemorrhagic stroke, traumatic brain injury, spinal cord injury, neonatal encephalopathy of prematurity, and metastatic brain tumor. Glibenclamide acts on microvessels to reduce edema formation and secondary hemorrhage, it inhibits necrotic cell death, it exerts potent anti-inflammatory effects and it promotes neurogenesis—all via inhibition of Sur1. Two clinical trials, one in TBI and one in stroke, currently are underway. These recent findings, which implicate Sur1 in a number of acute pathological conditions involving the CNS, present new opportunities to use glibenclamide, a well-known, safe pharmaceutical agent, for medical conditions that heretofore had few or no treatment options. View Full-Text
Keywords: glibenclamide; Sur1-Trpm4 channel; cerebral ischemia; traumatic brain injury; spinal cord injury; encephalopathy of prematurity; metastatic brain tumor glibenclamide; Sur1-Trpm4 channel; cerebral ischemia; traumatic brain injury; spinal cord injury; encephalopathy of prematurity; metastatic brain tumor
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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MDPI and ACS Style

Kurland, D.B.; Tosun, C.; Pampori, A.; Karimy, J.K.; Caffes, N.M.; Gerzanich, V.; Simard, J.M. Glibenclamide for the Treatment of Acute CNS Injury. Pharmaceuticals 2013, 6, 1287-1303.

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