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Basics on the use of acid-sensing ion channels' inhibitors as therapeutics

Neural Regeneration Research 2019年第3期14卷 395-398页

作者： jamileh dibas Houssam Al-Saad Adnan dibas Faculty of Pharmacy Applied UniversityAmman Jordan North Texas Eye Research Institute Department of Pharmacology and Neuroscience University of North Texas Health Science Center at Fort Worth

Since the discovery of acid-sensing ion channels in 1997, their importance in the health of neurons and other non-neuronal cells has gained significant importance. Acid-sensing ion channels play important roles in mediating pain sensation during diseases such as stroke, inflammation, arthritis, cancer, and recently migraine. More interestingly, acid-sensing ion channels may explain the sex differences in pain between males and females. Also, the ability of acid-sensing ion channel blockers to exert neuroprotective effects in a number of neurodegenerative diseases has added a new dimension to their therapeutic value. The current failure rate of ～45% of new drugs(due to toxicity issues) and saving of up to 7 years in the life span of drug approval makes drug repurposing a high priority. If acid-sensing ion channels' blockers undergo what is known as "drug repurposing", there is a great potential to bring them as medications with known safety profiles to new patient populations. However, the route of administration remains a big challenge due to their poor penetration of the blood brain and retinal barriers. In this review, the promise of using acid-sensing ion channel blockers as neuroprotective drugs is discussed.

关键词： optic nerve glaucoma neurodegeneration neuroprotection acid sensing ion channel calpain

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