Title:Ion Channels as Drug Targets in Central Nervous System Disorders
Volume: 20
Issue: 10
Author(s): A. M. Waszkielewicz, A. Gunia, N. Szkaradek, K. Sloczynska, S. Krupinska and H. Marona
Affiliation:
Keywords:
ASIC, central nervous system, CNS, KCNQ, ion channels, NMDA, P2X, TRP
Abstract: Ion channel targeted drugs have always been related with either the central nervous system (CNS), the peripheral
nervous system, or the cardiovascular system. Within the CNS, basic indications of drugs are: sleep disorders, anxiety,
epilepsy, pain, etc. However, traditional channel blockers have multiple adverse events, mainly due to low specificity
of mechanism of action. Lately, novel ion channel subtypes have been discovered, which gives premises to drug discovery
process led towards specific channel subtypes. An example is Na+ channels, whose subtypes 1.3 and 1.7-1.9 are responsible
for pain, and 1.1 and 1.2 – for epilepsy. Moreover, new drug candidates have been recognized. This review is focusing
on ion channels subtypes, which play a significant role in current drug discovery and development process. The knowledge
on channel subtypes has developed rapidly, giving new nomenclatures of ion channels. For example, Ca2+ channels
are not any more divided to T, L, N, P/Q, and R, but they are described as Cav1.1-Cav3.3, with even newer nomenclature
α1A-α1I and α1S. Moreover, new channels such as P2X1-P2X7, as well as TRPA1-TRPV1 have been discovered, giving
premises for new types of analgesic drugs.
