PMID- 19562650 OWN - NLM STAT- MEDLINE DCOM- 20100128 LR - 20121115 IS - 2040-3437 (Electronic) IS - 1367-6733 (Linking) VI - 12 IP - 4 DP - 2009 Jul TI - Small molecules targeting sodium and calcium channels for neuropathic pain. PG - 543-61 AB - Neuropathic pain is a chronic disease, which impacts millions of individuals worldwide. The condition is currently treated with several drugs that provide pain relief that is inconsistent and complicated by CNS or cardiovascular (CV) side effects. Voltage-gated sodium channels (VGSCs) and voltage-gated calcium channels (VGCCs) are of particular interest as targets for neuropathic pain because they control electrical signals in both the central and peripheral nervous system. Recent research has demonstrated that the expression of voltage-gated ion channels changes significantly under conditions of neuropathic pain in rodents and humans. Selective modulation of the channels involved in the pathology of the disease, while sparing the channels that are essential for normal nociception, offers promising opportunities for therapeutic intervention. This review summarizes recent developments of small molecules that target VGSCs and VGCCs. FAU - Bear, Brian AU - Bear B AD - Vertex Pharmaceuticals San Diego, San Diego, CA 92121, USA. brian_bear@sd.vrtx.com FAU - Asgian, Juliana AU - Asgian J FAU - Termin, Andreas AU - Termin A FAU - Zimmermann, Nicole AU - Zimmermann N LA - eng PT - Journal Article PT - Review PL - England TA - Curr Opin Drug Discov Devel JT - Current opinion in drug discovery & development JID - 100887519 RN - 0 (Calcium Channel Blockers) RN - 0 (Calcium Channels) RN - 0 (NAV1.7 Voltage-Gated Sodium Channel) RN - 0 (NAV1.8 Voltage-Gated Sodium Channel) RN - 0 (SCN10A protein, human) RN - 0 (SCN9A protein, human) RN - 0 (Small Molecule Libraries) RN - 0 (Sodium Channel Blockers) RN - 0 (Sodium Channels) SB - IM EIN - Curr Opin Drug Discov Devel.2009 Sep;12(5):705 MH - Animals MH - Calcium Channel Blockers/chemistry/*pharmacology/therapeutic use MH - Calcium Channels/metabolism MH - Humans MH - Molecular Structure MH - NAV1.7 Voltage-Gated Sodium Channel MH - NAV1.8 Voltage-Gated Sodium Channel MH - Neuralgia/drug therapy/metabolism MH - Pain/*drug therapy/metabolism MH - Peripheral Nervous System Diseases/*drug therapy/metabolism MH - Small Molecule Libraries/chemistry/*pharmacology/therapeutic use MH - Sodium Channel Blockers/chemistry/*pharmacology/therapeutic use MH - Sodium Channels/metabolism RF - 85 EDAT- 2009/06/30 09:00 MHDA- 2010/01/29 06:00 CRDT- 2009/06/30 09:00 PHST- 2009/06/30 09:00 [entrez] PHST- 2009/06/30 09:00 [pubmed] PHST- 2010/01/29 06:00 [medline] PST - ppublish SO - Curr Opin Drug Discov Devel. 2009 Jul;12(4):543-61.