Biomedical Engineering Reference
In-Depth Information
such, there is a concerted effort to develop not only isoform selective blockers, but
also blockers that exhibit state selectivity, particularly to the inactivated state of the
channel. This article provides a brief historical perspective and primarily focuses on
recent advances in the development of isoform specific and state selective sodium
channel blockers and the medicinal chemistry involved, surveying the emerging
therapeutic fields.
Keywords Voltage-gated sodium channels • Blockers • Epilepsy • Pain •
Migraine • Myotonic syndromes • Cardiovascular diseases • Neurodegenerative
diseases • Psychiatric disorders • Cancer
Abbreviations
AEDs
Antiepileptic drugs
AFib
Atrial fibrillation
ALS
Amyotrophic lateral sclerosis
BD
Bipolar depression
BPD
Borderline personality disorder
BrS
Brugada syndrome
CAMs
Neural cell adhesion molecules
CIP
Congenital insensitivity to pain
CNS
Central nervous systems
CSD
Cortical spreading depression
DMC
Dilated cardiomyopathy
DRG
Dorsal root ganglion
FHM
Familial hemiplegic migraine
GEFS+
Generalized epilepsy with febrile seizures plus
HD
Huntington disease
IEM
Inherited erythromelalgia
IFM motif
Isoleucine, phenylalanine, and methionine
LAs
Local anesthetics
LQT-3
Long QT syndrome type 3
MS
Multiple sclerosis
PAMs
Potassium-aggravated myotonias
PCCD
Progressive cardiac conduction disease
PD
Parkinson disease
PEPD
Paroxysmal extreme pain disorder
PMC
Paramyotonia congenita
PNS
Peripheral nervous systems
PPs
Periodic paralyses
SIDS
Sudden infant death syndrome
SMEI
Dravet syndrome
