Abstract
Potassium (K+) channels are the most heterogeneous and widely distributed class of ion channels. K+ channels are dynamic pore-forming transmembrane proteins known to play important roles in all cell types underlying both normal and pathophysiological functions. Essential for such diverse physiological processes as nerve impulse propagation, muscle contraction, cellular activation and the secretion of biologically active molecules, various K+ channels are recognized as potential therapeutic targets in the treatment of multiple sclerosis, Alzheimer's disease, Parkinson's disease, epilepsy, stroke, brain tumors, brain/spinal cord ischemia, pain and schizophrenia, migraine, as well as cardiac arrhythmias, pulmonary hypertension, diabetes, cervical cancer, urological diseases and sepsis. In addition to their importance as therapeutic targets, certain K+ channels are gaining attention for their beneficial roles in anesthesia, neuroprotection and cardioprotection. The K+ channel gene families (subdividing into multiple subfamilies) include voltage-gated (Kv: Kv1-Kv12 or KCNA-KCND, KCNF-KCNH, KCNQ, KCNS), calcium-activated (KCa: KCa1-KCa5 or KCNM-KCNN), inwardly rectifying (Kir: Kir1-Kir7 or KCNJ) and background/leak or tandem 2-pore (K2P: K2P1-K2P7, K2P9-K2P10, K2P12-K2P13, K2P15-K2P18 or KCNK) K+ channels. Worldwide, the pharmaceutical industry is actively developing better strategies for targeting ion channels, in general, and K+ channels, in particular, already generating over $6 billion in sales per annum from drugs designed to block or modulate ion channel function. This review provides an overview of recent patents on emerging K+ channel blockers and activators (openers) with potential for development as new and improved nervous system therapeutic agents. © 2007 Bentham Science Publishers Ltd.
| Original language | American English |
|---|---|
| Journal | Recent Patents on CNS Drug Discovery |
| Volume | 2 |
| State | Published - Jan 1 2007 |
Keywords
- 4 aminopyridine
- A-type K+ channels
- Alzheimer disease
- Animals
- Background or leak or tandem 2-pore K+ channels
- Calcium-activated K+ channels
- Central Nervous System Diseases
- Central nervous system
- Delayed rectifiers
- Humans
- Inward rectifiers
- Inwardly rectifying K+ channels
- Ion Channel Gating
- K+ channels
- K2P K+ channels
- KCa channels
- Kir channels
- Kv channels
- Parkinson disease
- Potassium channel blockers
- Potassium channel openers
- Potassium channels
- Rapidly inactivating K+ channels
- Shaker potassium channel
- Shal potassium channel
- Voltage-gated K+ channels
- acetylsalicylic acid
- amantadine
- amfebutamone
- amitriptyline
- amoxapine
- analgesic agent
- anesthesia
- antidepressant agent
- benzimidazole derivative
- benzopyran derivative
- brain ischemia
- brain tumor
- calcium activated potassium channel
- cell activation
- cell type
- central nervous system agents
- central nervous system disease
- clinical trial
- corticosteroid
- diabetes mellitus
- drug industry
- epilepsy
- glatiramer
- heart arrhythmia
- heart protection
- human
- hydroxymethylglutaryl coenzyme A reductase inhibitor
- inwardly rectifying potassium channel
- membrane protein
- methylprednisolone
- migraine
- mitoxantrone
- modafinil
- multigene family
- multiple sclerosis
- muscle contraction
- nerve conduction
- neuroprotection
- nonhuman
- pain
- paroxetine
- patent
- pathophysiology
- pharmacological blocking
- phentermine
- phenytoin
- potassium channel
- potassium channel KCNQ
- potassium channel blocking agent
- priority journal
- protein function
- pulmonary hypertension
- pyrimidine derivative
- review
- schizophrenia
- sepsis
- spinal cord ischemia
- stroke
- unindexed drug
- urinary tract disease
- uterine cervix cancer
Disciplines
- Neuroscience and Neurobiology