Clinical Application of alpha2-delta Ligand.
- Author:
Jae Hang SHIM
1
Author Information
- Publication Type:Review
- Keywords: Alpha2-delta ligand; Calcium channel; Chronic pain; Neuropathic pain
- MeSH: Amines; Animals; Calcium Channels; Central Nervous System Sensitization; Chronic Pain; Cyclohexanecarboxylic Acids; gamma-Aminobutyric Acid; Horns; Ligands; Neuralgia; Neurotransmitter Agents; Nociceptors; Pain Management; Spinal Cord; Pregabalin
- From:Hanyang Medical Reviews 2011;31(2):55-62
- CountryRepublic of Korea
- Language:Korean
- Abstract: Chronic pathological pain is sustained by mechanisms of peripheral and central sensitization, which are being increasingly investigated at the molecular and cellular levels. The molecular mechanisms of sensitization that occur in peripheral nociceptors and the dorsal horns of the spinal cord are putative targets for context-dependent drugs. Pregabalin and gabapentin are analogs of the neurotransmitter gamma-aminobutyric acid (GABA). They are alpha2-delta ligands that have analgesic, anticonvulsant, and anxiolytic activity. Alpha2-delta is an auxiliary protein associated with voltage-gated calcium channels. They bind potently to the subunit resulting in modulation of calcium channels and reduction in the release of several neurotransmitters. This review discusses the pharmacology of these medications briefly as well as available clinical applications in pain management.
