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KMID : 1134220110310020055
Hanyang Medical Reviews
2011 Volume.31 No. 2 p.55 ~ p.62
Clinical Application of ¥á2-¥ä Ligand
Shim Jae-Hang

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.
KEYWORD
Alpha2-delta ligand, Calcium channel, Chronic pain, Neuropathic pain
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