N-type calcium channel blockers: novel therapeutics for the treatment of pain.
Med Chem
; 2(5): 535-43, 2006 Sep.
Article
de En
| MEDLINE
| ID: mdl-17017994
ABSTRACT
Highly selective Ca(v)2.2 voltage-gated calcium channel (VGCC) inhibitors have emerged as a new class of therapeutics for the treatment of chronic and neuropathic pain. Cone snail venoms provided the first drug in class with FDA approval granted in 2005 to Prialt (omega-conotoxin MVIIA, Elan) for the treatment of neuropathic pain. Since this pioneering work, major efforts underway to develop alternative small molecule inhibitors of Ca(v)2.2 calcium channel have met with varied success. This review focuses on the properties of the Ca(v)2.2 calcium channel in different pain states, the action of omega-conotoxins GVIA, MVIIA and CVID, describing their structure-activity relationships and potential as leads for the design of improved Ca(v)2.2 calcium channel therapeutics, and finally the development of small molecules for the treatment of chronic pain.
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Collection:
01-internacional
Base de données:
MEDLINE
Sujet principal:
Douleur
/
Inhibiteurs des canaux calciques
/
Canaux calciques de type N
Limites:
Animals
/
Humans
Langue:
En
Journal:
Med Chem
Sujet du journal:
QUIMICA
Année:
2006
Type de document:
Article
Pays d'affiliation:
Australie