Evolving therapeutic indications for N-type calcium channel blockers: from chronic pain to alcohol abuse.

Abstract

Clinical exploitation of the therapeutic potential of calcium channels has long been limited to L-type blockers for cardiovascular diseases. Recently, N-type blockers have been fully validated for the treatment of chronic pain, following approval of the intrathecally active ziconotide (Prialt(®)). This review describes the successful efforts to broaden the therapeutic scope of this mechanism to other major CNS indications, based on the discovery of N-type blockers orally active against pain. In animal models, the N-type blocker and pain-reducing NP078585 is efficacious against key elements of ethanol dependency, including self-administration and relapse. NP078585 moderately stimulates brain dopamine release without inducing reward or hyperlocomotion. N-type blockers may emerge as a novel class of 'dopamine stabilizers' for the treatment of drug dependency and other neuropsychiatric disorders without the side effects of current therapies.

• Authors: Francesco Belardetti
• Journal: Future medicinal chemistry (Future Med Chem) Vol. 2 Issue 5 Pg. 791-802 (May 2010) ISSN: 1756-8927 [Electronic] England
• PMID: 21426203 (Publication Type: Journal Article, Review)

Chemical References

• Calcium Channel Blockers
• Calcium Channels, N-Type

Topics

• Alcoholism (drug therapy)
• Animals
• Calcium Channel Blockers (chemistry, pharmacology, therapeutic use)
• Calcium Channels, N-Type (metabolism)
• Chronic Disease
• Humans
• Pain (drug therapy)