Cited by 96Nicotinic Acetylcholine Receptors StudySmoking Behavior and CessationTreatment of Major Depression

Mecamylamine - a nicotinic acetylcholine receptor antagonist with potential for the treatment of neuropsychiatric disorders

Bacher, Ingrid, Wu, Becky, Shytle, Douglas R, George, Tony P·2009·Expert Opinion on Pharmacotherapy

Abstract

Mecamylamine (Inversine), the first orally available antihypertensive agent launched in the 1950s, is rarely used today for hypertension because of its widespread ganglionic side effects at antihypertensive doses (25 - 90 mg/day). However, more recent clinical studies suggest that mecamylamine is effective at much lower doses for blocking the central and peripheral effects of nicotine. Pharmacologically, mecamylamine has been well characterized as a nonselective and noncompetitive antagonist of nicotinic acetylcholine receptors (nAChRs). Because mecamylamine easily crosses the blood - brain barrier at relatively low doses (2.5 - 10 mg), it has been used by several research groups over the past two decades investigating the role of central nAChRs in the etiology and treatment of various neuropsychiatric disorders, including addiction disorders, Tourette's syndrome, schizophrenia and various cognitive and mood disorders. Two independent Phase II clinical trials recently confirmed mecamylamine's hypothesized antidepressant activity and suggest that it may be effective as an augmentation pharmacotherapy for SSRI treatment resistant major depression. These areas of investigation for mecamylamine are reviewed and recommendations for future research directions are proposed.

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Crossref · 10.1517/14656560903329102

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Authors
Bacher, I., Wu, B., Shytle, D. R., & George, T. P.
Affiliations
Centre for Addiction and Mental Health (CA)
Venue
Expert Opinion on Pharmacotherapy
Published
2009-10-30
Volume
10
Issue
16
Pages
2709-2721
ISSN
  • 1465-6566 (ISSN-L)
  • 1744-7666
OpenAlex
W2131349644
Cited by
96
References
107
Citations by year
2026: 3 · 2025: 1 · 2024: 4 · 2023: 4 · 2022: 3 · 2021: 12 · 2020: 8 · 2019: 6 · 2018: 3 · 2017: 3 · 2016: 7 · 2015: 8 · 2014: 6 · 2013: 8 · 2012: 10
FWCI
2.66
Type
journal article
Language
en
Open access
closed
Locations
  • Expert Opinion on Pharmacotherapy (publishedVersion)
  • PubMed (publishedVersion)
Funders
Canadian Institutes of Health Research
Topics
  • Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Nicotinic Acetylcholine Receptors Study
  • Health Sciences › Medicine › Physiology › Smoking Behavior and Cessation
  • Health Sciences › Medicine › Pharmacology › Treatment of Major Depression
Keywords
mecamylamine, nicotinic acetylcholine receptors, neuropsychiatric disorders, antidepressant effects, treatment-resistant depression, SSRI augmentation, Tourette syndrome, schizophrenia, nicotine antagonism, addiction, blood-brain barrier penetration, noncompetitive antagonists, antihypertensive side effects
MeSH terms
Mental Disorders, Humans, Mecamylamine, Nicotinic Antagonists

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