Mecamylamine - a nicotinic acetylcholine receptor antagonist with potential for the treatment of neuropsychiatric disorders
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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Nicotinic blockers (antagonists or partial agonists) can alleviate depression-like behaviors in mice, either alone or in combination with monoaminergic drugs.
“Several pharmacological studies have confirmed that nicotinic blockers (antagonists or partial agonists) can alleviate depression-like behaviors in mice, either alone or in combination with monoaminergic drugs”
From Mood and anxiety regulation by nicotinic acetylcholine receptors: A potential pathway to modulate aggression and related behavioral states (2015) · cites this paper as Bacher et al., 2009
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- Authors
- Bacher, I., Wu, B., Shytle, D. R., & George, T. P.
- Affiliations
- Centre for Addiction and Mental Health (CA)
- ORCID
- George, Tony P
- Venue
- Expert Opinion on Pharmacotherapy
- Publisher
- Informa UK Limited
- 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
About these checks
Registry, retraction, Cites and statistics results are computed, not judged, with one exception: a printed reference that no index lists is read once by a model before it counts as a citation error. Claims are extracted by a model and kept only when their quote appears verbatim in the text; each cited source is then checked, with a model’s help, for whether it says what the claim relies on. Those verdicts can be wrong — read the claim’s quote and the cited source before relying on one.
Statistics and arithmetic are recomputed, not judged.
Confidence bands are shown only for fields calibrated on our annotated test set. None is calibrated yet, so no band is shown.
What counts as a claim ›How we measure confidence ›How we check this ›
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