Potential therapeutic uses of mecamylamine and its stereoisomers

Justin R. Nickell, Vladimir P. Grinevich, Kiran B. Siripurapu, Andrew M. Smith, Linda P. Dwoskin

Research output: Contribution to journalReview articlepeer-review

36 Scopus citations


Mecamylamine (3-methylaminoisocamphane hydrochloride) is a nicotinic parasympathetic ganglionic blocker, originally utilized as a therapeutic agent to treat hypertension. Mecamylamine administration produces several deleterious side effects at therapeutically relevant doses. As such, mecamylamine's use as an antihypertensive agent was phased out, except in severe hypertension. Mecamylamine easily traverses the blood-brain barrier to reach the central nervous system (CNS), where it acts as a nicotinic acetylcholine receptor (nAChR) antagonist, inhibiting all known nAChR subtypes. Since nAChRs play a major role in numerous physiological and pathological processes, it is not surprising that mecamylamine has been evaluated for its potential therapeutic effects in a wide variety of CNS disorders, including addiction. Importantly, mecamylamine produces its therapeutic effects on the CNS at doses 3-fold lower than those used to treat hypertension, which diminishes the probability of peripheral side effects. This review focuses on the pharmacological properties of mecamylamine, the differential effects of its stereoisomers, S(+)- and R(-)-mecamylamine, and the potential for effectiveness in treating CNS disorders, including nicotine and alcohol addiction, mood disorders, cognitive impairment and attention deficit hyperactivity disorder.

Original languageEnglish
Pages (from-to)28-43
Number of pages16
JournalPharmacology Biochemistry and Behavior
StatePublished - 2013

Bibliographical note

Funding Information:
The original research findings reported herein were supported by NIH grants U19 DA17548 and T32 DA16176 , and a research contract from Layton Biosciences, Inc.


  • Alcoholism
  • Depression Anxiety
  • Mecamylamine
  • Nicotinic acetylcholine receptors
  • Smoking cessation

ASJC Scopus subject areas

  • Biochemistry
  • Toxicology
  • Pharmacology
  • Clinical Biochemistry
  • Biological Psychiatry
  • Behavioral Neuroscience


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