Cholinergic channel activators: novel opportunities for the treatment of CNS disorders

Proc West Pharmacol Soc. 1995:38:127-30.

Abstract

Negative connotations associated with the use of (-)-nicotine has limited medicinal chemistry research in the area of nAChRs [5]. However, recent evidence suggests that a diversity of nAChR subunits exist, that each subtype may be involved in mediating specific neurochemical/behaviors, and that these subtypes have a defined pharmacology that may be selectively targeted [1]. (+/-)-Epibatidine, GTS-21 and ABT-418 differentially interact with nAChR subtypes to elicit a diversity of behavioral effects including analgesia, neuroprotection and cognitive enhancement. These agents therefore represent important new pharmacological probes to dissect the nAChR subtype(s) mediating specific pharmacological responses to nAChR activation.

Publication types

  • Review

MeSH terms

  • Animals
  • Anti-Anxiety Agents / pharmacology
  • Benzylidene Compounds / pharmacology
  • Bridged Bicyclo Compounds, Heterocyclic / pharmacology
  • Central Nervous System Diseases / drug therapy*
  • Cholinergic Antagonists*
  • Humans
  • Ion Channels / drug effects
  • Ion Channels / metabolism*
  • Isoxazoles / pharmacology
  • Nicotinic Agonists / pharmacology
  • Parasympathetic Nervous System / drug effects
  • Parasympathetic Nervous System / metabolism*
  • Pyridines / pharmacology
  • Pyrrolidines / pharmacology
  • Receptors, Cholinergic / metabolism

Substances

  • Anti-Anxiety Agents
  • Benzylidene Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Cholinergic Antagonists
  • Ion Channels
  • Isoxazoles
  • Nicotinic Agonists
  • Pyridines
  • Pyrrolidines
  • Receptors, Cholinergic
  • 3-methyl-5-(1-methyl-2-pyrrolidinyl)isoxazole
  • 3-(2,4-dimethoxybenzylidene)anabaseine
  • epibatidine