Actions of Alcohols and other Sedative/Hypnotic Compounds on Cation Channels Associated with Glutamate and 5-HT3 Receptors

  • David M. Lovinger
  • Robert W. Peoples


The neural actions of a number of sedative/hypnotic agents appear to be mediated via alterations in the function of neurotransmitter receptors of the ligand-gated ion channel class. For example, it has long been known that barbiturates and benzodiazepines potentiate responses mediated by GABAA receptors (Schmidt, 1963; Nicoll, 1972; Ransom and Barker, 1976; Choi et al., 1981; Study and Barker, 1981; Olsen, 1982; Gage and Robertson, 1985; Vicini et al., 1987) and that this action likely underlies the sedative and anesthetic actions of these compounds. Ethanol (EtOH) also has potent actions on a number of different ligand-gated channels. Intoxicating concentrations of ethanol have been shown to inhibit responses mediated by the NMDA-type glutamate receptor (Dildy and Leslie, 1989; Hoffman et al., 1989; Lima-Landman and Albuquerque, 1989; Lovinger et al., 1989; Göthert and Fink, 1989), while ethanol is less potent in inhibiting AMPA/kainate receptor-mediated responses (Hoffman et al, 1989; Lovinger et al., 1989; Lovinger et al., 1990). In contrast, ethanol potentiates the function of other ligand-gated ion channels including some types of GABAA receptors (Mehta and Ticku, 1988; Suzdak et al., 1986; Nakahiro et al., 1991; Wafford et al., 1990), 5-HT3 receptors (Lovinger, 1991), strychnine-sensitive glycine receptors (Celentano et al., 1988) and nicotinic acetylcholine receptors (Okada, 1967; Miller et al., 1991).


NMDA Receptor Glutamate Receptor GABAA Receptor Discriminative Stimulus Effect Ethanol Sensitivity 
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Copyright information

© Springer Science+Business Media New York 1993

Authors and Affiliations

  • David M. Lovinger
    • 1
  • Robert W. Peoples
    • 2
  1. 1.Department of Molecular Physiology and BiophysicsVanderbilt University Medical SchoolNashvilleUSA
  2. 2.Laboratory of Molecular Physiology and PharmacologyNational Institute on Alcohol Abuse and AlcoholismRockvilleUSA

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