Psychopharmacology

, Volume 136, Issue 4, pp 409–414

Agonist activity of LSD and lisuride at cloned 5HT2A and 5HT2C receptors

  • Christina T. Egan
  • Katharine Herrick-Davis
  • Keith Miller
  • Richard A. Glennon
  • M. Teitler
ORIGINAL INVESTIGATION

DOI: 10.1007/s002130050585

Cite this article as:
Egan, C., Herrick-Davis, K., Miller, K. et al. Psychopharmacology (1998) 136: 409. doi:10.1007/s002130050585

Abstract

Evidence from studies with phenylisopropylamine hallucinogens indicates that the 5HT2A receptor is the likely target for the initiation of events leading to hallucinogenic activity associated with LSD and related drugs. Recently, lisuride (a purported non-hallucinogenic congener of LSD) was reported to be a potent antagonist at the 5HT2C receptor and an agonist at the 5HT2A receptor. LSD exhibited agonist activity at both receptors. These data were interpreted as indicating that the 5HT2C receptor might be the initiating site of action for hallucinogens. To test this hypothesis, recombinant cells expressing 5HT2A and 5HT2C receptors were used to determine the actions of LSD and lisuride. LSD and lisuride were potent partial agonists at 5HT2A receptors with EC50 values of 7.2 nM and 17 nM, respectively. Also, LSD and lisuride were partial agonists at 5HT2C receptors with EC50 values of 27 nM and 94 nM, respectively. We conclude that lisuride and LSD have similar actions at 5HT2A and 5HT2C receptors in recombinant cells. As agonist activity at brain 5HT2A receptors has been associated with hallucinogenic acitivity, these results indicate that lisuride may possess hallucinogenic activity, although the psychopharmacological effects of lisuride appear to be different from the hallucinogenic effects of LSD.

Key words Lisuride Lysergic acid diethylamide (LSD) 1-(2 5-Dimethoxy-4-methylphenyl)2-aminopropane (DOM) N-Dimethyltryptamine (DMT) 5-Hydroxytryptamine (5HT) 5HT2A receptor 5HT2C receptor Inositol phosphate (IP) production Hallucinogenic drug 

Copyright information

© Springer-Verlag Berlin Heidelberg 1998

Authors and Affiliations

  • Christina T. Egan
    • 1
  • Katharine Herrick-Davis
    • 1
  • Keith Miller
    • 2
  • Richard A. Glennon
    • 3
  • M. Teitler
    • 1
  1. 1.Department of Pharmacology and Neuroscience, Albany Medical College, Albany, NY 12208, USA Fax: +1-518-262-5799, e-mail: mteitler.ccgateway.amc.eduUS
  2. 2.Department of Pharmaceutical Science, College of Pharmacy, Nova Southeastern University, Davie, FA 333328, USAUS
  3. 3.Department of Medicinal Chemistry, Medical College of Virginia, Virginia Commonwealth University, Richmond, VA 23298-0540, USAUS

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