Skip to main content
Log in

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

  • ORIGINAL INVESTIGATION
  • Published:
Psychopharmacology Aims and scope Submit manuscript

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.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

Author information

Authors and Affiliations

Authors

Additional information

Received: 19 September 1997/Final version: 31 October 1997

Rights and permissions

Reprints and permissions

About this article

Cite this article

Egan, C., Herrick-Davis, K., Miller, K. et al. Agonist activity of LSD and lisuride at cloned 5HT2A and 5HT2C receptors. Psychopharmacology 136, 409–414 (1998). https://doi.org/10.1007/s002130050585

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1007/s002130050585

Navigation