5-HT(3A) receptor subunit is required for 5-HT3 antagonist-induced reductions in alcohol drinking

Neuropsychopharmacology. 2004 Oct;29(10):1807-13. doi: 10.1038/sj.npp.1300498.

Abstract

The ionotropic serotonin subtype-3 (5-HT3) receptor has emerged as a potential therapeutic target in the treatment of alcohol abuse and alcoholism because selective pharmacological antagonists reduce alcohol consumption in preclinical and clinical models. 5-HT binds to the extracellular N-terminus of the 5-HT(3A) receptor subunit but receptor activation is also enhanced by distinct allosteric sites, which indicates the presence of other receptor subunits. It is not known if specific molecular subunits of the 5-HT3 receptor modulate alcohol drinking. To address this issue, we characterized acute locomotor response to alcohol and alcohol consumption in a two-bottle home-cage procedure by congenic C57BL/6J mice with a targeted deletion of the 5-HT(3A) receptor subunit gene. 5-HT(3A)-null mice did not differ from wild-type littermate controls on measures of spontaneous locomotor activity, habituation to a novel environment, or locomotor response to ethanol (0, 0.5, 1, or 2 g/kg). Moreover, null mice did not differ from controls on measures of ethanol (2-10%) intake and preference during or after a two-bottle home-cage sucrose fading procedure. Systemic administration of the 5-HT3 antagonist LY-278,584 (0-10 mg/kg) decreased intake of both sweetened (2% sucrose+10% ethanol) and unsweetened (10% ethanol) ethanol in wild-type mice only. These findings indicate that reduction of alcohol drinking produced by 5-HT3 antagonism is dependent on the presence of 5-HT(3A)-containing receptors.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Alcohol Drinking / psychology*
  • Animals
  • Dose-Response Relationship, Drug
  • Indazoles / pharmacology
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Motor Activity / drug effects
  • Receptors, Serotonin, 5-HT3 / drug effects*
  • Receptors, Serotonin, 5-HT3 / genetics
  • Serotonin Antagonists / pharmacology*
  • Sweetening Agents / pharmacology
  • Taste / drug effects
  • Tropanes / pharmacology

Substances

  • Indazoles
  • Receptors, Serotonin, 5-HT3
  • Serotonin Antagonists
  • Sweetening Agents
  • Tropanes
  • LY 278584