Comparison of the behavioral effects of gamma-hydroxybutyric acid (GHB) and its 4-methyl-substituted analog, gamma-hydroxyvaleric acid (GHV)

Lawrence P. Carter, Weibin Chen, Huifang Wu, Ashok K. Mehta, R. Jason Hernandez, Maharaj K. Ticku, Andrew Coop, Wouter Koek, Charles P. France

Research output: Contribution to journalArticlepeer-review

30 Scopus citations

Abstract

Gamma-hydroxybutyrate (GHB), a metabolite of GABA, is a drug of abuse and a therapeutic. The illicit use of GHB precursors and analogs reportedly has increased worldwide. Gamma-hydroxyvaleric (GHV) is a 4-methyl-substituted analog of GHB that reportedly is abused and is marketed as a dietary supplement and replacement for GHB. The purpose of these studies was to compare the pharmacological and behavioral profiles of GHV and GHB. In radioligand binding studies, GHV completely displaced [3H]NCS-382 with approximately 2-fold lower affinity than GHB and did not markedly displace [3H]GABA from GABAB receptors at a 20-fold larger concentration. In drug discrimination procedures, GHV did not share discriminative stimulus effects with GHB or baclofen. GHV shared other behavioral effects with GHB, such as sedation, catalepsy, and ataxia, although larger doses of GHV were required to produce these effects. Lethality (50%) was observed after the largest dose of GHV (5600 mg/kg), a dose that produced less-than-maximal catalepsy and ataxia. To the extent that large doses of GHV might be taken to in an attempt to produce GHB-like effects (e.g., hypnosis) GHV toxicity may pose a greater public health concern than GHB.

Original languageEnglish (US)
Pages (from-to)91-99
Number of pages9
JournalDrug and Alcohol Dependence
Volume78
Issue number1
DOIs
StatePublished - Apr 4 2005

Keywords

  • Baclofen
  • Club drug
  • Drug discrimination
  • GABA
  • GHB
  • GHV

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology
  • Psychiatry and Mental health
  • Pharmacology (medical)

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