Historique
Périodique
Comparison of the behavioral effects of gamma-hydroxybutyric acid (GHB) and its 4-methyl-substituted analog, gamma-hydroxyvaleric acid (GHV)
(Comparaison des effets comportementaux du GHB et de son analogue 4-méthyl substitué : l'acide gamma-hydroxyvalérique ou GHV)
Auteur(s) :
CARTER, L. P. ;
CHEN, W. ;
WU, H. ;
MEHTA, A. K. ;
HERNANDEZ, R. J. ;
TICKU M. K. ;
COOP A. ;
KOEK W. ;
FRANCE, C. P.
Année
2005
Page(s) :
91-99
Langue(s) :
Anglais
Refs biblio. :
47
Domaine :
Drogues illicites / Illicit drugs
Discipline :
PRO (Produits, mode d'action, méthode de dépistage / Substances, action mode, screening methods)
Thésaurus mots-clés
GHB
;
GABA
;
DROGUES DE SYNTHESE
;
TOXICITE
;
MECANISME D'ACTION
;
MODELE ANIMAL
Note générale :
Drug and Alcohol Dependence, 2005, 78, (1), 91-99
Note de contenu :
fig. ; tabl.
Résumé :
ENGLISH :
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 GABA béta 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. (Review's abstract.)
Affiliation :
Dept. Pharmacol., Univ. Texas Health Sci. Ctr. San Antonio, 7703 Floyd Curl Drive, Mail Code 7764, San Antonio, TX 78229-3900
Etats-Unis. United States.
Etats-Unis. United States.