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Lack of effects of GHB precursors GBL and 1,4-BD following i.c.v. administration in rats.
Eur J Neurosci. 2006 Nov; 24(9):2595-600.EJ

Abstract

Gamma-hydroxybutyrate (GHB) is used therapeutically and recreationally worldwide. Since the scheduling of GHB by the USA and the United Nations in 2000-2001, the recreational use of GHB precursors has reportedly increased. The aim of this study was to examine if potency differences of GHB and GHB-like compounds are due to their blood-brain barrier permeability. The effects of peripheral and central administration of GHB, GHB precursors gamma-butyrolactone (GBL) and 1,4-butanediol (1,4-BD), and the gamma-aminobutyric acid (GABA)(B) receptor agonist baclofen on schedule-controlled responding were examined in rats. GHB and baclofen were 276- and 253-fold more potent, respectively, after intracerebroventricular (i.c.v.) administration than after intraperitoneal (i.p.) administration, whereas GBL and 1,4-BD, up to a dose of 1780 microg were without effect after i.c.v. administration. These data suggest that GBL and 1,4-BD are not metabolically converted to GHB in the brain, that enhanced brain penetration cannot account for potency differences between compounds, and that baclofen, like GHB, can readily cross the blood-brain barrier.

Authors+Show Affiliations

The University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive - MC7764, San Antonio, TX 78229, USA.No affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, N.I.H., Extramural

Language

eng

PubMed ID

17100847

Citation

Carter, Lawrence P., et al. "Lack of Effects of GHB Precursors GBL and 1,4-BD Following I.c.v. Administration in Rats." The European Journal of Neuroscience, vol. 24, no. 9, 2006, pp. 2595-600.
Carter LP, Koek W, France CP. Lack of effects of GHB precursors GBL and 1,4-BD following i.c.v. administration in rats. Eur J Neurosci. 2006;24(9):2595-600.
Carter, L. P., Koek, W., & France, C. P. (2006). Lack of effects of GHB precursors GBL and 1,4-BD following i.c.v. administration in rats. The European Journal of Neuroscience, 24(9), 2595-600.
Carter LP, Koek W, France CP. Lack of Effects of GHB Precursors GBL and 1,4-BD Following I.c.v. Administration in Rats. Eur J Neurosci. 2006;24(9):2595-600. PubMed PMID: 17100847.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Lack of effects of GHB precursors GBL and 1,4-BD following i.c.v. administration in rats. AU - Carter,Lawrence P, AU - Koek,Wouter, AU - France,Charles P, PY - 2006/11/15/pubmed PY - 2007/1/20/medline PY - 2006/11/15/entrez SP - 2595 EP - 600 JF - The European journal of neuroscience JO - Eur J Neurosci VL - 24 IS - 9 N2 - Gamma-hydroxybutyrate (GHB) is used therapeutically and recreationally worldwide. Since the scheduling of GHB by the USA and the United Nations in 2000-2001, the recreational use of GHB precursors has reportedly increased. The aim of this study was to examine if potency differences of GHB and GHB-like compounds are due to their blood-brain barrier permeability. The effects of peripheral and central administration of GHB, GHB precursors gamma-butyrolactone (GBL) and 1,4-butanediol (1,4-BD), and the gamma-aminobutyric acid (GABA)(B) receptor agonist baclofen on schedule-controlled responding were examined in rats. GHB and baclofen were 276- and 253-fold more potent, respectively, after intracerebroventricular (i.c.v.) administration than after intraperitoneal (i.p.) administration, whereas GBL and 1,4-BD, up to a dose of 1780 microg were without effect after i.c.v. administration. These data suggest that GBL and 1,4-BD are not metabolically converted to GHB in the brain, that enhanced brain penetration cannot account for potency differences between compounds, and that baclofen, like GHB, can readily cross the blood-brain barrier. SN - 0953-816X UR - https://www.unboundmedicine.com/medline/citation/17100847/Lack_of_effects_of_GHB_precursors_GBL_and_14_BD_following_i_c_v__administration_in_rats_ L2 - https://doi.org/10.1111/j.1460-9568.2006.05146.x DB - PRIME DP - Unbound Medicine ER -