Abstract
After Roth and Giarman 1 discovered the “anesthetic” activity of gammabutyrolactone (GBL) numerous pharmacological and clinical studies have been conducted using either GBL or the product of its hydrolytic cleavage gamma-hydroxybutyrate (GHB). The present study was conducted to clarify whether GBL or GHB is the substance active as a depressant of C.N.S. Using a spectrophotometric method of assay (based on the Hestrin reaction) we found that while it is possible to obtain a correlation between the loss of righting reflex and the concentration of GHB in rat brain, a strict correlation is not obtained with GBL. The study of plasma and cerebral levels of GHB and GBL as a function of the route of administration illustrates the importance of consideration of this factor in the appraisal of the action of these two agents. GBL given per os, i.p. or i.v. is capable of producing higher concentrations of GHB in brain and blood than an equimolecular amount of GHB-Na administered by the same route. This result is particularly evident when GBL and GHB-Na are given orally.
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