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γ-butyrolactone and γ-hydroxybutyric acid—II. The pharmacologically active form

1966; Pergamon Press; Volume: 5; Issue: 6 Linguagem: Inglês

10.1016/0028-3908(66)90007-4

1878-1713

R.H. Roth, José M. R. Delgado, Nicholas J. Giarman,

Neuroscience and Neuropharmacology Research

Three lines of evidence are presented to establish γ-hydroxybutyric acid (GHB) as the pharmacologically active form of γ-butyrolactone (GBL). A greater delay in the onset of blockade of transmission in the superior cervical ganglion of the cat was seen with GBL than with GHB, suggesting that the lactone must be converted to the acid before pharmacologie activity can be observed. Only GHB was active in depressing the rat by the intra-cisternal route of administration. When administered by micro-injection into the thalamus and hippocampus of unanesthetized monkeys, GHB produced slow-wave, high amplitude activity in the electroencephalogram, while GBL was without effect. GHB administered directly into the brain produced these effects almost immediately.