| Popis: |
The neuropharmacological effects of 1,4-butanediol (1,4 BD), 1,3-butanediol (1,3 BD), and related congeners were compared with those of γ-hydroxybutyrate (GHB) and γ-butyrolactone (GBL). This was accomplished by studies in the rat of gross behavioral changes, anesthetic effects, lethal effects, and electroencephalogram (EEG) tracings. With some minor variations, 1,4 BD, but not 1,3 BD, exhibited neuropharmacological effects similar to those of GHB and GBL. Neuropharmacological screening tests of structure-activity relationships with 1,4 BD congeners showed the following: (a) an increase in toxicity with increasing unsaturation at the 2,3-position of 1,4 BD, (b) a decrease in activity and toxicity with change in position of hydroxyl groups, and (c) a decrease in activity with variation in length of the aliphatic chain. Preliminary studies indicate that pyruvate can prevent or reverse the anesthetic effects induced by GHB, GBL, and 1,4 BD. |
