Reference

Evaluation of isonicotinoyl-g-aminobutyric acid (GABA) and nicotinoyl-GABA as pro-drugs of GABA

Evaluation of isonicotinoyl-g-aminobutyric acid (GABA) and nicotinoyl-GABA as pro-drugs of GABA. Matsuyama, Kenji; Yamashita, Chikamasa; Noda, Atsuko; Goto, Shigeru; Noda, Hiroshi; Ichimaru, Yasuyuki; Gomita, Yutaka (Fac. Pharm. Sci., Kyushu Univ., Fukuoka 812, Japan). Chem. Pharm. Bull., 32(10), 4089-95 (English) 1984. CODEN: CPBTAL. ISSN: 0009-2363. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Section cross-reference(s): 2 Isonicotinoyl-GABA (IG) [34562-97-5] and nicotinoyl-GABA (NG) [34562-97-5], candidate prodrugs of GABA [56-12-2], were assessed by measuring various pharmacol. responses such as anticonvulsant effect, prolongation of pentobarbital [76-74-4] sleeping time, and depressive effect on rearing or ambulation in general behavior, in relation to the GABA level in the mouse brain. The GABA level after the i.p. administration of IG at a dose of 1000 mg/kg increased significantly from 2.30 mmol/g wet wt. in the control to 2.93 mmol/g wet wt., whereas NG caused only a slight increase in GABA level. IG showed a stronger anticonvulsant effect, greater prolongation of pentobarbital sleeping time, and greater depressive effect on rearing in general behavior than NG did. The pharmacol. effect of IG or NG corresponded well to the GABA level in the brain.

Effects of sodium valproate on GABA in rat brain

Effects of sodium valproate on GABA in rat brain. Gerardy, J. (Belg.). J. Pharm. Belg., 39(4), 205-8 (French) 1984. CODEN: JPBEAJ. ISSN: 0047-2166. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Na valproate [1069-66-5] (400 mg/kg, i.+.) slightly increased GABA [56-12-2] levels in the frontal cortex of rats, but had no effect on these levels in the striatum or the hypothalamus. Valproate had no effect on dopamine [51-61-6], noradrenaline [51-41-2], or DOPAC [102-32-9] levels in any of the 3 brain regions examd. In contrast, isoniazid [54-85-3] (300 mg/kg, i.p.) decreased GABA levels in all 3 brain regions by 30-50%. Valproate antagonized the action of isoniazid in the striatum and hypothalamus.