GABA uptake

Figure 4.13 GABA release by reversed uptake ( retrotransport ). Depolarization of a neuronal, or glial cell process by glutamate, with a concomitant rise in [Na+]i reverses the operation of the GABA uptake carrier, raising [GABA]o. (Modified from Attwell, Barbour and Szatkowski 1993, with permission from the publisher Cell Press)...

Thompson, SM and Gahwiler, BH (1992) Effects of the GABA uptake inhibitor tiagabine on inhibitory synaptic potentials in rat hippocampal slice cultures. J. Neurophysiol. 67 1698-1701. 

All three GABA-uptake systems are inactive in the presence of ammonium ions (see below). 

N GokaV et al. (1991) GABA-uptake inhibitors construction of a general pharmacophore model and successful prediction of a new representative. J Med Chem 34(8) 2547-2557... 

GABA-A receptor ligands GABA uptake inhibitors... 

Correlation Between Lipophilicity and Size of the Side Chain on Inhibition of GAT1- or Neuronal-Mediated GABA Uptake ... 

Krogsgaard-Larsen, P., Frplund, B., and Frydenvang, K. (2000) GABA uptake inhibitors. Design, molecular pharmacology and therapeutic aspects. Curr. Pharm. Des. 6, 1193-1209. 

Krogsgaard-Larsen, P. and Johnston, G. A. R. (1975) Inhibition of GABA uptake in rat brain slices by nipecotic acid, various isoxazoles and related compounds. J. Neurochem. 25, 797-802. 

Larsson, O. M., Falch, E., Schousboe, A., and Krogsgaard-Larsen, P. (1991) GABA uptake inhibitors Kinetics and molecular pharmacology, in Presynaptic Receptors, and Neuronal Transporters (Langer, S. Z., Galzin, A. M., and Costentin, J., eds.), Pergamon Press, Oxford, UK, pp. 197-200. 

Knutsen, L. J., Andersen, K. E., Lau, J., et al. (1999) Synthesis of novel GABA uptake inhibitors. 3. Diaryloxime and diarylvinyl ether derivatives of nipecotic acid and guvacine as anticonvulsant agents. J. Med. Chem. 42, 3447-3462. 

Andersen, K. E Lau, J., Lundt, B. F Petersen, H Huusfeldt, P. 0., Suzdak, P. D., and Swedberg, M. D. (2001) Synthesis of novel GABA uptake inhibitors. Part 6 preparation and evaluation of N-Omega asymmetrically substituted nipecotic acid derivatives. Bioorg. Med. Chem. 9,2773-2785. 

Meldrum, B. S., Croucher, M. J., and Krogsgaard-Larsen, P. (1981) GABA-uptake inhibitors as anticonvulsant agents, in Problems in GABA Research From Brain to Bacteria (Okada, Y. and Roberts, E., eds.) Excerpta Medica, Amsterdam, pp. 182-191. 

Wood, J. D., Johnson, D. D., Krogsgaard-Larsen, P., and Schousboe, A. (1983) Anticonvulsant activity of the glial-selective GABA uptake inhibitor, THPO. Neuropharmacology 22, 139-142. 

Yunger, L. M., Fowler, P. J., Zarevics, P., and Seder, P. E. (1984) Novel inhibitors of gamma-aminobutyric acid (GABA) uptake anticonvulsant actions in rats and mice../. Pharmacol. Exp. Ther. 228,109-115. 

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