GABA-uptake inhibition

Octahydroindolo[2,3-a]quinolizin-2-one, a novel structure for i-ami-nobutyric acid (GABA) uptake inhibition. Eur. J. Med. Chem. 1985, 21, 151-154. 

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

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. 

Kava Kavalactones Facilitation of GABA binding Inhibition of Nan-, Ca2-i- channels Inhibits NE uptake MAO inhibition Inhibits TXA2 synthesis... 

Valerian Sesquiterpenes GABA release and reversal of uptake Inhibition of GABA breakdown... 

Of the many drugs that have been developed which modulate GABA function, the inhibitors of GABA transaminase have been shown to be effective anticonvulsants. These are derivatives of valproic acid that not only inhibit the metabolism of GABA but may also act as antagonists of the GABA autoreceptor and thereby enhance the release of the neurotransmitter. GABA-uptake inhibitors have also been developed (for example, derivatives... 

Romero J, de Miguel R, Ramos JA, Fernandez-Ruiz J (1998a) The activation of cannabinoid receptors in striatonigral neurons inhibited GABA uptake. Life Sci 62 351-363... 

PHARMACOLOGICAL EFFECTS AND MECHANISM OF ACTION Tiagabine inhibits the GABA transporter, GAT-1, and thereby reduces GABA uptake into neurons and glia. 

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