GABA Dynamics

GABA Turnover Rate in Various Regions of Rat BraiW 

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Wagner DA, Czajkowski C. 2001. Structure and dynamics of the GABA binding pocket a narrowing cleft that constricts during activation. J Neurosci 21 (1) 67. 

Table 3 Options for Pharmacodynamic Endpoints in Kinetic-Dynamic Studies of GABA-Benzodiazepine Agonist Drugs...

It is interesting to notice that the characterization of the cellular and molecular mechanisms of the star fruit intoxication needs to pass through a group of different experimental protocols among them in vivo and the in vitro bioassays. The correlation between in vivo and in vitro models is then more complex that we should think it is [53]. Thus, the particular case of synaptosomes and GABA and glutamate release and re-uptake, shows neurochemical dynamics associated to star fruit intoxication mechanisms in a preparation which consists of isolated synaptic terminals (44). However, additional studies are needed with brain slices from control brains treated with the AcTx and even the use of ex vivo models in vitro bioassays from tissue after in vivo experiments), for example, in our case, brain slices from treated animals. 

Fig. 16. Schematic diagram to illustrate the concept of dynamic interrelationships between taurine, motilin, and gamma-aminobutyric acid (GABA) in a single neuron. A neuron with both substances in coexistence may have fluctuating levels of one or both substances depending upon parameters of rhythm, time, and physiologcal demands for one or another mediator during specific types or phases of activity. Chan-Palay (1984).

The multiple pathways whereby the amino acid neuro-transmitters may be interconverted and the multiple compartments in which the amino acid neurotransmitters may be functional makes dynamic studies of glutamate, aspartate, and GABA a very difficult problem. So far, only GABA has been studied m detail. 

A related approach was also described for the chemoenzymatic synthesis of 4-phenylpyrrolidin-2-one, a cyclic analog of the pharmaceutically relevant y-aminobutyric acid (GABA). The strategy involved a m-TA-catalyzed dynamic KR, followed by an intramolecular lactamization cascade (Scheme 4.12) [45]. 

NMR and molecular dynamics investigations of the second transmembrane domain of GABA(A) which forms the inner-lining surface of chloride ion-chaimel. ... 

For the first time, dynamic kinetic resolution was mentioned for the production of 4-arylpyrrolidin-2-ones and their acyclic GABA analogs (Scheme 29.9) [37]. 

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