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GABA involvement in the action of anti-anxiety drugs were studied. Because GABA is contained exclusively within Glial cells in the rat superior cervical ganglion and pineal gland, they were chosen as the models in determining the role of glial GABA in synaptic transmission and the effect of diazepam on glial GABA mechanisms. Increased noradrenergic activity produced an elevation of glial GABA and reduced noradrenergic activity reduced GABA activity. This was born out by diurnal fluctuations in pineal GABA levels. GABA has a function in the pineal gland which may be receptor mediated and was also found to significantly inhibit the norepinephrine-stimulated increase in cGMP in the pineal. This effect was blocked by picrotoxin. GABA was responsive to altered neuronal activity and in turn to have an effect on the presynaptic nerve terminals in the pineal gland, indicating that glial GABA has a role in synaptic transmission. The binding of 3H-diazepam to partially purified phosphoxiesterase was also examined as was the anti-anxiety action of diazepam.