Possible Interaction: Gamma-Aminobutyric Acid and Ketamine

“It is hypothesized that ketamine blocks NMDA receptors on gamma-aminobutyric acid (GABA) neurons inside the thalamic reticular nucleus, which leads to disinhibition of dopaminergic neurons and increased release of dopamine.”

“ GABA and NMDA receptors are also involved in the antinociceptive actions of gabapentin and ketamine , respectively.”

“Unlike the NMDA-insensitive glutamate receptors for kainate and AMPA, the LOC activated by acetylcholine and the principal inhibitory amino acid GABA gamma-aminobutyric acid ) were both sensitive to clinical concentrations of ketamine , although in different ways.”

“A single dose of …-T inhibitors, gamma-vinyl GABA (1200 mg/kg, IP) or gamma-acetylenic GABA (100 mg/kg, IP) administered 4 hours prior to ketamine , shortened the first rotation phase, increased the anesthetic phase, changed the pattern of postanesthetic rotation and reduced total and net rotation scores.”

“Although numerous other receptors (e.g., GABA , nicotinic acetylcholine, opiate, voltage-operated channels) have been reported to interact with ketamine , their role in inducing dissociative anaesthesia is still under discussion.”

“These results support a growing literature that increased GABA inhibition contributes to ketamine anesthesia, while increased excitatory transmission contributes to its antidepressant effects.”

“In contrast, a single dose of ketamine can reverse CUS-induced deficits of GABA markers, in conjunction with reversal of CUS-induced depressive-like behaviors.”

“As PCP, ketamine inhibits GABA neurons of the reticular thalamic nucleus.”

“However, whether ketamine , at clinically relevant concentrations, increases the activity of inhibitory & ggr;-aminobutyric acid (GABA) receptor type A (GABAA) receptors in different brain regions remains controversial.”

“The selective increase in tonic current was attributed to ketamine increasing the apparent potency of GABA at high-affinity extrasynaptic GABAA receptors.”

“BACKGROUND It has been suggested that dysregulation of γ-aminobutyric acid (GABA)-mediated neurotransmission is involved in the etiology of major depressive disorder and in the action of the fast-acting antidepressant ketamine.”