Possible Interaction: Cannabinoids and Gamma-Aminobutyric Acid

“ Cannabinoids have been demonstrated to modulate several voltage-gated channels (including Ca2+, Na+, and various type of K+ channels), ligand-gated ion channels (i.e., GABA , glycine), and ion-transporting membranes proteins such as transient potential receptor class (TRP) channels.”

“The endogenous cannabinoid system , including CB1 receptors, is proposed to play a role in modulating neurotransmission via affecting the release of a variety of neurotransmitters, (e.g. GABA).”

“ Cannabinoids may attenuate the tonic inhibitory effect of GABA (gamma-aminobuteric acid) neurons in the central pattern generator for swallowing.”

“Taken together, these results show that while the exacerbated GABA release induced by early cannabinoid exposure may be compensated by an increment in GABA(B) receptors, which normally function as inhibitory autoreceptors, adolescent cannabinoid exposure in the females disturbs the normal balance between glutamate and GABA transmission.”

“Using blockers to isolate inhibitory or excitatory currents, we found that cannabinoids significantly reduced the release probability of both GABA and glutamate, respectively.”

“Higher concentrations of cannabinoid inhibit GABA release through mechanisms that are independent of D2 receptor activation.”

“Functional studies have shown that activation of cannabinoid CB(1 ) receptors inhibits the synaptic release of many neurotransmitters such as gamma-aminobutyric acid , glutamate, acetylcholine and monoamines.”

“It is widely accepted that cannabinoids regulate GABA release by activation of cannabinoid receptor type 1 (CB1).”

“The effect of these agonists was prevented by the CB1-selective antagonists SR141716A [N-(piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-… AM251 [1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-1-piperidinyl-1H-pyrazole-3-carboxamide trifluoroacetate salt] (1 μm), indicating that cannabinoids … GABA ….”

“CB(1) receptor activation increases GABA release in the hypothalamus, a central locus for thermoregulation, suggesting that cannabinoid and GABA systems may be functionally linked in body temperature regulation.”