Possible Interaction: Gamma-Aminobutyric Acid and Steroids

“Voltage-clamp fluorometry demonstrated that steroids differing in the presence of a charged group on C3 or nature of substituent on C17 uniquely modified fluorescence changes elicited by GABA in the extracellular domain.”

“The GABA system is the major inhibitory system in the adult CNS and most positive modulators of the GABA-A receptor (benzodiazepines, barbiturates, alcohol, GABA steroids ), induce inhibitory (e.g. anesthetic, sedative, anticonvulsant, anxiolytic) effects.”

“Together with the observation that physiological levels of these metabolites are sufficient to influence the function of the GBRC, the evidence clearly suggests a role for these steroids in the normal regulation of brain excitability by potentiating the postsynaptic effects of γ-aminobutyric acid (GABA).”

“Certain naturally occurring pregnane steroids act in a nongenomic manner to potently and selectively enhance the interaction of the inhibitory neurotransmitter GABA with the GABA(A) receptor.”

“The serotonergic, adrenergic and gamma-aminobutyric acid (GABA)-ergic systems are also modulated by sex steroids , albeit to a varying degree and with potentially contrasting effects on migraine outcome.”

“This review discusses the effects of steroids such as 3α-OH-5α-pregnan-20-one (3α,5α-THP or allopregnanolone) which alter GABA function in distinct ways dependent upon the time course of exposure, to either enhance or decrease inhibition in the brain.”

“Both BZ ligands and certain "neurosteroid" derivatives of steroid hormones can modulate GABA responses through direct interactions with the GABA receptor complex.”

“On the other hand, all the orally active steroid regimens used significantly increased the GABA content of the rat brain.”

“Some steroids , whose levels are raised in autism (allopregnanolone, androsterone, pregnenolone, dehydroepiandrosterone and their sulfate conjugates) are neuroactive and modulate GABA , glutamate, and opioid neurotransmission, affecting brain development and functioning.”

“ Steroids with minor effects on calcium influx were less effective as stimulators of GABA uptake.”

“The results demonstrate a twofold increase in GABA uptake following preincubation with progesterone or steroids known to stimulate calcium influx.”