Comment · Tue, August 22, 2017 · Ceretropic & Nootropics Depot
Are Increased Gaba Receptors By Chronic Caffeine Intake A Good Thing?
Original post in this thread
trulybadass · 34 points
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3437321/
"The density of cortical benzodiazepine-binding sites associated with GABAA receptors is increased by 65%"
What they were answering
Direct reply to the original post — see the thread post above.
u/MisterYouAreSoDumb · Ceretropic & Nootropics Depot
Nicotine up-regulates nicotinic ACh receptors, but also desensitizes them. It's more complex than just up/down-regulation. Acutely, caffeine lowers GABAergic neurotransmission.
Inhibition of a gamma aminobutyric acid A receptor by caffeine
So caffeine antagonizes GABAa. It's no surprise that long-term use of caffeine would lead to an increase in GABAa receptor density. Even the study you posted states the following:
There also appears to be a small but significant decrease in the affinity of diazepam; the nature of this decrease requires further investigation. Such an increase suggests an up-regulation of GABAA channels as a result of a decrease in GABAergic function during chronic caffeine treatment.
So it seems that it does desensitize GABAergic function over time, even if the density of receptor expression increases. Is this a good or bad thing? I suppose it depends on one's own brain chemistry.