Creatine, similarly to ketamine, affords antidepressant-like effects in the tail suspension test via adenosine A1 and A2A receptor activation ncbi.nlm.nih.gov/pmc/arti…
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πŸ‘€︎ u/Redditor561
πŸ“…︎ Jun 10 2020
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Caffeine prevents antihyperalgesic effect of gabapentin in an animal model of CRPS-I: evidence for the involvement of spinal adenosine A1 receptor. ncbi.nlm.nih.gov/pubmed/2…
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πŸ‘€︎ u/_svyatogor_
πŸ“…︎ Nov 06 2019
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Adenosine A1 receptor agonist induces visceral antinociception via 5-HT1A, 5-HT2A, dopamine D1 or cannabinoid CB1 receptors, and the opioid system in the central nervous system sciencedirect.com/science…
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πŸ‘€︎ u/Robert_Larsson
πŸ“…︎ Mar 24 2020
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Despite decrease in sleep measured in older mammals, adenosine metabolic enzyme activity increases with age, pointing to other factors causing decrease in sleep homeostasis including A1 receptors. sciencedirect.com/science…
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πŸ‘€︎ u/careerthrowaway10
πŸ“…︎ Apr 07 2020
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Cordycepin Modulate Body Weight by Reducing Prolactin via an Adenosine A1 Receptor preprints.org/manuscript/…
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πŸ‘€︎ u/Disturbed83
πŸ“…︎ Jun 01 2018
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Is there a way to prevent adenosine A1 receptor upregulation?

Is there a way to prevent adenosine A1 receptor upregulation. As everyone knows, caffeine causes an upregulation and sensitization for the neural and peripheral adenosine a1 receptors. I'm wondering if there's any supplement that could possibly halt or slow down this process? I know Curcumin is an a1 agonist, so maybe that would be of use? Any thoughts would be appreciated.

Thanks

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πŸ‘€︎ u/HappyMosizwe
πŸ“…︎ Dec 12 2016
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Anxiolytic Effect of Exogenous Ketone Supplementation Is Abolished by Adenosine A1 Receptor Inhibition in Wistar Albino Glaxo/Rijswijk Rats.2018 ncbi.nlm.nih.gov/pubmed/2…
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πŸ‘€︎ u/spyderspyders
πŸ“…︎ Dec 15 2018
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Increased Signaling via Adenosine A1 Receptors, Sleep Deprivation, Imipramine, and Ketamine Inhibit Depressive-like Behavior via Induction of Homer1a. - PubMed ncbi.nlm.nih.gov/pubmed/2…
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πŸ‘€︎ u/Disturbed83
πŸ“…︎ Jun 01 2018
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Regulation of Hippocampal Cannabinoid CB1 Receptor Actions by Adenosine A1 Receptors and Chronic Caffeine Administration: Implications for the Effects of Ξ”9-Tetrahydrocannabinol on Spatial Memory ncbi.nlm.nih.gov/pmc/arti…
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πŸ‘€︎ u/PrinceMachiavelli
πŸ“…︎ Dec 16 2013
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Cordycepin Modulate Body Weight by Reducing Prolactin via an Adenosine A1 Receptor preprints.org/manuscript/…
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πŸ‘€︎ u/Disturbed83
πŸ“…︎ Jun 01 2018
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Caffeine occupancy of human cerebral A1 adenosine receptors: in vivo quantification with 18F-CPFPX and PET. (2012) ncbi.nlm.nih.gov/pubmed/2…
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πŸ“…︎ Jan 31 2016
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Complex formation and functional interaction between adenosine A1 receptor and type-1 metabotropic glutamate receptor (2015) sciencedirect.com/science…
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πŸ‘€︎ u/dysmetric
πŸ“…︎ Jun 23 2015
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Combined neuroprotective action of adenosine A1 and cannabinoid CB1 receptors against NMDA-induced excitotoxicity in the hippocampus [2015] sciencedirect.com/science…
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πŸ‘€︎ u/roionsteroids
πŸ“…︎ Jun 15 2015
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[Science] A ketogenic diet suppresses seizures in mice through adenosine A1 receptors jci.org/articles/view/578…
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πŸ‘€︎ u/xmnstr
πŸ“…︎ Jul 08 2011
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"Control of cannabinoid CB1 receptor function on glutamate axon terminals by endogenous adenosine acting at A1 receptors" (2010) ncbi.nlm.nih.gov/pmc/arti…
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πŸ‘€︎ u/Ballaticianaire
πŸ“…︎ May 20 2015
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Physiological roles of A1 and A2A adenosine receptors in regulating heart rate, body temperature, and locomotion as revealed using knockout mice and caffeine. (2009) ncbi.nlm.nih.gov/pubmed/1…
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πŸ‘€︎ u/ribroidrub
πŸ“…︎ Jul 29 2014
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Cordycepin Increases Nonrapid Eye Movement Sleep via Adenosine Receptors in Rats ncbi.nlm.nih.gov/labs/pmc…
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πŸ‘€︎ u/Experienced8
πŸ“…︎ Oct 29 2021
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Adenosine Receptors Modulate the Exogenous Ketogenic Supplement-Evoked Alleviating Effect on Lipopolysaccharide-Generated Increase in Absence Epileptic Activity in WAG/Rij Rats. (Pub Date: 2021-11-15)

https://doi.org/10.3390/nu13114082

https://pubmed.ncbi.nlm.nih.gov/34836344

Abstract

It has been previously demonstrated that KEKS food containing exogenous ketogenic supplement ketone salt (KS) and ketone ester (KE) decreased the lipopolysaccharide (LPS)-generated increase in SWD (spike-wave discharge) number in Wistar Albino Glaxo/Rijswijk (WAG/Rij) rats, likely through ketosis. KEKS-supplemented food-generated ketosis may increase adenosine levels, and may thus modulate both neuroinflammatory processes and epileptic activity through adenosine receptors (such as A1Rs and A2ARs). To determine whether these adenosine receptors are able to modify the KEKS food-generated alleviating effect on LPS-evoked increases in SWD number, an antagonist of A1R DPCPX (1,3-dipropyl-8-cyclopentylxanthine, 0.2 mg/kg) with LPS (50 Β΅g/kg) and an antagonist of A2AR SCH58261 (7-(2-phenylethyl)-5-amino-2-(2-furyl)-pyrazolo-[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine, 0.5 mg/kg) with LPS were co-injected intraperitoneally (i.p.) on the ninth day of KEKS food administration, and their influence not only on the SWD number, but also on blood glucose, R-beta-hydroxybutyrate (R-Ξ²HB) levels, and body weight were measured. We showed that inhibition of A1Rs abolished the alleviating effect of KEKS food on LPS-generated increases in the SWD number, whereas blocking A2ARs did not significantly modify the KEKS food-generated beneficial effect. Our results suggest that the neuromodulatory benefits of KEKS-supplemented food on absence epileptic activity are mediated primarily through A1R, not A2AR.

------------------------------------------ Info ------------------------------------------

Open Access: True

Authors: Brigitta Brunner - Csilla Ari - Dominic P. D’Agostino - Zsolt KovΓ‘cs -

Additional links:

https://www.mdpi.com/2072-6643/13/11/4082/pdf

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πŸ‘€︎ u/Ricosss
πŸ“…︎ Nov 29 2021
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If you continually drank caffeine enough to block any adenosine from getting into its receptors, could you theoretically stay awake indefinitely and never get tired, until you died from sleep deprivation?

From what I understand about caffeine, it attaches itself to adenosine receptors because it’s chemically pretty similar to it. Adenosine, the chemical that tells your brain that you’re tired and need sleep, gets blocked out of the receptors, and you don’t feel tired. If adenosine has already reached and attached to the receptors, then caffeine won’t work as effectively.

However, if you started drinking caffeine before you ever got tired at all, and kept drinking enough to prevent any adenosine from leaking through, could you stay awake and alert indefinitely?

Obviously not gonna try this, as prolonged sleep deprivation can cause all sorts of health issues, and excessive caffeine intake can as well, but would this actually work?

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πŸ‘€︎ u/MaskerPlayz
πŸ“…︎ Nov 25 2021
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So i know caffeine works by commandeering adenosine receptors...

here's a case scenario:

Lets say that i'm not a regular caffeine user. i've just woken up about 2 hours ago and i'm fully awake. I decide out of the blue to have a half a cup of coffee, even though i don't feel like i need it. as a result i feel more energized and focused.

since caffeine doesn't actually "give" you energy, but replaces adenosine in receptors so you don't feel as tired, i would imagine that the only reason caffeine would give a non caffeine dependent person energy in the morning time would be because their sleep quality is not optimal. even though it's hard to imagine the best of sleepers to not feel energized from a cup of coffee, i wonder about this.

is there something else about caffeine that produces the psychoactive effects of focus and energy?

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πŸ‘€︎ u/PapaDomino9923
πŸ“…︎ Sep 22 2021
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Have we tried reducing adenosine receptor count?

Full disclosure: I found nothing on this online, which makes me think it's probably a stupid nonsensical idea.

It seems like the main concern with nootropics is the maintenance of a sustained positive effect: even if you find something that works for you, you typically hit tolerance issues sooner or later. So we (or at least, I) end up looking for new substances that could provide the desired boost, or resort to cycling.

One of the strongest nootropics out there is caffeine, which works, in part, by blocking adenosine receptors. The tolerance, at least to the wakefulness/stimulant effects, seems to be a result of additional adenosine receptors our brains develop in response to routine caffeine administration (note: based on a quick lit review, this may not be the only pathway, but it at least seems worth experimenting with).

So this leads to my naive, uninformed question: what if we developed an intervention that targets adenosine receptor count/growth, downregulating it? Could we then enjoy caffeine without worrying as much about tolerance, maintaining its powerful effect? Has something like this been explored/considered?

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πŸ‘€︎ u/ablasionet
πŸ“…︎ Jul 20 2021
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Increasing Dopamine receptors through increasing Adenosine? Supplements in addition?

Adenosine prevents release of Dopamine, Acetylcholine and Noradrenaline. If I quit dopaminergic substances at the same time as increasing Adenosine, this should theoretically cause a deficit in Dopamine, which in turn should cause an upregulation of Dopamine receptors. Do you guys think this will work out?

Also, do you have any supplement recommendations for me to add during my break? Thanks a bunch!

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πŸ‘€︎ u/Bavarian0
πŸ“…︎ Sep 16 2021
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Caffeine fully blocks antidepressant-like effect of Creatine in mice [requires Adenosine receptors] (2015) ncbi.nlm.nih.gov/pmc/arti…
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πŸ‘€︎ u/Regenine
πŸ“…︎ Sep 24 2020
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Stimulation of adenosine receptors in the nucleus accumbens reverses the expression of cocaine sensitization and cross-sensitization to dopamine D2 receptors in rats.2012 ncbi.nlm.nih.gov/pmc/arti…
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πŸ‘€︎ u/spyderspyders
πŸ“…︎ Mar 20 2021
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Limonene has anti-anxiety activity via adenosine A2A receptor-mediated regulation of dopaminergic and GABAergic neuronal function in the striatum.2021 pubmed.ncbi.nlm.nih.gov/3…
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πŸ‘€︎ u/spyderspyders
πŸ“…︎ Mar 07 2021
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Interactions Between Adenosine Receptors and Cordycepin (3'- Deoxyadenosine) from Cordyceps Militaris: Possible Pharmacological Mechanisms for Protection of the Brain and the Amelioration of Covid-19 Pneumonia , clinical studies review , [ 06 - 2021 ]

At present, the novel Covid-19 pneumonia is prevalent, affecting millions of people. Here, we summarized the pharmacological basis of adenosine, adenosine receptors, adenosine agonist cordycepin (3'- deoxyadenosine), and Cordyceps product in the brain protection and amelioration of pneumonia to provide useful information to cope with the global pandemic of novel coronavirus (COVID-19).

Adenosine, a mediator of innate immunity, is abundantly secreted by the injured lung tissues during inflammation. Through the activation of adenosine receptors A1, A2A, A2B and A3, adenosine plays an important role in protecting against acute lung injury and brain injury.

Cordycepin (3'-deoxyadenosine) is an activator of adenosine receptors. It can enhance human immunity, promote anti-inflammatory processes, inhibit RNA virus reproduction, protect against brain, lung, liver, heart, and kidney damage, and ameliorate lungfibrosis in clinical and animal models.

Cordyceps and cordycepin products could be used as a potential medicinal adenosine receptor agonist that can play a beneficial role in the amelioration of Covid-19 pneumonia and protection of brain .

Full text :

- https://fortunepublish.com/articles/10.26502.jbb.2642-91280035.pdf

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πŸ‘€︎ u/Sorin61
πŸ“…︎ Jul 03 2021
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Univ of Bonn researchers find that older mice with drug-activated adenosine A2B receptors become much fitter and as healthy as younger mice. They then compared the fat cells and pathways in the mice with human cells and found they were essentially the same, meaning it should do the same with people sciencedirect.com/science…
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πŸ‘€︎ u/snooshoe
πŸ“…︎ Jul 03 2020
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Can the similarities between adenosine and caffeine have an impact on your mind? Yes, it certainly can. According to research, the receptor cells in our brain bind with caffeine rather than adenosine, preventing the brain from slowing down. However, withdrawal symptoms can be observed after 24 hours youtu.be/3psZUq8XaTE
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πŸ“…︎ Jul 12 2021
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Transient Receptor Potential Vanilloid 4 Regulation of Adenosine Triphosphate Release by the Adenosine Triphosphate Transporter Vesicular Nucleotide Transporter, a Novel Therapeutic Target for Gastrointestinal Baroreception and Chronic Inflammation karger.com/Article/Fullte…
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πŸ‘€︎ u/Robert_Larsson
πŸ“…︎ May 24 2021
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If adenosine is already bound to it’s receptors does it block caffeine?

I was curious about this. If adenosine is already in its receptors, can it block caffeine from binding?

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πŸ‘€︎ u/ATLTriumph
πŸ“…︎ Oct 15 2021
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