Coffee Contains Opioid Antagonists

Elephanto

Member
Joined
May 21, 2015
Messages
820
Sci-Hub | Beyond Caffeine: Coffee Contains Opioid Antagonists | 10.1089/jcr.2014.0024

1983, Boubliket al. screened common foodstuffs for opiate receptor binding activity and reported that both normal and decaffeinated coffee contain compounds with binding affinity comparable to that of naloxone.2 These compounds are unrelated to caffeine and were shown to be antagonistic and specific for opiate-induced inhibition of twitch in rats. In the past decade, researchers at the Vanderbilt Institute for Coffee Studies (VICS) have identified these compounds—including 4-Caffeoyl-1,5-quinide (4-CQL)—which are created in the roasting process and ‘‘show in-vivo inhibition of morphine-induced anti-nociceptive behavior in mice with the same order of magnitude as that reported for naloxone.’’3

I think this explains why I get an urge to drink coffee after consuming dietary opioid peptides such as gluten exorphins and casein's casomorphins, and that it relieves feelings of uneasiness and stupor.
 

DavidGardner

Member
Joined
Jul 1, 2015
Messages
165
So would daily coffee consumption upregulate opioid receptor sensitivity? That seems like a good thing.
 
Joined
Apr 8, 2018
Messages
1,142
Location
The Netherlands
...Upregulating of opiod receptor density = less sensitivity, mate. And yes that can be good unless you have restless leg syndrome.
Damn. What a brain fart. Need to correct myself here, sorry. Upregulation happens with an antagonist and results in more sensitivity.
And it seems it is unrelated to the density of the receptors, the following study claims:

The role of opioid receptor density in morphine tolerance. - PubMed - NCBI

"The effect of chronic opioid antagonist-induced functional supersensitivity and receptor upregulation on morphine tolerance was examined in Swiss Webster mice obtained from Taconic Farms and Charles River Laboratories. Mice were implanted s.c. with either naltrexone (NTX) or placebo pellets for 8 days.

...In both tolerance protocols, NTX-pretreated mice were significantly more sensitive to the analgesic effects of morphine than placebo pretreated controls. Binding studies ([3H][D-Ala,2NMePhe4,Gly-ol5]enkephalin) indicated an approximately 40% increase in opioid receptor density with no significant alteration in affinity after chronic NTX treatment. These results indicate that acute and chronic tolerance to morphine develops comparably in control and upregulated, supersensitive mice. These findings suggest that new binding sites in upregulated mice mediate tolerance similarly to existing binding sites and that the degree of tolerance is unrelated to the density of opioid receptors. ..."
 

DavidGardner

Member
Joined
Jul 1, 2015
Messages
165
So the gist of it is that coffee, as an opioid antagonist, like naltrexone, should increase the sensitivity of the opioid receptors. My thoughts were that it would generally be desirable to have more sensitive opioid receptors due to the importance of the endogenous opioid system in mitigating pain and alleviating depression for instance.
 
Joined
Apr 8, 2018
Messages
1,142
Location
The Netherlands
So the gist of it is that coffee, as an opioid antagonist, like naltrexone, should increase the sensitivity of the opioid receptors. My thoughts were that it would generally be desirable to have more sensitive opioid receptors due to the importance of the endogenous opioid system in mitigating pain and alleviating depression for instance.
Yes, I agree. And this higher sensitivity should prevent the urge to abuse opiod like substances to get that high or anti-depressant effect, like in the case of downregulation seen in morphine / heroin addicts.

How does the opioid system control pain, reward and addictive behavior?

edit grammar
 
Back
Top Bottom