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A Cannabinoid Enhancer In Your Medicine Cabinet?

Richard Richardson

Well-Known Member
An endocannabinoid enhancer (eCBE) is a type of cannabinoidergic drug that enhances the activity of the endocannabinoid system by increasing extracellular concentrations of endocannabinoids.

An example of an actual eCBE is AM404, the active metabolite of the analgesic Paracetamol (acetaminophen; Tylenol).

Endocannabinoid enhancer - Wikipedia, the free encyclopedia

Other than toxicity research and recreational use, eCBRIs could have some potential in fighting tumors and possibly cancer. A study done in 2004 on rats with thyroid tumors showed that reuptake inhibition of the endocannabinoid system using VDM-11 and AA-5-HT reduced the ultimate size of the tumors in the treated rats. These findings suggest that the use of cannabinoids and/or eCBR inhibitors could be used to effectively treat tumors and/or cancer, which only adds to the controversy around cannabinoids and the cannabis plant as medicine. Example of eCBRI - AM404

Endocannabinoid reuptake inhibitor - Wikipedia, the free encyclopedia

It stops the cannabinoids from being absorbed so quickly by the synapses and leaves more in between, which means more is available for longer! Plus, they get concentrated where there is most pain.

If it works on endocannabinoids, then it should also stop the reuptake of THC & CBD, thus prolonging the time that they have to work their magic, as well as sending them to the right places.

Any thoughts? :thanks:
 

Anchutz

Active Member
An endocannabinoid enhancer (eCBE) is a type of cannabinoidergic drug that enhances the activity of the endocannabinoid system by increasing extracellular concentrations of endocannabinoids.

An example of an actual eCBE is AM404, the active metabolite of the analgesic Paracetamol (acetaminophen; Tylenol).

Endocannabinoid enhancer - Wikipedia, the free encyclopedia



Endocannabinoid reuptake inhibitor - Wikipedia, the free encyclopedia

It stops the cannabinoids from being absorbed so quickly by the synapses and leaves more in between, which means more is available for longer! Plus, they get concentrated where there is most pain.

If it works on endocannabinoids, then it should also stop the reuptake of THC & CBD, thus prolonging the time that they have to work their magic, as well as sending them to the right places.

Any thoughts? :thanks:

Well, it's been a few years and so I imagine by now anyone who had did have "Any Thoughts?" about this, must have been fleeting ones. It's an interesting subject, did any of this go anywhere?
 

Richard Richardson

Well-Known Member

SweetSue

Well Known Member
Well this was intriguing Richard. I don't see why it'd have any different effect on THC or CBD, since they so closely mirror endocannabinoids. That toxicity to the liver is a bit off-putting.

I found the paper interesting. I'll have to give it another pass later, after Callanetics. I keep getting sidetracked. :laugh2: It has me thinking again that I need to get the pain info posted this weekend. Everywhere I turn today people are in pain.
 

Richard Richardson

Well-Known Member
Hi Sue, here is the important bit :ciao:

In summary, our data provide evidence that AM404 relieves neuropathic pain acting via CB1, CB2 and TRPV1 receptors without producing any relevant cannabimimetic effects and that this action is accompanied by a modulation of nitric oxide and cytokine pathways and by a reduction in the extent of apoptosis occurring in neuropathic animals. Taken together, these findings suggest that the elevation of the extracellular endocannabinoid level might have therapeutic benefit in alleviating neuropathic pain, although the concomitant activation of TRPV1 receptors may be also required. Although less potent or specific as an inhibitor of endocannabinoid uptake than other compounds (VDM11, UCM707), AM404 has the additional advantages of being able to directly activate vanilloid receptors, of exhibiting anti-oxidant properties due to the presence of a phenolic group in its chemical structure and of inhibiting, at least in vitro, purified COX-1 and COX-2 (Hogestatt et al., 2005), activities that could be useful to counteract neurogenic inflammation occurring during neuropathy.

AM404 is the active metabolite of Paracetamol - It concentrates cannabinoids in areas of pain or inflammation. It doesn't mirror cannabinoids, it stops them being broken down/absorbed by the body, allowing them to work longer.
 

SweetSue

Well Known Member
Hi Sue, here is the important bit :ciao:



AM404 is the active metabolite of Paracetamol - It concentrates cannabinoids in areas of pain or inflammation. It doesn't mirror cannabinoids, it stops them being broken down/absorbed by the body, allowing them to work longer.

Makes me wish I'd taken chemistry in high school. Now I'll have to find a way to learn the fundamentals so I can understand pathways.
 
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