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Acetaminophen as cannabinoid pro-drug

Isn't the more important question "How can we modify APAP so that it can be metabolized into a CB1 agonist?"
 
I don't know that anyone would want AM414. It's not psychoactive.

Structurally, APAP bears no resemblance to any psychoactive cannabinoids so it makes no sense to start with it for that purpose.

Olivetol, OTOH...
 
No, I don't mean as a precursor. Couldn't modifying APAP's structure cause it to metabolize differently, possibly into an active cannabinoid?
 
Maybe if you coupled it with anandamide and took a FAAH inhibitor.. but I hear the amide gets cleaved anyway.

I dont know if thats true, though.
 
A couple of weeks ago I spoke with a drug expert in my country and he told me that paracetamol, in large doses, is used in prisons as a substitute when other drugs are unavailable. I wondered. The paper clarified this issue for me.
 
I think nobody's claiming that APAP gets you high or that an anandamide reuptake inhibitor should have the same effects as a direct agonist*.

But I find it odd that something with this mechanism of action should have no psycho-effect at all (assuming it gets to the brain). I think I do feel better when I take APAP for mild pain, but obviously that's easily explained by the pain relief :) As has already been said, be careful of liver toxicity.

* It doesn't for other neurotransmitters.
 
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No, nothing of the sort at all, I have known someone who routinely would dose several grams of APAP at a time (I wonder if shes still around sometimes..) and she never described any effects other than sleepiness. To sum it up THC does what APAP does, and both can relieve pain, but APAP doesn't do what THC does, except for that one effect. IME, APAP can greatly potentiate THC as an analgesic, but on its own, its quite limited.
 
We'll be seeing about that tonight in my incredibly unscientific "pop some Panadols before smoking up" trial :p .
(In all seriousness though, I too would like to hear a proposed mechanism)
 
As I understand, one of the effects of THC is the same effect APAP has at one specific receptor site, which would explain at least part of THC's analgesic qualities.
 
Have you seen that:
the anaesthetic agent propofol and the non-steroidal anti-inflammatory drugs indomethacin and flurbiprofen (when given spinally), activate cannabinoid receptors as an important part of their actions.
Pubmed
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not surprised

obviously the Endocannabinoid system is a complex system that serves many purposes and one key area is analgesic

a fair amount of substrates likely can elicit this effect while far fewer can potentiate the additional aspects elicited by substrates such as THC et al can
 
As I understand, one of the effects of THC is the same effect APAP has at one specific receptor site, which would explain at least part of THC's analgesic qualities.

So you're saying if I took codeine with my morphine the codeine would potentiate the morphine because they both work on the same receptor sites?
 
Acyl said:
So you're saying if I took codeine with my morphine the codeine would potentiate the morphine because they both work on the same receptor sites?
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^^isn't it the case?
 
well, codeine and morphine isn't a very good example. How about Morphine and Hydromorphone.

I'm sure they'll have additive effects, possibly synergise, but potentiate? Probably not.

I assume we're considering that "potentiate"is to increase by increasing bioavailability, decreasing metabolism, and "synergise" is do something mysterious to increase the effects, where (A + B) = C where C > (A + B). And where A + B = C and C = A + B, there isn't synergy, but two seperate drugs doing the same thing at the same time.

Is that final clause considered potentiation or not? I don't really know.

I do love semantic math involved, though.

Anyway, I do indeed think that THC + AM404 will yield a "C" that's more than the literal sum of the two parts- but probably not when considering the psychoactive effects. I'd assume that AM404 has a higher binding affinity and may indeed decrease the psychoactive effects of THC because of competition at binding sites.
 
MattPsy said:
We'll be seeing about that tonight in my incredibly unscientific "pop some Panadols before smoking up" trial :p .
(In all seriousness though, I too would like to hear a proposed mechanism)
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If I've got a bad headache, typically I'd take 2 grams of APAP, but if i've happen to have a spliff to smoke, 1 gram will do quite nicely. :)
 
jasoncrest said:
^^isn't it the case?
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No, that doesnt make any sense.

Codeine wouldnt increase morphines potency, if anything it would decrease it.

It just synergizes, as hammilton said. The drugs stack.
 
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