The loperamide of cannabinoids

[Reminisant B]

Does anyone know of a cannabinoid affecting CB1 or CB2 receptors that does not pass the blood brain barrier?

All the ones read about seem particularly good at this.

 

[vecktor]

Does anyone know of a cannabinoid affecting CB1 or CB2 receptors that does not pass the blood brain barrier?

All the ones read about seem particularly good at this.

surely if it was a selective cb2 ligand then it wouldn't matter too much that it crosses the BBB as there a are relatively few CB2's in the brain and CB2 agonism is not associated with the undesirable (depending on who you are) effects of getting you high. I think that is the approach that is being taken by the pharmaceutical companies.
I would be interested in a mixed CB1 CB2 agonist that didn't cross the BBB, as it would almost certainly have to be a water soluble creature too
V

 

[LuxEtVeritas]

yeah, if it is CB2 specific it does not really matter

CB1 is interesting though as i believe a somewhat purely orexigenic substrate could be had if it did not cross BBB and have psychoactive effect

Then again though i think the orexigenic effect of cannabis is via indirect mechanism of stimulating Ghrelin which then leads one to perhaps say just go and use the direct substrate

 

[The Monkey Mantra]

surely if it was a selective cb2 ligand then it wouldn't matter too much that it crosses the BBB as there a are relatively few CB2's in the brain and CB2 agonism is not associated with the undesirable (depending on who you are) effects of getting you high. I think that is the approach that is being taken by the pharmaceutical companies.
I would be interested in a mixed CB1 CB2 agonist that didn't cross the BBB, as it would almost certainly have to be a water soluble creature too
V

I'm imagining a hydrophobic end (to fit into the receptor) with a hydrophilic tail, keeping it out of the brain. Kinda like a soap!

 

[Reminisant B]

^That's what I was imagining myself, wonder if it would work. Possibly it might just be a good surfactant.

a non-psychotactive cannabinoid would be incredibly profitable for inflammatory conditions of the GI tract.

 

[LuxEtVeritas]

CB2 again is more indicated in inflammation and thus BBB issues are moot as CB2 is NOT psychoactive

 

[Splatt]

What makes cannabis give you such a nice refreshed long sleep?
I can't smoke weed anymore, don't like the effects, but weed sleep was always the best. I'd love that chemical(s) in a non psychedelic pill.

 

[Recept]

^ Try melatonin supplements. I use those when I'm abstinent from weed and they seem to help a great deal with sleep problems I usually get from cannabis WD. Which kinda makes sense, because cannabis enhances endogenous production of melatonin.