Are there such things as opioid receptor reuptake inhibitors? As a chronic pain patient, I feel as though the existence and concomitant use of one of these with a full agonist opioid could drastically improve analgesia. Anyone ever heard of such a thing/the development of one? Might go into drug R&D and, if so, may have found my money maker if one doesn't exist lmao...
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N&PD Moderators: Skorpio
Existence of µ/κ/σ-reuptake inhibitors?
- Thread starter Jktm
- Start date
sekio
Bluelight Crew
I don't think endogenous opioids are uptaken so much as destroyed. Yes, there are endorphin/enkephalin hydrolase inhibitors but none have been reslly developed for use in humans.Ah, thanks for the input...I know I'm pretty useless in ADD, but I'd say I'm not too shabby considering I'm still working on my A.S. and just really started the self-education process everyone here knows about so well in the past year...well...only got deep into it in the past year lol...I remember hearing about one. It might have been in the California poppy or lettuce opium.
Nagelfar
Bluelight Crew
Wild lettuce inhibits the enzymes which breaks down endogenous opioids. Not the same thing.Well then I don't think that's what I came across.
Nagelfar
Bluelight Crew
The mechanism wouldn't make sense because there is no opioid re-uptake system.I was speaking of the hydrolase inhibitor (really)
Gaius
Bluelighter
- Joined
- Jul 4, 2011
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- 75
Not to say that humans don't use 'em! D-phenylalanine seems pretty common and is a carboxypeptidase A6 inhibitor.
EDIT: Stray apostrophe.Last edited:MrFister
Bluelighter
Reuptake inhibitors are intended for abundant neuro-transmitters, especially ones that are crucial to communication and function. To my knowledge, endogenous opoids are released when they body undergoes sensations of pain. Common neuro-transmitters are released frequently and therefore benefit more from re-uptake, as re-uptake allows a build up so to speak of the neurotransmitter. Are there even any endogenous ligands for the sigma receptor? I can't seem to think of any
ebola?
Bluelight Crew
Why would a cell produce a receptor with no endogenous ligand?
ebola
Good point. This is a myth held on to by over spiritualised hippies, as opposed to drop out stoner hippies like me. The myth is and has been on the decline ever since i got into pharmacolgy (last 10 yrs). This reminds me when i was an undergrad. All the smokers where real proud that there was no endogenous ligand for the THC receptor. Anandamide was discovered the following year.
ebola?
Bluelight Crew
heh...upon second glance, though, the answer is, when it wants to sense the presence of some exogenous compound. But yeah, this'd be pretty weird for brain neurons to do.
ebolaThat's intetesting, i never thought of that before. That's how the immune system works after all though. The only trouble with this theory is that the immune system works on the blood before it gets to the brain. This is ofcourse the bain of every drug user - the 1st and 2nd pass through the liver of an injested chemical, which is why so many of us turn to vaporising, snorting, injecting etc so as to bypass those bastard liver enzymes.
I like your idea though, its logically sound and could well be true, i'm certainly no authority on whats true and whats not.
Also one last thing, i screwed up on the endogenous ligand for the THC receptor. It was discovered back in 1992, a good 10 years before the date that i thought it was. Must have been when i first read about studies using on rats etc.MrFister
Bluelighter
Perhaps unused receptors could be evolutionary remains of when there was an endogenous ligand? Kind of like how the appendix still remains in the body
atara
Bluelighter
As far as I can tell, it's easier to find things that aren't sigma ligands than it is that are.
http://en.wikipedia.org/wiki/Sigma_receptor#Ligands
http://en.wikipedia.org/wiki/BD1063
qwe
Bluelight Crew
more likely, assuming the cell makes a receptor that responds only to an exogenous compound, what if the "receptor" could simply be a vestigial structure with normally no signalling to the cell through that receptor type, but that structure happens to fit with a few molecular shapes found in the environment?
this is a little off topic, but still interesting.
that's not how the sigma receptor operates, though, afaik..
Love that!
Just an observation regarding reuptake proteins and deactivation enzymes: the same transmitter substances can be regulated by both processes. Serotonin for example gets broken down by monoamine oxidase but is also taken back up by the neuron that just fired. So you can get both mechanisms, not that i know about the case of opioid receptors unfortunately.Last edited:opiate/oids work both differently than and similar to the monoamines
