Opiorphin endogenous peptide opioid

[jacky]

dont know how this has escaped me for so long....

"Natural-born painkiller
found in human saliva

Saliva from humans has yielded a natural painkiller up to six times more powerful than morphine, researchers say. The substance, dubbed opiorphin, may spawn a new generation of natural painkillers that relieve pain as well as morphine but without the addictive and psychological side effects of the traditional drug.
When the researchers injected a pain-inducing chemical into rats’ paws, 1 gram of opiorphin per kilogram of body weight achieved the same painkilling effect as 3 grams of morphine."




very interesting. gives credence to the idea that licking ones wounds is a defense and immune booster.


I read somewhere, trying to look up the chemical structure of the compound, that its easily synthesized, and in large amounts apparently.


I know some peptides, probably most peptides cant just be used like other opioid/opiate compounds.
but perhaps there is a way for this compound to be used.


its rather amazing, how many opioids exist in nature, and just how prolific/ubiquitous they can really be...in our spit, our blood, in all types of body tissues and organs peppered throughout many living beings.....
in frogs,
mollusks
mammals, plants, and for all we know, there is a mineral opioid active substance out there ....


great name on this compound...and also great media knowledge to spread...
"hey, fight the drug war, human saliva has a compound that is nearly as potent as heroin!"
I am confused to as if this compound would be active in our bodies...or if we have such a natural defense to the compound as to render it almost non active


what a strange world it would be if the next big thing was a factory of cloned saliva glands churning out tanks of opiorphin that is then crystallized and ground to a fine powder....perhaps the substance could be grown in vats of bacteria.....
a global police force trying to stop a wave of opiorphin production and initially that legal window of opportunity that resourceful entrepeneurs take advantage of.
quick scheduling turns every person's and possibly mammals mouth into an illicit drug production factory.


I wonder what the concentration in saliva is normally?


a person produces alot more saliva than you would think
wiki reports that around .75 liters to 1.5 approx per person.
if saliva is just 1% in opiorphin content, that that is ALOT of analgesic potential just in a persons daily saliva production!
of course opiorphin content could be quite low, literally trace amounts.
Ill have to look up and see if there is any ratio's listed in the research that I can understand.

[hovadagod]

Wow...I'll be spitting in a cup for a while. Solvents?

[duck]

*draws up syringe w/ needle in mouth*

[30_Units]

Vurry interesting. The list keeps growing of where opioids are found in nature.

[Thai_Stick]

I want to make it very clear that NOBODY should be yakking loogies down their barrels without first boiling them! Once sterilized you're fine though :P

I've actually read about analgesics in saliva before, but was never given enough detail to really look into it further. Very intriguing. I hope one of our resident chemists will give us the status report on the outlook for this soon.

[hovadagod]

Is this stuff legal to procure?

[ryan]

Any more info on this?
There's gotta be a catch somehow, like 0.000005% or something.

[ryan]

So anyways --- what if SWIM were to get ahold of some of this compound...how exactly would you take it?
I mean it's a peptide so you can't just eat it....hm...

[jacky]

I dont know how one would take it...but I reckon that browing it would/might work.
possibly this substance doesnt cross the BBB...and who knows what other uses the body has for a compound this potent.

I think that the possiblity that opiorphin has analogs that are active is pretty good...but then again, I am not a chemist, and know little about peptides other than they are not as exciting as people initially think. (though they have more potential than many give them credit!)

maybe all one needs to do, it brown some saliva....as gross as that sounds, feels, and smells.

heh heh.

I am more excited about the implications of this compound, than the hedonistic possibilitys.

one thing that should be considered....with the certian types of beverages that contain human spit as a yeast/alcohol inducer, is that possiblity that opiorphin might just have some activity when mixed with other substances.

[Paregoric Kid]

when I first read this I wondered how an opiate agonist could have such properties, it turns out that it isn't an agonist of any of the opiate receptors. it just increases the levels of certain endogenous opiates, called enkephalins, by preventing their breakdown through metabolism. I thought opiorphin sounded similar to thiorphan, a compound that acts as an enkephalin reuptake inhibitor. opiorphin is kind of similar, it prevents the reuptake of enkephalins (and possibly endorphins?) through inhibiting 2 enkephalin-catabolizing enzymes, neutral ecto-endopeptidase (MME) and ecto-aminopeptidase N (ANPEP). so its kind of like an SSRI but instead of increasing serotonin through inhibiting the breakdown of serotonin its increasing enkephalin through inhibiting the breakdown of enkephalin.
also one study suggests that in rats opiorphin is only equivalent to morphine in terms of analgesic effect. in this study and others they compared its effects to thiorphan:

Human Opiorphin, a natural antinociceptive modulator of opioid-dependent pathways
Anne Wisner,* Evelyne Dufour,* Michaël Messaoudi,† Amine Nejdi,† Audrey Marcel,* Marie-Noelle Ungeheuer,‡ and Catherine Rougeot*§
Abstract
Mammalian zinc ectopeptidases play important roles in turning off neural and hormonal peptide signals at the cell surface, notably those processing sensory information. We report here the discovery of a previously uncharacterized physiological inhibitor of enkephalin-inactivating zinc ectopeptidases in humans, which we have named Opiorphin. It is a QRFSR peptide that inhibits two enkephalin-catabolizing ectoenzymes, human neutral ecto-endopeptidase, hNEP (EC 3.4.24.11), and human ecto-aminopeptidase, hAP-N (EC 3.4.11.2). Opiorphin displays potent analgesic activity in chemical and mechanical pain models by activating endogenous opioid-dependent transmission. Its function is closely related to the rat sialorphin peptide, which is an inhibitor of pain perception and acts by potentiating endogenous μ- and δ-opioid receptor-dependent enkephalinergic pathways. Here we demonstrate the functional specificity in vivo of human Opiorphin. The pain-suppressive potency of Opiorphin is as effective as morphine in the behavioral rat model of acute mechanical pain, the pin-pain test. Thus, our discovery of Opiorphin is extremely exciting from a physiological point of view in the context of endogenous opioidergic pathways, notably in modulating mood-related states and pain sensation. Furthermore, because of its in vivo properties, Opiorphin may have therapeutic implications.

I could see drugs being developed from opiorphin and thiorphan that end up being used as antidepressants and as an adjunct to other analgesics. I don't believe these types of drugs will ever replace opiate agonists.