Opioids Super strong natual Opioid Peptides

[KinoTheBlueElf]

Anyone heard of an Opioid Peptide? Its some sort of opiate produced within living things like how endorphins are. There's this really powerful one I found called Dermorphin.

From Wikipedia:

Dermorphin is a hepta-peptide first isolated from the skin of South American frogs belonging to the genus Phyllomedusa. The peptide is a natural opioid that binds as an agonist with high potency and selectivity to mu Opioid receptors. Dermorphin is about 30-40 times more potent than morphine but less likely to produce drug tolerance and addiction.

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[sekio]

The problem with opioid peptides is that they cross the blood brain barrier only poorly (because they're peptides) and are very unstable.

As far as I know dermoprhin is the active ingredient in "sapo", a drug administered by rubbing frog venom into burn blisters. The experiences on the whole seem very unpleasant and not anything like the "classical" opioids.

Few Westerners have partaken in the sapo ritual, but there is one consistency in their reports. Within moments of administration, one falls wretchedly ill; nausea; vomiting; facial flush; rapid heart rate; stomach ache; loss of bladder and bowel control; sweating; and lachrymation. This generally lasts 15 minutes or so, but once this adverse reaction resolves the user feels invigorated, and sapo’s therapeutic effects are said to last several days.

[...]

After burning me, E then applied saliva to the sapo stick, and using a knife scraped up the sapo into gum-like clumps. He then daubed the sapo onto the burned area of skin with the knife.

The onset of sapo was inordinately rapid--within 1 minute of application. I’m still quite impressed by its fast onset. I initially felt a mild throbbing sensation on my thigh, followed by a noticeable increase in heart rate and faintness. My vision started to go a bit blurry, as though not enough oxygen was getting to my brain. This feeling was more odd than unpleasant, but increased in severity quite rapidly.

[...]

Over the next 15 minutes, I was confronted with a host of ailments. My throat, mouth, tongue and lips became inflamed, with the same numbness I imagine getting punched in the mouth or having a bad allergic reaction would feel. My mouth was extremely dry. My heart was racing and I was sweating. And for some reason my eyes wept profusely. I could hardly speak. I mumbled to T to get me some water. Unable to muster the strength to sit upright, I lay sprawled out on the floor and drank the water sideways.

The burn on my thigh was killing me and I was overwhelmed with anxiety. When the fuck is this going to end? I had the persistent feeling that I was going to barf without a moment’s warning. I also experienced bowel distension. I got the impression that if my bowels weren’t empty then I’d have likely soiled myself as a matter of course.

The remainder of this period is a blur, but I recall that in this state I had a frank and extensive inner-monologue as to why I like to subject myself to these sorts of things. I kept thinking to myself that the after-effects of sapo had better be worth it, because this physical feeling simply pointed to sapo being more like a poison than a medicine.

This sounds like a Salvia-type compound: too powerful to be anything more than a novelty.

The experience sounds to me (suprisingly) like getting poisoned by frog venom. You know the kind - toxic amazonian rainforest forgs used by the natives to paralyse and kill animals.

 

[Coraline]

That sounds pretty crazy to me. I think I'll stick to modern medication like lidocaine and pain relievers.

 

[PoppyLlama]

there have been threads made about this previously on BL and other places: the decision was that it's not that recreational, doesn't much cross the BBB. And it is really hard to store, and SUPER expensive

 

[Fail Fighter]

You're better off eating cheese.

http://en.wikipedia.org/wiki/Casomorphin

 

[THC2LSD]

The problem with opioid peptides is that they cross the blood brain barrier only poorly (because they're peptides) and are very unstable.

I think there is some synthetic ones that do cross the blood-brain barrier and have longer half-lives. Also one called dalargin, a Russian opioid peptide ulcer drug that normally doesn't cross the BBB, but will with the magical polysorbate 80 PBCA nanoparticles(uh oh). Can't find much in English at least about dalargin. The nanoparticles work by binding to apolipoproteins and hitching a ride into the brain. Also works with some drugs that already cross the blood-brain barrier.

I remember that guy on that Discovery Channel show "Going Tribal" said that sapo was the second most intense experience he's had in his life, after iboga.

 

[sekio]

Anything will cross BBB with polysorbate nanoparticles, it's essentially mixing the compound into soapy little bubbles.

 

[Sprout]

Someone mentioned PS80 nanoparticles and opiods, I'm awaiting a loperamide derailment...

 

[THC2LSD]

^LOL, hopefully not8(.

 

[mindash]

if much loperamide was to readily cross the BBB ne would more likely experience a state (possibly permanent) of somthing very strongly akin to parkinson's disease according to everything ive read regarding the matter. i know in high enough doses my vision goes quite screwy and bug eyed from it which i would not wish to experience on a stronger level what so ever

 

[Gaz_hmmmm]

if much loperamide was to readily cross the BBB ne would more likely experience a state (possibly permanent) of somthing very strongly akin to parkinson's disease according to everything ive read regarding the matter. i know in high enough doses my vision goes quite screwy and bug eyed from it which i would not wish to experience on a stronger level what so ever

Why do you think you'd experience Parkinson's like symptoms if 'enough' loperamide crossed the BBB? It's related to methadone and pethidine from what I know and also I've seen on other opioid websites people using loperamide to detox and usingg around 50mg a day for about a week and apparently they say it completely stops cold turkey from Oxy'/diamorphine withdrawl.

I'd love to test this but have an immune diorder that unfortunately means if I go into withdrawl I'll die if I don't get immediet med' attention.

 

[THC2LSD]

Oh God, SproutOnSmack was right. I feared this would happen.

Loperamide metabolize into something similar to MPTP, an impurity in the designer opioid MPPP. MPTP selectively kills off dopamine cells, causing Parkinson's. A similar drug haloperidol also metabolizes into something similar to MPTP. It can cause Parkinson's too, though it may mainly be because it's a dopamine antagonist and not a very strong antichlolinergic. The metabolite may play a role though.IME I can say haldol is some nasty shit, only lithium is worse.

Some think loperamide might not be like MPTP, but it'd suck to be the guinea pig to test this. And someone said that they took quinidine to let loperamide work but it sucked. Quinidine has some shitty, potentially lethal side effects, particularly in doses to block PGP. And a later study casts doubt on PGP inhibitors working. They used a potent selective PGP inhibitor to see if loperamide would work, it didn't. Although it may have been due to PGP in the gut. Fuck, the first study only looked for constricted pupils and respiratory depression.

I will say AFAIK that everything anyone's tried online with supposed loperamide nanoparticles is wrong and will not work. I could see a pathogen or nasty chemical hitching a ride into the brain if not done properly, stuff that would normally be harmless. And I think it's not so much the surfactant action of PS80 that works as the binding to apolipoprotein E that occurs in vivo. PS80 just causes it to combine with apolipoproteins, it'll work with just them with no PS80.

Lets get back on topic. How potent are those casomorphins? Do they have any opioid effects besides histamine release, even intrathecally? What about in humans? That would be crazy if there was an opioid made from milk!

Are there any other opioid peptides in other animals? Will some work with enzyme inhibitors(forgot which) like a DMT/MAOI combo?

 

[KinoTheBlueElf]

Lets get back on topic. How potent are those casomorphins? Do they have any opioid effects besides histamine release, even intrathecally? What about in humans? That would be crazy if there was an opioid made from milk!

Thats how I found about these, from reading the Wikipedia article on Milk. Not really sure about the other stuff, I'm gonna have to research some more info about it.

 

[sekio]

Caseomorphins would have an opioid effect if administered intrathecally, but lots of drugs have effects if instilled directly into the CSF...

I don't think anyone is going to go so far as hydrolysing milk on a large scale to make IT painkillers.

 

[THC2LSD]

^Yeah it was half joking, half wishful thinking. No way could intrathecal drugs be used outside of a hospital.

 

[Elilrac]

I once read of some sea creature that produces thc.

 

[mindash]

basically what THC2LSD said covers it but ive seen a few articles online talking about it as well. just google loperamide and parkinson's, somthing should come up

 

[tanfan]

I heard somewhere that this caseomorphin that you mentioned is a possible reason some people feel addicted to eating cheese, being dairy's opiate and all.

 

[The Dope Man]

I once read of some sea creature that produces thc.

I know what your talking about.

its like a sea cucumber or something. It dosent produce THC. it has canabinoid receptors and it was like the first living organism with canabinoid receptors or something.

I saw a youtube video on it ill try to find it

EDIT: FOUND IT

 

[pbuilder]

The ole' licking frogs to get high.