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New legal endorphin analgesics; metkephamid and actinonin!
Hey, good news from the endogenous front, there are two new substances with great potential in terms of euphoria, analgesia and warm glowing warming glow, and at the moment they are totally legal!
The first is metkephamid. The trouble so far with opioid peptides is that they are not systemicallyally acting. What's that mean? You can't snort it, smoke it, shoot it up, and you certainly can't swallow it. This is because they are delicate protein like materials which #1 are too big to cross the blood brain barrier and #2 they are quickly degraded in the body. They are only active via nasty stuff like epidural, intrathecal and cerebroventricular injection [Drilling a bur hole in the skull and slamming the sweet sweet endorphins DIRECTLY INTO THE BRAIN!] Well, it's pretty clear most people wouldn't want that, and wouldn't be qualified even if they did.
For a long time this has rendered endogenous peptides like beta endorphins and endomorphins as mere medical playthings among researchers able to carry out the difficult and dangerous act of administering the peptides by the aforementioned methods.
But now, there is metkephamid, an analog of methionine enkephalin, centrally acting, powerful analgesic agent, so stable and effective they have even done non injection trials [ie, where the sun don't shine], but it certainly works when slammed. The best part is it is not an analog of any existing drug, it is a peptide, and therefore completely legal. Many times more powerful than morphine, it nevertheless is thought to act mainly on the kappa receptor rather than the mu, effecting antinociception via a relatively unstudied pathway. It needs urgent research.
Second, is an interesting new drug with a lot of promise, especially for the opiate naive.
Actinonin [3-((1-((2-[Hydroxymethyl]-1-pyrrolidinyl)carbonyl)-2-methylpropyl)carbamoyl)octanohydroxamic acid] chemical name stolen from site of A. G. Scientific
is a substance that prevents or delays the degradation of of pentapeptides in the brain, and this way boosts the levels of endogenous opioid peptides, effecting analgesia and euphoria!
Unfortunately addiction potential is similar to actual opiates, as the surplus of endogenous opioids triggers a decline in their production. On the bright side, the pleasurable effects are the result of the action of natural substances, so that the decrease in production will only reflect the increased levels of natural peptides, rather than their replacement by outside chemicals. The advantage of this is that the immune and anti cancer properties of natural lipotropins/endorphins.
Actinonin actually has powerful antibacterial and anti cancer effects, so this could well be due to the natural properties of the peptides that are boosted by it. Again, it is systemically active.
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