Comment · Wed, February 18, 2015 · Ceretropic
Anyone experimented with THT's CNTF fragment 147-150?
Original post in this thread
Debonaire_Death · 5 points
They posted it up awhile ago, and with all of the fuss over P21, it seems to have been swept under the rug.
Has anyone tried it? Is it a good value? I tried to check the price but THT.co is down.
I'm interested in trying another CTNF-related drug, thought it might be worth a shot if there are any good reports out there, but everyone seems busy with GTS-21.
What they were answering
Direct reply to the original post — see the thread post above.
u/MisterYouAreSoDumb · Ceretropic
No!!!! You can't just say, "Ohh, the active sequence in P21 is DGGL, so let's just sell powdered DGGL!" Pharmacodynamics do not work like that! That would be like saying, "Ohh dopamine is good. Let's sell powdered dopamine!" No no no! I have been wary of a lot of THT's new stuff for a while, but their new foray into peptides makes it very clear they do not care about the efficacy of the products they are selling, only the novelty. Sure, selling powdered CNFT fragments and a suspicious powdered Cerebrolysin is novel. But being novel and inactive is useless!
Let's just focus on the DGGL for now. That's aspartic acid-glycine-glycine-leucine. A simple 4 mer peptide that makes up the cognitive effects of the human CNTF peptide. If one were to say inject that right into the brain, then it would probably have some good effects. However, you have to deal with the blood brain barrier, unless you are a researcher doing a mouse study. That is a very big obstacle for a lot of peptides out there. Some are not actively transported across the BBB, which DGGL is not. Then you have to deal with plasma peptidase enzymes in your blood, which rip apart peptide bonds. That's only if you IV the stuff. If you plan on subcutaneous, it takes longer to reach the BBB. If you plan on oral, you have the entire GI tract to contend with. I would bet DGGL is no more than 1% bioavailable, if that. It's probably more like .1% orally bioavailable. Just look at noopept. That is a smaller dipeptide, and has a phenylacetyl group to protect it, and it is only 9% orally bioavailable. A 4 mer peptide with no enzymatic protection? Forget about it.
So that means THT is assuming we are going to inject it then? Well if it is for injection, offering it as a powder in a cosmetics jar is not the way to do that. Was it processed in a bacteria-free environment? What temperatures was the peptide exposed to after production? Did it oxidize? Even if all the variables were controlled for, there is no way I am injecting myself with something out of a cosmetics jar without filtering it through a micron filter first. Then let's say I do inject it. Let's just say IV for shits and giggles. Now I have DGGL floating around in my blood. My enzymes are going to rip that thing to bits within minutes. Some will reach my BBB. However, it's not lipophillic, and has no active transport. So it will just knock on the door to my brain, while being ravaged to bits by savage peptidase enzymes. Goodbye DGGL. Hello free glycine, leucine, and aspartic acid. It's nice to have you here, but not really useful.
So yes, the DGGL sequence is a good peptide to investigate for neurogenesis. However, you have to modify the shit out of it to make it actually work in the human body. So you acetylate the N-terminus and add a 3-amino-adamantane-1-carboxylic acid (A Gly) on the C-terminus, and you get P21. The acetylation/amidation, like in our latest Semax, protects the termini from enzymatic degradation. Then the adamantane moiety increases the lipophilicity, and allows it to pass the BBB. You also got the adamantane to the brain, which has it's own benefits. Straight DGGL in powder form is useless.
So in short, innovation is good. However, that innovation must be based in science, and have the ultimate goal of efficacy. Vendors that just want to pump out novel shit, without any regard to whether or not it is safe, or even works, are harming the community as a whole. TLR is on a whole other level, but THT is doing it now too. I may bring out risky and novel things. However, I do a hell of a lot more research and testing before okaying it for sale to customers.