Comment · Mon, May 9, 2016 · Ceretropic & Nootropics Depot
Why is there such little information on N-Acetyl Semax Amidate or N-Acetyl Selank?
What they were answering
Noobsessed · 1 points
Alright, my comment's forms were pretty idiotic and I apologize for that. Still, even when taking into account the posibility of increasing some parameters like membrane permeability and shelf-life, what are your reasons to modify a peptide that was already developed by modern scientists? What do you think would be the reason for them to not make this improvement? What is it known about semax's pharmacology to determine that it won't change significantly with respect to the original?
Thanks for being so polite to my rude comment, I'm feeling some unusual irritability recently.
u/MisterYouAreSoDumb · Ceretropic & Nootropics Depot
Because everything can be improved. That's the whole point of our community. If nothing could be improved, then why are we all here trying?
Regular Semax is a very polar peptide. That is why it is so water soluble. However, polar things do not pass the blood brain barrier very well. So reducing the overall charge of a peptide is going to make it more able to pass lipid membranes like the blood brain barrier. Also, an open N and C terminus is very susceptible to enzymatic degradation. Your plasma peptidase enzyme is going to rip apart Semax as soon as it hits the blood stream. Its half life in the blood is 5 minutes! N-terminal acetylation and C-terminal amidation protects those termini, leading to longer plasma times. The two biggest factors in a peptide being able to reach the brain are peak plasma levels/AUC, and how polar it is. Adding the acetyl and amide helps both. Not only that, but most of your endogenous peptides are acetylated and amidated.
They thought up Semax by taking ACTH (adrenocorticotropic hormone) 4-7, and adding a tripeptide based on endogenous prolyglycine. Well natural ACTH has an N-acetyl and C-amide. Therefore, I thought it was silly to have Semax without those groupings, as regular Semax would be less like the endogenous peptides it is based off of than our N-Acetyl Semax Amidate. If you really think about it, it's regular Semax that is weird. Why leave off the N-acetyl and C-amide groups, when the individual components have them naturally in your body? Also, Noopept is the one that inspired them to think of adding the proline-glycine-proline group to ACTH 4-7. What does Noopept have on its N-terminus? It's a phenylacetyl, which is an acetylated phenyl group. So Noopept has a modified N-acetyl group to try and improve its pharmacokinetics. I thought it only logical to add one to Semax to do the same thing. The C-amide was just an extension of that logic.