Tuesday, December 22, 2009


fun with neuromodulators and enzymatic inhibition

i went to whole foods today and asked them if they sold phenethylamine or PEA, they led me to their phenylalanine
"no not phenylalanine - Phen-Ethyl-Amine"
"whats it do?"
"its a stimulant"
"oh no stimulant is not a whole food words, cummon man, stimulant is not a whole foods word!"

PEA is a neurotransmitter and the wildly addictive backbone of most classic stimulants, seemingly its even more addictive than amphetamine (of which PEA is the parent compound). its unclear to me if this is because it's a subjectively superior stimulant (likely) or because the shortened duration makes it fit all of the classic criterion of a super addictive substance ((fast onset/short duration/frequent administration required) also likely) the reason that PEA has not gained widespread popularity is that it's almost immediately deamined by MAO rendering it inactive moments after ingestion. there are two popular ways of overcoming the enzymatic tyranny of MAO, the first being direct inhibition via a pharmaceutical MAOI (with the MAO-B selective selegiline being most popular) and the second is to overwhelm MAO by taking mega doses often in excess of a gram. with MAO-B inhibition the dose of PEA is comparable to amphetamine ie >25mg ie very strong.

it seems to be a small minority of people that can play with the selegiline+PEA combo without getting miserably addicted, a miniscule minority. in many ways it is the holy grail of stimulants: (arguably) safe, dirt cheep, and completely legal. yet it's not something people can use responsibly, like crack (although i have used crack very responsibly in the (distant) past). so how can one change this, how can one take advantage of this beautiful molecule which holds so much potential? PEA has a half life of 1 minute ((comp. to smoked crack which has a half life of 56 min) although PEA's t1/2 must be longer with MAO inhibition (more research is required)) thusly it necessitates continuous redosing - the first solution is to create some kind of mechanical time release mechanism, ill leave that to others. the second is to introduce a time release mechanism inherent to the molecule รก la vyvanse.

so here is my solution: lys-PEA aka alpha-desmethyl-lisdexamfetamine. a time release PEA prodrug, when taken with a MAOI it should have a long and healthy duration (im guessing something closer to normal dexamp sans lysine) a low dose, low toxicity, and ultra-low illegality. it will overcome the SAS criterion i outlined above and will probably be an incredibly effective ADHD treatment. the TRUE holy grail of psychostimulants. perhaps it would even be embraced by whole foods, after all lysine and phenethylamine are both TOTALLY natural. i only want to help people.

Equilibrium dissociation constants:

Phenethylamine: NE: 10.9; DA: 39.5; SE > 10000.*
Amphetamine: NE: 7.07; DA: 24.8; SE: 1765.
Methamphetamine: NE: 12.3; DA: 24.5; SE: 736.

*gotta love the way it gives 5HT the cold shoulder, harsh bro!