SPEED 2: CRUISE CONTROL

Fun with trace amines and enzyme inhibition

I went to whole foods today and asked if they sold phenethylamine or PEA, they led me to their phenylalanine.

"No not phenylalanine - Phen-Ethyl-Amine"

"What's it do?"

"It's a stimulant"

"Oh no stimulant is not a Whole Foods word, cummon man, stimulant is not a Whole Foods word!"

PEA is a trace amine, putative neurotransmitter, and the chemical backbone of most dopaminergic stimulants. Additionally it's reported to be more addictive than amphetamine (of which PEA is the parent compound). It's unclear to me if this is because it's a qualitatively superior stimulant (likely) or because the shortened duration makes it fit the classic criteria for an addictive drug ((fast onset/short duration/frequent administration required) also likely) the reason that PEA has not gained widespread popularity is that it's almost immediately deaminated 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 megadoses in excess of a gram. With MAO-B inhibition the dose of PEA is comparable to amphetamine i.e., 25mg is reported to be very strong.

It seems to be a small minority of people that can play with the selegiline+PEA combo without getting miserably addicted, perhaps even a minuscule minority. In many ways it's the holy grail of stimulants: (arguably) safe, dirt cheep, and completely legal. Yet it's not something people can use responsibly. 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 t_1/2 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, I'll leave that to others. the second is to introduce a time release mechanism into the molecule itself á 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 (I'm 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!

SPEED

I cant help but wonder about the nature of these two unnamed unstudied unsynthesized and generally unknown (tentative) psychostimulants - and by "wonder about the nature" i mean to say "obsess over the possibility" that they will be the most earth shatteringly powerful stimulants known to man which will usher in a new and sleepless era of hyperproductivity and total self-realization.

the molecule on the left is an analog of desoxypipradrol featuring the notorious 3,4-dicholoro substitution which sextuples the potency of methylphenidate, when added to the already perfect desoxypipradrol it could produce a stimulant fully active in the tens of micrograms.

the molecule on the right is the alpha-propyl homolog of buphedrone, elongating the alpha substituent in cathinones causes an increase in potency (the opposite effect is seen amphetamines) so one could imagine this chemical having a dosage in the general league of MDPV (whose subjective effects are toxic and miserable) but with no concern over a pro-oxidant dihydroxy conjugation ready metabolite (is that a legit concern ive never been sure?) i think its name should be penthedrone which has a nice ring to it - and im done.

UPDATE

OK, this blog does not really exist. This time last year I felt as if I should blog but my blog spirit is weak. I may try to change that though.

I'm speaking in a lineup with Laurie Anderson and David Wilson on Halloween at the Cantor Film Center, I will be talking about TTX, DiPT and other pharmacological oddities.

On November 4th I'm talking in a lineup with Alex Grey and Daniel Pinchbeck at Webster Hall: the topic will be ayahuasca.

Three new VBS episodes are being edited, and the new best of Vice book is out and filled with incredible articles including a revised and corrected version of The Magic Jews as well as A Giant Chinese Fingertrap Made Of rainbows Tried to Suck Me Into The Sky

Love,

hamitlon

FRIGHTENINGLY LARGE DRUG COLLECTION DESTROYED (NOT MINE (SERIOUSLY))

I'm not sure if these three pictures are real or if it's a sadistic prank made to freak-out drug addicts. The 4-methylaminorex and crystalline PCP are especially impressive as are the several thousand hits of LSD. At the very least it would appear he mixed up his coca leaves with some wrappers in a large foil envelope?

Maybe it's performance art: the spectacle of destroying a drug collection.

2011 Update: I have spoken with the man who once possessed this collection and it was indeed real and he did actually destroy it (at his girlfriend's behest).

UBULAWU NOMATHOTHOLO

Brominated Cathine Witchdoctors! 

May the Ancestors 

Be with us

May the Ancestors

Bless us Camagu!