From painkiller to brainkiller: Parkinson-inducing opiate analoguea

[W4RGASM]

In Maryland, 1976, a 23 year old chemistry graduate named Barry Kidston was studying a 1947 paper by Albert Zeiring, and struck upon the idea of reversing the ester of the skeleton of the medical opiate painkiller mepiridine (Demerol), producing a synthetic opiate about 70% the strength of morphine. Unfortunately he didn't realise that at temperatures above about -30*C the tertiary alcohol produced at an intermediate step is dehydrated under the acidic conditions of the reaction. This was a bad thing, as he wound up producing as a major product 1-methyl 4-phenyl 1,2,3,6-tetrahydropyridine, aka MPTP, which although also giving the desired opiate high, is the prodrug for MPP+. ANY dose (even below the threshold for the high) for MPP+ causes irreversible ripping up of the neurons in the substantia nigra. What does this cause? Anyone? Bueller? Bueller?

PARKINSONS.

Massive, irreversible parkinson's disease.

MPTP can be produced all on it's own by reacting formaldehyde, methylamine and alpha-methylstyrene.

[Man Down Under]

http://www.roguesci.org/theforum/showthread.php?t=1567&highlight=MPTP
or
http://www.roguesci.org/theforum/showthread.php?t=1580&highlight=MPTP

[hatal]

Now thats an interesting effect. I always wondered how they produce lab animals with parkinson for medical testing (before human tests)?

A couple of practical uses almost instantly came into my mind. "This is your brain on drugs (forever)".

[ciguy007]

It's not all bad - researchers were able to track down people who had contact with MPTP in labs (legitimate settings). They found a handful of people who were in nursing homes, "frozen" by parkinson's. Most of the victims had diagnoses like "catatonia." Administration of anti-parkinsonian drugs resulted in a few "miracles" but most remained very resistant to treatment. Those who responded described being locked in their bodies with sensoria and higher faculties intact. Maybe the worse prison you can imagine

[xx932]

I read "The Case of the Frozen Addicts" by Dr. William Langston probably 3x over summer. Good read, and probably only 5$ used on amazon.

They used multiple freshly killed fetuses' (looked up spelling) brain tissue to restore three of the six addict's motor functions, secretly traveling to a hospital in Sweden (if I remember correctly).

The same was later tried on a Parkinson's patient without success. Seems chopped featus brains don't work for those with Parkinson's.

Book has a few pictures of the patients before and after I believe. Comparing the recovered 'addicts' to the fully rigid ones.