[ExI] Human Testing

[spike]

>... On Behalf Of david
Subject: Re: [ExI] Human Testing

On Sat, 3 Mar 2012 06:39:10 -0800
"spike" <spike66 at att.net> wrote:



>>... If so, bexarotene might be a huge leap forward, for it is low cost (if
taken at reagent grade) and its side effects are probably mild in most
patients.   spike
 
>...It has been a long time since I seriously studied chemistry, but given
that the data sheets claim it to be "moderately soluble in ethanol (with
warming)" the reageant grade would seem to be a candidate for a simple
re-crystallization...Personally, this would be enough for oral medication,
but I would be a lot more wary if you are planning to inject it.  -David
_______________________________________________


Injection is out of the question, and recrystallization is probably
unnecessary for this application.

The signal one gets in studying a number of these kinds of molecules is that
several of them are thought to have beneficial effects on beta amyloids, but
in general they do not readily cross the blood brain barrier.  The challenge
then is to get that to happen.  If a particular molecule crosses one per
thousand in the bloodstream, and we figure out a chemical cousin with
similar beneficial effects that crosses ten per thousand, then it requires a
tenth the dose, meaning a tenth the harmful side effects.  The reason J147
was creating such excitement is that it is lipophilic and a more eager
barrier permeant.

I am struck by the feeling the researchers generally agree that J147, CLR01
and bexarotene probably have beneficial effects on the brain, but the
challenge is in getting the molecule to the site without poisoning the
patient.

spike