http://www.molecularbrain.com/content/2/1/4

http://www.addexpharma.com/allosteric-modulation

Addex has a clinical trial:
http://www.addexpharma.com/pipeline/

Now i'm in over my head but this delivery and the rationale for development seem solid. Polyamines is the new potential player but there is not much out there....at least for those who are not librarians. i was reading old articles about polyamines and ach and could not figure out if it was good or bad to block the receptor.

I have a question for anyone who might know the answer:

is blocking a receptor, like the acetylcholine receptor nAchR, increasing or decreasing acetlycholine?
Does the block prohibit the breakdown by acetylcholinesterase or does it enhance it?

thanks!

Blocking a receptor inhibits it or stops the transmission of a transporting neurotransmitter at the vesicle so no action signal takes place. This is done with an antagonist drug or naturally when your neurotransmitter are committing mass suicide like our dopamine neurons.

An agonist, like Mirapex or Requip, stimulates receptors so to ensure transmission takes place. Dopa antagonists block; they are used to treat schizophrenia and the old school drugs left the poor folks with symptoms of PD.

All depends on purpose...if you want to inhibit one then it may be a good thing to block. The anticholinesterase prevents reuptake of the neurotransmitter once an action signal takes place. Stopping the reuptake leaves more acetycholine in brain, so that is why it is used in treating AD.

BTW, read that we have over 10 BILLION of the other neurotransmitters and roughly only 1 MILLION dopa neurons; no wonder we're screwed!

Laura