• N&PD Moderators: Skorpio

Tezampanel

I'm interested in Tezampanel for being seemingly the only ionotropic glutamatergic antagonist that is not for NMDA. I wonder if it would feel subjectively like a dissociative anesthetic?
 
The term "antihyperalgesic" is a term that (to me) does not engender much promise in respect to recreational potential, or as an adjunct to, etc.....
 
it was in the development pipeline for a drug company that went belly up in late 2009 the name of which I do not recall. It was a "new type" of anti migraine drug. Calcium channel as someone above mentioned. The synthesis is not terribly difficult most things that are pipelined are not.
Read Stephens, Cole. "AMPA vs NMDA (Not real title) Psychopharmacology. 1996 Aug;126(3):249-59.
 
negrogesic said:
The term "antihyperalgesic" is a term that (to me) does not engender much promise in respect to recreational potential, or as an adjunct to, etc.....

The study in question investigated the effect of tezampanel on hypersenstitivity to pain induced by opioid withdrawal, and the effect was amelioration of such pain. However, why would such activity bode poorly?

ebola
 
Also from what I can remember, potent AMPA antagonists seem to cause a very fast tollerance.
Not sure where exactly I read this but it was while I was doing some research on the CX-series ampakines.

Also piracetam is quite weak as an ampakine drug and it has a multitude of other effects on ion channels and muscarinic receptors, at least so it seems. I wouldnt consider it a 'central' example of an ampakine modulating drug.
Aniracetam, considering a study, is more selective as an ampakine allosteric modulator and binds to a more specific site on the AMPA receptor compared to piracetam (hence it's greater resemblance with the CX drugs).
This is a good study comparing the two:
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2872987/?tool=pmcentrez
 
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