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Post AVANIR Pharmaceuticals Submits Complete Response to FDA Approvable Letter for ... - E - 04-30-2010, 08:40 PM

AVANIR Pharmaceuticals Submits Complete Response to FDA Approvable Letter for ... - EON: Enhanced Online News (press release)
04-30-2010 09:33 AM



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Default 05-02-2010, 12:29 PM

Quote:
This first-in-class drug candidate is believed to help regulate excitatory neurotransmission in two ways: through pre-synaptic inhibition of glutamate release via sigma-1 receptor agonist activity and through postsynaptic glutamate response modulation via uncompetitive, low-affinity NMDA antagonist activity.
Interesting. I was unaware that DXM also inhibited glutamate release. Glutamate activates the NMDA receptor (along with co-agonist glycine). Glutamate (the principal excitatory neurotransmitter) also serves as the precursor for the synthesis of GABA (the principal inhibitory neurotransmitter). So I'm guessing that DXM may lower concentrations of GABA as well.

Fascinating.

Last edited by viscosity; 05-02-2010 at 01:15 PM. Reason: add more info on glutamate
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Default 05-08-2010, 11:49 AM

Also related:
DXM binds better to the PCP receptor in the absence of L-Glutamate, but DXO binds better in the presence of L-Glutamate. Since DXM inhibits glutamate release, I figure it increases it's own ability to bind to the receptor.
http://molpharm.aspetjournals.org/co...1/160.abstract
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