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GABA for the brain damage caused by psychotropics (Pfizer patent)

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Mort Zuckerman

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Mar 24, 2010, 3:32:59 PM3/24/10
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Subject: GABA for the brain damage caused by psychotropics (Pfizer
patent)

Date: Mar 24, 2010 3:31 PM

http://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO1&Sect2=HITOFF&d=PALL&p=1&u=%2Fnetahtml%2FPTO%2Fsrchnum.htm&r=1&f=G&l=50&s1=6,342,529.PN.&OS=PN/6,342,529&RS=PN/6,342,529

TECHNICAL FIELD

The present invention relates to novel compounds that are analogs of
glutamic acid and gamma-aminobutyric acid (GABA). More specifically,
the analogs are useful as antiseizure therapy for central nervous
system disorders such as epilepsy, Huntington's chorea, cerebral
ischemia, Parkinson's disease, ***tardive dyskinesia,*** and
spasticity. It is also possible that the present invention could be
used as an antidepressant, anxiolytic, and antipsychotic activity.

http://www.actionlyme.org/BRAINDAMAGE.htm

BACKGROUND OF THE INVENTION

Gamma aminobutyric acid (GABA) and glutamic acid are two major
neurotransmitters involved in the regulation of brain neuronal
activity. GABA is the major inhibitory neurotransmitter and L-glutamic
acid is an excitatory transmitter (Roberts E, et al, GABA in Nervous
System Function, Raven Press: New York, 1976; McGeer E G, et al,
Glutamine, Glutamate, and GABA in the Central Nervous System; Hertz L,
Kvamme E, McGeer E G, Schousbal A, eds., Liss: New York, 1983;3-17).
An imbalance in the concentration of these neurotransmitters can lead
to convulsive states. Accordingly, it is clinically relevant to be
able to control convulsive states by controlling the metabolism of
this neurotransmitter. When the concentration of GABA diminishes below
a threshold level in the brain, convulsions result (Karlsson A, et al,
Biochem. Pharmacol 1974;23:3053-3061). When the GABA levels rise in
the brain during convulsions, seizures terminate (Hayashi T J,
Physiol. (London) 1959;145:570-578). The term seizure as used herein
means excessive unsynchronized neuronal activity that disrupts normal
neuronal function. In several seizure disorders there is concomitant
with reduced brain GABA levels a diminished level of L-glutamic acid
decarboxylase (GAD) activity also observed (McGeer P O, et al, In:
GABA in Nervous System Function; Roberts E, Chase T N, Tower D B,
eds., Raven Press: New York 1976:487-495; Butterworth J, et al,
Neurochem. 1983;41:440-447; Spokes E G, Adv. Exp. Med. Biol.
1978;123:461-473; Wu J Y, et al, Neurochem. Res. 1979;4:575-586; and
Iversen L L, et al, Psychiat. Res. 1974;11:255-256). Often, the
concentrations of GAD and GABA vary in parallel because decreased GAD
concentration results in lower GABA production.
=======================

I am not fooling around
as you can see. This is one
of many patents for the same
application - how to undo the
brain damage from psychotropics.


Kathleen M. Dickson
http://www.actionlyme.org

"[Real] scientists are *fiercely* independent. That's the good
news."-- NIH's Top Fool, Anthony Fauci

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