Pfizer Scientists Discover Chemical Block For Brain's Response To Stress

Smurfeh

Smurfeh

Bluelighter
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Feb 20, 2006
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162
Interesting PR from Pfizer. Could benzos be obsolete in 10 years?

/ADVANCE/ GROTON, Conn., Sept. 16 /PRNewswire/ -- Scientists at Pfizer
Central Research have designed a molecule that blocks the cascade of events in
the brain that occur in response to stress. Described in this week's
Proceedings of The National Academy of Science, the discovery molecule can be
administered orally, and has been shown in preclinical experiments to have
potential for treating depression and anxiety.
The Pfizer compound arrests the action of a neurotransmitter,
corticotropin releasing factor (CRF), which scientists believe is an important
chemical messenger for transmitting the stress response in the brain.
Excessive levels of this chemical signal may ultimately produce a host of
central nervous system disorders such as depression, anxiety, anorexia and
post-traumatic stress disorder.
"This breakthrough Pfizer compound has implications as a revolutionary
tool for researchers," said George M. Milne, Jr., Ph.D., president of Pfizer
Central Research. "This first non-peptide CRF antagonist should offer an
opportunity, for the first time, to probe the important function of CRF in the
brain. The compound could ultimately emerge as a novel therapy for treating
depression, anxiety and other diseases triggered by increased CRF activity."
Dr. Milne emphasized that while this is a pathfinding scientific discovery, it
will be some years before it is determined whether it will yield a new drug
that is available to patients.
Research has shown that patients with stress-related conditions have a
high concentration of CRF in their cerebrospinal fluid and that CRF levels
decrease following treatment with antidepressant therapies. The challenge for
scientists seeking to block CRF's activity has been to discover a small
molecule that is both effective and can penetrate the blood-brain barrier, a
membrane filtering system that permits entry of some chemicals into the brain
while denying access to others.
Although there have been reports of compounds that successfully block the
CRF receptor--the site on the nerve cell where CRF binds--these compounds have
been large peptide molecules, incapable of crossing the blood-brain barrier.
These drugs could only be administered by direct injection to the brain, and
thus have no practical utility as a medicine.
The report published today describes key attributes of the Pfizer
molecule: Its potency (determined by its ability to bind to CRF receptors and
block CRF's activity at very low concentrations); its unique ability to
penetrate the blood-brain barrier; and its selectivity for the CRF receptor
(decreasing the chances of side effects that can result when numerous
receptors are blocked simultaneously). Finally, preclinical tests, according
to the study, show that the compound has strong anxiolytic and anti-depressant
activity.
Where previous blockers of CRF's effect, could not be developed into
practical medicines because they were peptides, the Pfizer compound is the
first CRF antagonist that is a small non-peptide molecule. "This is the first
non-peptide antagonist of CRF receptors," the authors wrote, "and possesses
clear pharmaceutical advantages over peptide antagonists."
Pfizer Central Research, with major worldwide research facilities in
Groton, Connecticut; Sandwich, England; Amboise, France; Nagoya, Japan; and
Terre Haute, Indiana, is the principal pharmaceuticals, and animal health
research and development arm of Pfizer. Pfizer Inc (NYSE: PFE) is a research-
based health-care company with global operations. In 1995, the company
reported sales of over $10 billion and, in 1996, expects to invest
approximately $1.7 billion in research and development.
Click to expand...
Link!
 
Please only post current articles.

I'll let this slide since it is interesting and it might lead to some good discussion. :)
 
I'm really intrigued and excited about these findings (even though they are a tad old).

Something I would find myself benefiting from immensely hopefully.
Has anyone been able to find any developments in the production of the first test substance?
 
Benzodiazepines won't become obsolete by any standards. They will still have important roles in the emergency treatment of seizures, status epilepticus, mania as well as other things i can't think of right now. Also they will still be used in the treatment of insomnia, as muscle relaxants and in the long term treatment of epilepsy.

Also any drug like this will no doubt be outrageously expensive so i doubt benzos will be replaced for a long time if ever. Who's to say that a drug that blocks crf receptor will even do that well in clinical trials compared to benzodiazepines or even anti-depressants. People don't react to every drug the same.

So no need to go out snatching up as much diazepam and alprazolam scripts as you can just yet :\ .

If anybody who knew jack shit about this kind of stuff could chime in that would be good. Advanced drug discussion might be a good place to discuss this if it already has not been discussed there.
 
wow

I'm amazed I've never heard of this. Very cool. Hope it does well in tests and can help a lot of people.
 
Emotionless flipper baby's please...

Why can't people just grow a soul... like ... the rest of us.... through extensive years of psychedelic exploration....

actually BLOCKS STRESS i am sorry but if the world... is going to end... which it is in 2012... I WANT TO BE STRESSED AND ON THE BALL lol...
 
Wow, the pharmaceutical companies are actually making something *new* rather than recycling acid-blockers and SSRI's.
Oooh! And a whole $1.7 Billion to research and development! The rest goes to advertising, lobbying, and Armani.:p

But yes, it sure would be nice to hear if anyone has heard any updates on this. I wonder what the natural origin of this chemical was.

And yes... the world is ending... as usual. Stressful!8(
 
Ack. Thought that might be a bit vague.
Armani = As in the high-end clothing / Ridiculously expensive luxuries.
 
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