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Nicotinic Receptors and Pain

Dope_User

Bluelighter
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Jun 20, 2004
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I'm just looking for any comments regarding actions on nicotinic receptors and pain. What do you think about ABT-594? Could a "pain management" drug act on nicotinic receptors yet not be addictive (considering it close relationship to the very addicting nicotine)? Here's some information on the subject...

Selected Information From: http://www.cumc.columbia.edu/news/in-vivo/Vol2_Iss08_apr28_03/postoperative-pain.html:

"From her previous research, Dr. Flood knew that nicotinic receptors in the central nervous system are blocked by the gas molecules at the same low concentration that increases pain. To see if the blockage causes an increase in pain sensitivity, Dr. Flood gave mice nicotine, a substance that activates the nicotinic receptors. Pain sensitivity was measured by applying heat to the mouse's paw and recording the time it took the mouse to lift its paw. Nicotine prevented isoflurane from increasing pain sensitivity, suggesting the involvement of the nicotinic receptors in the pain-enhancing action of volatile anesthetics. The results were published last July in Anesthesiology...that descend from the brain into the spinal cord can reduce the amount of pain signals that ultimately reach the brain. Nicotinic receptors are at the end of these descending adrenergic and serotonergic neurons and, when activated, enhance the release of neurotransmitters and reduce pain...whether nicotine nasal spray given to women after surgery can reduce their pain and narcotic requirements. Results are expected in about one year, but Dr. Flood has already filed a patent for the use of nicotinic agonists on postoperative pain."

Selected Information From: http://www.abdn.ac.uk/chemistry/abt/

Addictive tests on membranes containing acetylcholine receptors
ABT-594 appeared to be non-addictive. There are hopes that this is because it doesn’t act through the opioid receptors (through which morphine interacts), but nicotine is addictive.
 
This wont be a 'fun' molecule to play around with. It actually causes decreased locomotor stimulation. Sure it is a potent inhibitor of monoamines in vitro. I think the habit side of the drug is going to take a few months to develop itself. So you dont just take the drug for the first time and think "yeah this is it!"
 
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Picking up a "habit" or addiction to practically every drug will take awhile. What evidence do you have to back up the statements that it "decreased locomotor stimulation...is a potent inhibitor of monoamines in vitro...and that the habit will take a few months to develop?"
 
The actual link for this is:

Current Topics in Medicinal Chemistry 2004, 4, 369-384

Nicotinic Acetylcholine Receptor Agonists: A Potential New Class of Analgesics

Michael W. Decker, Lynne E. Rueter, and R. Scott Bitner

This is quite a landmark publication containing 146 refs. and has an asking price of $45.

FYI You can get this online here:
http://www.ingentaconnect.com/conte...004/00000003;jsessionid=4t6o4hmkeuce.victoria

Most of the cutting edge material was posted this issue. You can hack into it all with athens.
 
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