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Re: Are Neuroleptics brain specific anticholinergics? » Lamdage22

Posted by SLS on February 4, 2023, at 17:35:21

In reply to Re: Are Neuroleptics brain specific anticholinergics?, posted by Lamdage22 on February 4, 2023, at 15:55:42

> Damn it. I meant to say antihistaminergics in the subject line.


Yeah, but we all knew what you meant...


:-)


Usually, things in the blood stream are blocked from entering the brain by what's called the "blood brain barrier" - BBB. The barrier is actually a closely-packed layer of epithelial cells (flat and skin-like) coating both the inside and the outside of brain blood vessels. Unlike the peripheral circulatory vessels, the epithelial cells in the brain are packed tightly together. When cell membrane meet, they form "tight junctions". This barrier will allow some substances to pass through it and keep other substances out. Many substances cross the barrier passively by osmosis. Others are blocked from crossing passively and must be shepherded across the barrier by active transport. This takes energy, and the power generators in the cells are known as miitochondria. Lots of them cluster around the cell membranes to power the transporters.

In order to "feel" the sedation that Seroquel (quetiapine) or Remeron (mirtazepine) produce, the drug molecules must first cross the BBB, after which they bind to histamine receptors and sedate you. Most medical uses for anticholinergic drugs are peripheral. You don't want them to get into your brain. They tend to make you "stupid" and impairs memory. It would be great if they could invent a drug that would block acetylcholine receptors throughout the body without affecting the brain. There are such drugs. The drug designers created anticholinergic drugs that treat bodily functions while sparing the brain from being exposed.

Somewhere in there, I hope you find the answer to your question - especially since I didn't understand what it is you wanted to know.


- Scott


Some see things as they are and ask why.
I dream of things that never were and ask why not.

The only thing necessary for the triumph of evil is that good men do nothing.

 

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