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Re: +++ MAO-A or B ? Gerovital (procaine) selectivity undopaminergic

Posted by SLS on July 6, 2008, at 5:15:18

In reply to Re: +++ MAO-A or B ? Gerovital (procaine) selectivity, posted by undopaminergic on July 6, 2008, at 2:47:33

It might be worth your looking into if it is important enough to you. I have. Clorgyline is a specific inhibitor of MAO-A. Just enter "clorgyline" and "specific" as keywords when performing a Medline search.

http://www.ncbi.nlm.nih.gov/pubmed/15050826?ordinalpos=10&itool=EntrezSystem2.PEntrez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum

Just because clorgyline and selegiline are propargyl MAOIs doesn't guarantee any similarity in biological activity at all. Look at amineptine and tianeptine, for example. Tianeptine is a sister drug to amineptine, yet does not directly affect dopamine uptake at all.

You might have to relegate yourself to the uncomfortable position of having to trust me on this one. Inhibition of MAO-A is of greater therapeutic effect than is inhibition of MAO-B in treating depression. In fact, inhibiting MAO-B might be counterproductive. Clorgyline is a much more effective antidepressant than selegiline, especially when selegiline dosages are kept low enough to remain selective for MAO-B.

To the degree that one would want to assign the contribution of MAO inhibition to one subtype being more effective in treating depression, MAO-A has consistently shown itself to be more important.


- Scott

> > > Clorgyline, similarly to selgiline, is subtype selective in low doses.
> >
> > I am not aware of a loss of selectivity at any dose. It is not like selegiline in this regard. It is specific (not selective) to MAO-A.
> >
>
> My impression is definitely that clorgyline affects MAO-B - insignificantly at low doses, but very much so at higher doses. I don't have any references at this time, but I know they exist.
>
> To my knowledge, no perfectly specific MAO-inhibitors exist, although selegiline, rasagiline and clorgyline all have sufficient subtype-preference in order to be useful as research tools for clarifying the roles of the different types of MAO. As you suggest:
>
> > Clorgyline is the most reliable probe specific to MAO-A and is the standard of reference by which MAO-A is assayed.

 

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