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Novel reverse H3 inverse agonist/antagonists

h3 inverse agonist pitolsant wakefulness

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#1 MrSliz1724

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Posted 26 February 2014 - 02:12 PM


So for some time I have been trying to find some natural sources of reverse H3 antagonists and have a few of them in mind. Only issue there is either zero human studies or any pharmacokinetic research that I can find. Only one that I know of that has some sort of information is Connessine where the half life is extremely long and would lead to a build up from day-to-day use. When the target is wakefulness then something that stays in your system for 24+ hours is not a good idea IMO.

Additionaly Connessine also produces peripheral side effects which may be difficult for some to manage. After that there is Carcinine which is "molecular relative" if I may to carnosine. Carcinine does seem to be a decently potent H3 antagonist and you can see a general outline of its pharmacologic data in mice in the link below.

http://www.ncbi.nlm....les/PMC1575432/

After that I know of verongamine and apsylamine-1. I haven't done much research into these two as of yet.

What I do know that all of these have in common is that they all have a tertiary amine group that seems to be necessary for the function that is desired in regards to H3 inverse agonist/antagonist activity.

DISCUSS!!!
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#2 MrSliz1724

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Posted 28 February 2014 - 06:21 PM

bump

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Also tagged with one or more of these keywords: h3 inverse agonist, pitolsant, wakefulness

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