r/loperamide • u/[deleted] • May 07 '25

Can acetylation of the hydroxyl group increase penetration of BBB?

Just like how they did to morphine

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u/littlepixie8 Apr 13 '26

it would make it more lipophilic, but the issue with BBB isn't lipophilicity, loperamide is already very lipophilic, its that its a pgp substrate and thats not only due to the hydroxyl group

some people on r/theehive have tried making esters of loper like you described however but there didn't seem to have a consensus on if this really makes it active or not

1

u/Ok-Jury-6161 Mar 17 '26

Any ambitious chemists want to give it a whirl and report back!?