P-glycoprotein blood brain barrier question

[Cotcha Yankinov]

I'm confused, does P-glycoprotein carry compounds into the CNS as well as out of it, and if it does both, will P glycoprotein inhibiton (ignoring bioavailability) increase or decrease CNS drug concentrations, or would that depend on some factors concerning the blood nerve barrier?

 

[serotonin2A]

It works by moving compounds out of the brain.

 

[Cotcha Yankinov]

Are P-glycoprotein inhibitors used to increase CNS drug concentrations in practice?

 

[serotonin2A]

Not yet but they probably will be used for that purpose in the future. The inhibitors are actually probably much more useful for other purposes. Pgp also transports drugs out of cancer cells, so it might be useful to combine chemotherapeutic agents with Pgp inhibitors.

 

[Cotcha Yankinov]

It seems Pgp is up regulated in neuropathic pain conditions, which might present a challenge for getting anti-inflammatory drugs into the nervous tissues. Do you know of any good over the counter Pgp inhibitors besides Curcumin?