Gleevec (Imatinib) and it's effect on lowering opiod tolerance

[izuni]

I found this article and didn't find that it had been posted here before but I thought it might intrigue some of you.

Imatinib is a Tyrosine kinase receptor inhibitor which inhibits, amongst others the Platelet Derived Growth Factor-Receptor, PDGF-Rβ which affects the NMDAR. (NMDAR antagonists are afaik not clinically used to reduce tolerance to narcotics but the use of ketamine, PCP, DXM and their analogues to prevent and reduce tolerance seems to be frequent e.g. on Bluelight).

Here's an abstract from the article

For centuries, opioid drugs have been the mainstay of chronic pain treatment. However, over time analgesic tolerance
develops, leaving few treatment options. Here we show that platelet-derived growth factor receptor-b (PDGFR-b)-mediated
signaling plays a key role in morphine tolerance. PDGFR-b inhibition selectively eliminates morphine tolerance in rats.
PDGFR-b inhibitors are widely used and well tolerated, suggesting that clinical translation of our findings could reduce
the suffering endured by individuals with intractable pain.

Full text:http://www.nature.com/nm/journal/v18/n3/pdf/nm.2633.pdf

The opioid tolerance reversing/lowering effects of Gleevec has not been observed in human use owing to the inability of Imatinib to cross the BBB and as such it cannot affect opioid receptors in the CNS, this research relies on a different formulation of Imatinib which allows for BBB penetration.
It's a pity Gleevec costs tens of thousands of $, at least up until late 2015, otherwise it seems like a comparatively safe chematherapeutic agent. Perhaps it can be feasible for clinical use of lowering opioid tolerance in patients who rely on chronic opioid therapy.

I have merely skimmed the article as I am in a bit of a hurry but I will read it thorougly later and join in if theres any discussion.

Kindest regards

 

[SeenSoFar]

I recently stumbled onto this as well in my reading. Seems that our old friend cyclodextrin is what they're trying to use to increase BBB permeability. I'm really interested in these novel methods for halting and counteracting opioid tolerance, as well as the new research that's coming out on limiting and preventing dependence from forming. It could bring about the holy grail of opioid use, all the pleasure with none of the consequences. We live in exciting times...