Anyone off of full agonists ever try to dose a naloxone *habit*?

[borohydride]

AKA Nociceptin

AKA ORL1 receptor.

ORL1 agonists look promising for the treatment of neuropathic pain and also enhance mu-agonists and the rewarding nature of cocaine (the last point sort of inferring the link between the first 2).

Anyone care to perform an mm2-minimized overlay of:

http://en.wikipedia.org/wiki/MCOPPB

and the (S) isomer of compound XIX in this paper:

http://www.scribd.com/doc/78122995/B...ides-Helvetica


Note that the piperidine nitrogen of the former overlays the amide nitrogen of the latter. The latter, BTW, is 3.5x the potency of etonitazene (which is x60 in humans, not the x1500 in mice that people think applies).

I honestly don't think anybody ever looked at the ORL1 affinity in older high-potency agonists. Nothing to patent, I guess.

[Nagelfar]

Very interesting boro. Have any studies been conducted looking at dopaminergic drugs such as cocaine and their relative potency relationship between each other and their ORL1 receptor affinity?

[borohydride]

I think there has only been 1 or 2 studies in which ORL1 ligands were tested to see how they altered operant-models of self-administration (you know, those lovely ones where the rat gets food OR drugs or has to suffer pain to get drug - nice).

Buprenorphine is an ORL1 ligand and I know newer medical texts are recommending it as the opioid-of-choice for some types of neuropathic pain (I forget exactly what and cannot be bothered to hobble to the university library to find...

[QuittingTomorrow]

We all can dream. This is 2013 and research/development/technology is absolutely off the wall. Neil and Buzz rode the Saturn 5 to The Sea of Tranquility in 1969. Is it too much to ask for an opiate than creates no tolerance or WD upon cessation in 2013. I believe it to be entirely possible. Maybe there is no money in it for GlaxoSK?? They like selling the shit that hooks you to it like a shakle. Any drug dealer worth their salt want repeat business. Glaxo/Phizer/Purdue are no different. The cash is always in the treatment, never in the cure. So for today and the near future there will be (favorite quote coming) NO FREE LUNCH!!!!!

[HandMeSomeOpiates]

I dream about this.... an opiate that has no W/D symptoms, or tolerance. Only in a perfect world. Far from the world we live in unfortunately. We can all dream though right?

[DriveFast]

I dream about this.... an opiate that has no W/D symptoms, or tolerance. Only in a perfect world. Far from the world we live in unfortunately. We can all dream though right?

What a lovely thing that would be.
Good to see you around man! Haven't seen you in a while!