Author Topic: AT-121: an Experimental Opiod 100x stronger than Morphine and NON-ADDICTIVE  (Read 417 times)

Offline Chip (OP)

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source: https://www.sciencealert.com/experimental-non-addictive-painkiller-solution-opioid-crisis-at-121/amp

A Fucking Miracle ?

BY PETER DOCKRILL
AUGUST 30, 2018

It's no secret America is hurting right now. Life expectancy is in decline, fuelled by a deadly national addiction to painkillers that knows almost no bounds.
But a new experimental chemical compound developed by scientists in the US and so far tested on animals could be the ray of light so many desperately need.

Called AT–121, it's more powerful than morphine in delivering pain relief, it doesn't produce dangerous side effects, and – importantly – it's not addictive.
"In our study, we found AT–121 to be safe and non-addictive, as well as an effective pain medication," explains pharmacologist Mei-Chuan Ko from Wake Forest Baptist Medical Centre.

"In addition, this compound also was effective at blocking abuse potential of prescription opioids, much like buprenorphine does for heroin, so we hope it could be used to treat pain and opioid abuse."
Ko and fellow researchers developed AT–121 in their attempts to find a molecule that could act upon two key receptors in the brain: the mu opioid receptor, which conventional opioids and prescription painkillers target, and the nociceptin receptor, which regulates various brain activities, including feelings of addiction and chemical dependence.
In theory, an agonist that could successfully bind to both these receptors could promote sensations of pain relief without inviting the severe addiction that opioids often arouse.

"We developed AT–121 that combines both activities in an appropriate balance in one single molecule, which we think is a better pharmaceutical strategy than to have two drugs to be used in combination," Ko says.

Early results are positive. In tests with rhesus monkeys, AT–121 appeared to deliver pain relief equivalent to morphine, but at a dosage 100 times lower.
It also did so non-addictively, but more than that, when the compound was given to animals who had developed a dependence on the opioid oxycodone, it actually reduced their level of addiction, suggesting AT–121 might be able to help patients wean themselves off other drugs at the same time as treating their pain.

That, of course, is assuming the chemical works on humans the same way it does on monkeys. There's no guarantee of that, but the researchers are confident future work could show just that.

"The fact that this data was in nonhuman primates, a closely related species to humans, was also significant because it showed that compounds, such as AT–121, have the translational potential to be a viable opioid alternative or replacement for prescription opioids," Ko explains.

If that's the case, the drug could offer another benefit too. AT–121 didn't trigger respiratory depression (breathing difficulties) or cardiovascular issues even when given at high dosage, meaning we could be looking at an effective, non-addictive painkiller that's impossible to overdose on.

We'll need to see what results further studies produce, but with the ongoing tragedy of the opioid epidemic as a grave backdrop, it's hard to not get a little excited about the promise and potential here.
"I think this is pretty interesting," pharmacologist Bryan Roth from the University of North Carolina at Chapel Hill, who wasn't involved with the study, told Live Science.

"This is one of several of these types of studies that have been published recently that suggest there may be hope for creating safe medications for treating pain. It gives me hope for the field that we may be turning a corner."

The findings are reported in Science Translational Medicine .


Post Merged: September 21, 2018, 04:39:53 PM
Yes, it targets the mu opioid receptor !

No, it does not cause respiratory depression.

Yes, it may help addicts detox painlessly.

No, it's not tested on humans.

Yes, there is hope !
« Last Edit: September 22, 2018, 02:52:56 AM by Chip »
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Re: AT-121: an Experimental Opiod 100x stronger than Morphine and NON-ADDICTIVE
« Reply #1 on: September 21, 2018, 10:48:32 PM »
wow, hopefully they'll fastrack this

Offline bignasty

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Re: AT-121: an Experimental Opiod 100x stronger than Morphine and NON-ADDICTIVE
« Reply #2 on: September 22, 2018, 12:20:01 AM »
I'm not allergic to any medications as far as I know but I have a feeling that I'm gonna be allergic to this one. Non-addictive usually means no recreational value. I wish they would've said whether it's non addictive physically or non addictive psychologically too or what. If it's psychologically non-addictive, that means it's no fun. Hell, folks get addicted to meth/coke/stims/weed/psychedelics/nitrous even though they're not physically addictive so this one might not have any recreational value. It'd be awesome to keep some around for detoxes or lowering your tolerance or in your emergency kit though.

Also, I don't see why they don't study nubain/nalbuphine more. It's not physically addictive and works great for pain. When I had no tolerance and got pancreatitis which is severely painful, a shot of nubain was pure bliss and killed all the pain almost instantly even though they gave me the shot in the ass/hip. I did get psychologically addicted to it though 'cause I could get it online from Mexico for really cheap and I'd use it for pain before I'd work out and eventually lead to just using it for the fun of it. It sucks that I ruined all my good veins doing an opioid that doesn't even have much recreational value but I loved it at the time since I do have legit pain and truly DO need pain meds at least occasionally if not all day everyday.

Offline Chip (OP)

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Re: AT-121: an Experimental Opiod 100x stronger than Morphine and NON-ADDICTIVE
« Reply #3 on: September 22, 2018, 02:51:59 AM »
the drug activates 2 types of opioid receptors (not just the beloved mu guy) ...

i feel ya and yes, non-addictive has always mean't the same to me BUT this drug ALSO targets the NociceptinWiki opioid receptor which blocks the brain's addiction forming response whilst providing additional pain relief (Sep 8 2018 edition of New Scientist).

i wonder about it's bioavailability ?

at least there's some serious hope for many of us here.
« Last Edit: September 22, 2018, 02:56:56 AM by Chip »
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Re: AT-121: an Experimental Opiod 100x stronger than Morphine and NON-ADDICTIVE
« Reply #4 on: September 22, 2018, 03:11:57 AM »
i want to use this every day for the rest of my life

Offline bonedust

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Re: AT-121: an Experimental Opiod 100x stronger than Morphine and NON-ADDICTIVE
« Reply #5 on: September 23, 2018, 04:36:35 PM »
I doubt anyone (except a few people) really wanna help addicts detox painlessly. This also could be an excuse to phase out the fun drugs. No thanks, I'll pass.
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Re: AT-121: an Experimental Opiod 100x stronger than Morphine and NON-ADDICTIVE
« Reply #6 on: September 27, 2018, 12:19:08 AM »
I doubt anyone (except a few people) really wanna help addicts detox painlessly. This also could be an excuse to phase out the fun drugs. No thanks, I'll pass.
They'll eventually phase out all the fun drugs. I hope I don't see it during my lifetime but I have a feeling I will. At least the dealers and cartels and government will always keep the fun drugs flowing. If they were to spray herbicide on the coca and poppy fields once they get rid of the fun RX drugs, I'm going to have to go back to college and get a PHD in chemistry or organic chemistry so I can make my own shit. As long as they still have the low dose codeine pills in some countries, I can at least make some oxycodone and hopefully some oxymorphone and morphine and diamophine, nicomorphine, hydromorphone, etc.. If I could go back to high school, I'd make sure to take chemistry in high school and major in it in college.

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