Scientists take big step toward finding non-addictive painkiller

  1. DroppedYourPocket
    D3B21C42-AA69-4314-ADAD-AF59D61E7A80.jpeg Coastal Plains Toad (Incilius nebulifer)CREDIT: DYP

    With the support of the National Institute on Drug Abuse, scientists at Wake Forest School of Medicine have been working to find a safe, non-addictive pain killer to help fight the current opioid crisis in this country.

    And they may have done just that, though in an animal model.

    Known as AT-121, the new chemical compound has dual therapeutic action that suppressed the addictive effects of opioids and produced morphine-like analgesic effects in non-human primates.

    "In our study, we found AT-121 to be safe and non-addictive, as well as an effective pain medication," said Mei-Chuan Ko, Ph.D., professor of physiology and pharmacology at the School of Medicine, part of Wake Forest Baptist Medical Center.

    "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."

    The findings are published in the Aug. 29 issue of the journal Science Translational Medicine.

    The main objective of this study was to design and test a chemical compound that would work on both the mu opioid receptor, the main component in the most effective prescription pain killers, and the nociceptin receptor, which opposes or blocks the abuse and dependence-related side effects of mu-targeted opioids. Current opioid pain drugs, such as fentanyl and oxycodone, work only on the mu opioid receptor, which also produces unwanted side effects -- respiratory depression, abuse potential, increased sensitivity to pain and physical dependence.

    "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 said.

    In the study, the researchers observed that AT-121 showed the same level of pain relief as an opioid, but at a 100-times lower dose than morphine. At that dose, it also blunted the addictive effects of oxycodone, a commonly abused prescription drug.

    The bifunctional profile of AT-121 not only gave effective pain relief without abuse potential, it also lacked other opioid side-effects that patients typically struggle with, such as itch, respiratory depression, tolerance and dependence.

    "Our data shows that targeting the nociceptin opioid receptor not only dialed down the addictive and other side-effects, it provided effective pain relief," Ko said. "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."

    Next steps include conducting additional preclinical studies to collect more safety data, and then if all goes well, applying to the Food and Drug Administration for approval to begin clinical trials in people, Ko said.

    AT-121 was developed by Nurulain T. Zaveri, Ph.D., a member of the research team at Astraea Therapeutics.

    The work was supported by grants from the National Institutes of Health, National Institute on Drug Abuse R01DA032568, R01DA027811, R44DA042465, R21DA040104, and R21DA044775, and the U.S. Department of Defense W81XWH-13-2-0045.

    Original Source

    Written by: Wake Forest Baptist Medical Center, Aug 29, 2018, Scientists take big step toward finding non-addictive painkiller, Science Daily

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  1. TheBigBadWolf
    Well now. That's the philosopher's stone they all were looking for.

    I remember some time ago the med that was said to not form a morphine-like /dependency went by the name of "heroin", some decades later they sold us the absolute non-addictive oxycodone and its time release formula oxycontin.

    And still they are fumbling on the mu receptor. Sadly non-human primates are exactly this - non-human.
    I hope I am wrong, some good nonaddictive painkiller is what the world needs, a compound that has no effects that are able to destroy a human's life.

  2. trdofbeingtrd
    I’m no scientist, but, it just sounds like they made an opioid that you can just not die as easy......

    Really need to stay away from those “non/less addictive” line/s.

    Dr.s giving out tramadol like fucking crazy claiming it’s not addictive and don’t have opiate like effects.....fucking LIARS!!!!!
      DeepGreenSea likes this.
  3. ghoul
    Sounds too good to be true in my opinion. If a drug provides a relieving effect, chances are it will be psychologically addictive at the very least. It would be an amazing breakthrough if this holds up under further testing, but something tells me this is still an abusable drug. I don't see how targeting the nociceptin receptor would make the drug's effect on the traditional opioid receptors any less pleasurable or otherwise ripe for abuse. Maybe if the drug didn't target the opioid receptors at all, and it was selective towards the nociceptin receptors only it'd seem more promising, but at this point I'm highly skeptical.
  4. DeepGreenSea
    Exactly Tired! The Withdrawl from Tramadol can be(and often is) more medically dangerous than opiates! Worse-most people have no idea that it has the impact on the brain that it does so when they try to stop taking it and then go into WD they have NO IDEA what they will be experiencing. That misery can be compounded (and made even more dangerous) if their prescribing physician brushes off their symptoms as psychosomatic!

    Its an expense of spirit in a waste of shame
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