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Researchers are closing in on a non-addictive opiod-based pain-killer with limited side effects:
[...] [An] international team [has] captured the crystal structure of the kappa opioid receptor—critical for providing pain relief—in action on the surface of human brain cells. The researchers also made another important discovery: a new opioid-based compound that, unlike current opioids, activates only the kappa opioid receptor, raising hopes that they may develop a painkiller that has no risk of addiction and, therefore, none of the devastating consequences and side effects that accompany it.
The findings were published Jan. 4 in the journal Cell.
[...] Currently, most opioids bind to several opioid receptors on the membrane of brain cells, which has its share of drawbacks. They alleviate pain but cause a range of side effects, from nausea to numbness, constipation, anxiety, severe dependency, hallucinations and even death by respiratory depression.
In this study, the computer models revealed the formulations that would create the strongest bond between the ligand and the kappa opioid receptor without affecting other receptors.
Katritch said the latest research may pave the way for a major drug breakthrough.
"We have already found the structure of the inactive kappa opioid receptor highly useful for discovering potential candidates for a new painkiller," Katritch said. "Now with the structure of the active receptor, we have a template for designing new types of pain medications that have no disruptive side effects for patients and would reduce the burden that opioid addiction has placed on society."
Journal reference: Tao Che et al. Structure of the Nanobody-Stabilized Active State of the Kappa Opioid Receptor, Cell (2018). DOI: 10.1016/j.cell.2017.12.011
Having known several people who got addicted to painkillers after receiving prescriptions for oxycodone or similar compounds from their doctors, this can't happen soon enough.
(Score: 4, Informative) by Anonymous Coward on Saturday January 06 2018, @12:56AM (3 children)
While I find it great to hear there is research ongoing into non-addictive opioid painkillers, I don't believe the kappa receptor is a great target. Although it provides analgesia (in the case of oxycodone, its 14-hydroxy group allows it to bond to the kappa receptor, increasing the analgesia) it also comes with a host of negative side effects. In fact, one of the main side effects listed for mu-receptor agonists is actually a typical kappa-receptor agonist trait: Hallucinations. Not only that but the other typical side effect of kappa agonism is dysphoria, the opposite of euphoria (and quite a terrible feeling, speaking from experience). One well known example of a full kappa-opioid agonist would be Salvinorin A, a potent hallucinogen which acts through the kappa opioid receptors. Another example in the morphinan-class is Levorphanol, which has been around 60+ years and which also causes hallucinations. Colour me impressed when they find a painkiller with similar analgesic efficacy to morphine without causing dependence or terrible side effects (like hallucinations, delirium, and dysphoria to name a few).
I would be far happier to see more research going into drugs that can treat addiction. Non-addictive painkillers is nice, but there are always going to be people using opioids illicitly not to mention a whole host of other addictive drugs/activities. Research into drugs that could potentially alleviate an entire range of drug addictions (ala Ibogaine) is being put on the back-burner both legislatively and in terms of raw dollars drug companies are willing to spend. One of the most impressive and promising of these drugs, 18-MC, only had safety studies done on it after it was found to be suitable for treatment of a rare tropical disorder. But its not hard to understand why. Painkillers, even non-addictive ones, make billions of dollars. A one-time treatment for addiction stands to make next to nothing.
(Score: 0) by Anonymous Coward on Saturday January 06 2018, @03:21AM
I kinda liked salvia divinorom extract when it was legal... however it was far to violent and tolerance increased way too fast (about a minute to require a 10fold increased in dosages ) and took to much time to decrease to have the time to become physically addicted and only weirdos get addicted to a trip that is so hallucinogenic that is not psychédélique, salvia is just crazy, my experience range from the tame feet melting with the floor for a few minutes, to crazy reincarnation into others person future or past for what seemed like a long time , passing by blackout where your motor control is not inhibited... fun times ;)
postnihilist to high to remember my password and currently too apathic to care to reset it but not enough to not pseudo sign that post
(Score: 2) by gringer on Saturday January 06 2018, @08:23AM
Maybe this paper will help:
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3306836/ [nih.gov]
Ask me about Sequencing DNA in front of Linus Torvalds [youtube.com]
(Score: 2) by VLM on Saturday January 06 2018, @03:47PM
What's the big picture though?
I hurt my back when I was in a non-weight-lifting phase of life.
The stereotypical lazy ass american way to treat that injury would be to take a theoretically non-addicting pain pill on a regular basis for the rest of my life.
The way I fixed it permanently was weight lifting but actually exercising is very un-american and almost no one is seriously going to do this. Talking about how everyone should exercise is very American but actually exercising is almost forbidden.
I'm just saying, pain pills never fixed nothing, so you're going to have net trillions extra spent on more expensive later fixes. Its cheap to treat a pulled back muscle, but stuff the victim full of pain pills and they'll keep on screwing up until they need disk surgery if not worse. In fact they'll probably pop more and more pills until nerve damage kills their ability to move their legs. Or people with early state cancer, the kinda thing you could fix permanently for $10K, will take bottles of pills until it'll take $1M to save their life, or maybe $500K in terminal costs because they waited too long for treatment. Why slap a band aid on a clean paper cut, when you can just take a pain pill and work thru it while turning it into an abscess full of MRSA flesh eating bacteria costing $500K to treat or at least palliative care until death?
Cheap "safe" pain pills are going to be an incredible revenue generator for the industry as a whole. I would bet most "big ticket" medical care will have cheap non-addictive pain pills as step 2 of the disaster, with step 1 as something minor that could have been treated in days for practically free.
Another novelty; as I get older parts hurt more. Every time you get DOMS from weight lifting imagine some drug company selling a non-addictive pill to pop. There's a lot of functional low level alcoholics that can't get thru life without some oz of alcohol every night uncontrollably, I predict there's gonna be lots of people who can't get thru life without the safe non-addictive pill. In another post I discovered Oxy is (or was) a $3B revenue drug; I checked google and found a claim of $38B for wine. If 1/10th of "mommie sippy cup" meme of female nightly wine drinkers went to a non-addictive pain pill of similar cost, that would replace Oxy at identical revenue.