Tested on monkeys
The new painkiller is 100 times stronger than morphine and does not cause addiction
Anna Kerman, XX2 century
Normally, pain is necessary, it points us to the dangers in the environment. But in many diseases, the pain syndrome becomes an independent problem: the pain lasts for years and simply exhausts the patient.
An international team of scientists has created a molecule capable of suppressing pain 100 times more effectively than morphine, without leading to addiction. The compound has already been tested on monkeys, the results of the work have been published in the journal Science Translational Medicine.
"The new drug, AT-121, has been successfully tested on monkeys. The compound turned out to be an effective and safe remedy for pain relief. In addition, AT-121 can be used as a treatment for opiate addiction, since this drug blocks the effect of drugs," explains Mei–Chuan Ko from Wake Forest University.
Morphine and its derivatives (e.g. heroin) they are so effective because they are similar in affinity to receptors with molecules of endorphins, natural "pleasure hormones" synthesized in the body. Opiates act on the same receptors as endorphins, not only blocking pain, but also causing a feeling of euphoria. However, recently scientists have been able to detect small but significant differences in the mechanisms of action of endorphins and opiates. This discovery explained why endorphins do not cause addiction, which cannot be said about their artificial "substitutes". And, perhaps even more importantly, understanding the differences between endorphins and opiates gave hope for the imminent appearance of a new generation of painkillers that effectively relieve pain, but do not cause addiction.
Research in this area continues – a few years ago, a group of scientists led by Professor Ko discovered that the strength of the effect of opiates on nerve cells depended not only on the number of opioid receptors on the surface of neurons, but also on the concentration of the nociceptin protein. Nociceptin is well known as a compound that prevents opiates from causing a feeling of euphoria, it has been used for quite some time to develop drugs against opiate addiction.
But the authors of the new study approached the problem somewhat differently: to develop a drug that would simultaneously stimulate opioid receptors, as opiates do, and at the same time block the appearance of a sense of pleasure, like nociceptin. So the AT-121 molecule, a modified nociceptin, was born, differing from its predecessor in its ability to effectively suppress pain.
To check whether AT-121 really does not cause addiction, scientists took a group of rhesus monkeys and placed them in special enclosures where animals could choose a drug to their taste - the monkeys had dispensers with cocaine, oxycodone, fentanyl and other substances at their disposal. To get the next dose, it was enough for the macaque to press the lever.
The results of this experiment came as a surprise: it turned out that animals who repeatedly received AT-121 not only did not "bind" to the new compound, but also refused other drugs. In this regard, AT-121 is similar to drugs for substitution therapy, but, unlike them, it does not lead to a new form of addiction.
Now the authors plan to conduct another series of experiments on animals, and then – if the safety of AT-121 is confirmed – proceed to experiments on volunteers.
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