Body's Natural Pain Killers Enhanced: Study in Cells, Mice Finds Compound Works; Few Side Effects
upstart writes in with an IRC submission for TheMightyBuzzard:
Body's Natural Pain Killers Can Be Enhanced:
Work by John Traynor, Ph.D., and Andrew Alt, Ph.D., and their team at the University of Michigan Edward F. Domino Research Center, funded by the National Institute on Drug Abuse, seeks to side-step [opiod's] problems by harnessing the body's own ability to block pain.
[...] "Normally, when you are in pain, you are releasing endogenous opioids, but they're just not strong enough or long lasting enough," says Traynor. The team had long hypothesized that substances called positive allosteric modulators could be used to enhance the body's own endorphins and enkephalins. In a new paper published in PNAS, they demonstrate that a positive allosteric modulator known as BMS-986122 can boost enkephalins' ability to activate the mu-opioid receptor.
[...] What's more, unlike opioid drugs, positive allosteric modulators only work in the presence of endorphins or enkephalins, meaning they would only kick in when needed for pain relief. They do not bind to the receptor in the way that opioids do instead binding in a different location that enhances its ability to respond to the body's pain-relieving compounds.
"When you need enkephalins, you release them in a pulsatile fashion in specific regions of the body, then they are metabolized quickly," explains Traynor. "In contrast, a drug like morphine floods the body and brain and sticks around for several hours."
Journal Reference:
Ram Kandasamy, Todd M. Hillhouse, Kathryn E. Livingston, et al. Positive allosteric modulation of the mu-opioid receptor produces analgesia with reduced side effects [$], Proceedings of the National Academy of Sciences (DOI: 10.1073/pnas.2000017118)
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