Comment · Tue, July 12, 2016
CERC-501/ KOR or generally antagonists of opioidergic system?
Original post in this thread
homosuperiorr · 1 points
Toughts?
What they were answering
question2552 · 1 points
This may be a question you can't answer, but would antagonizing the κ opioid receptor act as an instance of hormesis and do more harm in the long run? I get that the acute effects of CERC-501 in the body would probably be an amazing antidepressant/anxiolytic. But the fun of low dose naltrexone is that it hormetically upregulates the μ opioid receptor by being a μ opioid antagonist. You take it before bed to have shitty dreams, then you wake up and slowly start feeling better/with less pain.
u/MisterYouAreSoDumb
We don't know yet. It has gone through phase 2 human trials, though, and has not shown any serious side effects. The kappa opioid receptor is unique in that agonizing it lowers pain, but also increases dysphoria, depression, and addiction. The μ opioid receptor works more like other ionotropic receptors. Also, activating the kappa opioid receptor antagonizes the effects of the μ opioid receptor. It's a balancing act.