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Salvinorin A and kappa opioid receptors

dicot
12 years ago

I've given casual Salvia divinorum use little regard in the past, but I have to say this new Scripps study confirms that its active ingredient, Salvinorin A, has true medicinal uses and may be useful in fighting opiate addiction. This research is in the latest edition of Nature.

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Opioid receptor subtypes in the human brain work together in a symphony of activity that is still not fully understood. The "mu" opioid receptors mediate feelings of pleasure and pain-relief; they are the prime targets of the body's own endorphin neurotransmitters as well as heroin, morphine, and most other opioid drugs. By contrast, "kappa" opioid receptors are bound by neurotransmitters known as dynorphins, and when activated can depress mood and produce dissociative, psychedelic experiences. The plant Salvia divinorum, which was originally cultivated by Mesoamerican societies for religious ceremonies and is now used widely as a recreational drug, has an active ingredient, Salvinorin A, that binds selectively and with high affinity to kappa opioid receptors.

"We don't know why kappa receptors evolved, but we know that they have been around for a long time in evolutionary terms; even frogs have them," said Bryan Roth, a professor of pharmacology and an opioid receptor expert at the University of North Carolina, whose group teamed with the Stevens lab for the new study.

If their psychedelic and mood-darkening effects could be avoided somehow, kappa opioid receptor activators, or "agonists," could be very useful medically. In animal studies, they act as mild and non-addicting pain-relievers, weaken the addictive effects of other drugs, and reduce irritable bowel signs. "Antagonist" compounds that block kappa opioid receptor activity also show promise as treatments for depression, anxiety, and other psychiatric conditions. Even the psychedelic effects associated with kappa receptor activation could be useful in providing insights into perception and consciousness. "This is a receptor that is important for how we see reality," said Roth.

Here is a link that might be useful: Salvinorin A

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