Resiniferatoxin is 10,000 times hotter than the hottest pepper, and has features that make it promising as a painkiller of last resort.
It takes a while for the heat to explode in your mouth, but soon searing pain is spreading from your tongue to your lips and down your throat. It helps a little when your tongue and lips go numb, but no one can understand anything you say. Your nose is running, you’re sweating profusely, and tears are flowing down your cheeks. Before long, you’re pounding the table, the walls, or your nearest friend. You’re pretty sure that drinking molten lava would be comforting.
But if you can survive the next 20 minutes or so, you’ll be mightily rewarded. By then, the capsaicin in that habanero pepper you just insanely chewed and swallowed will have released a flood of endorphins and dopamine into your brain. They will transmute all that pain into a prolonged rush of pleasure.
This sort of pain/pleasure union of opposites is reflected in folk medicine. Some sorts of homeopathic treatments rely on the maxim that “whatever harms you can also heal you”.
That sort of thinking led to the use of capsaicin, the active ingredient in hot chili peppers, in topical ointments for relief of pain. 1% capsaicin ointments are available over-the-counter. The FDA has approved a higher concentration (8%) capsaicin patch that has proven to be highly effective for some types of neuropathic pain. (The 8% capsaicin patch is to be applied only by a medical professional, under local anesthetic, in a clinic or hospital setting.)
The Scoville scale is a semi-official measurement of gastronomical heat. It gives the following rankings:
2,500 to 5,000 units – the ordinary jalapeno pepper
30,000 to 50,000 units – the cayenne pepper
100,000 to 350,000 units – that habanero that you so unwisely consumed
2,200,000 units – the currently recognized world champion Carolina Reaper pepper
5,300,000 units – police grade pepper spray
16,000,000 units – pure capsaicin
16,000,000,000 units – resiniferatoxin aka RTX
Resiniferatoxin (RTX) is a substance found in resin spurge, a cactus-like plant found in Morocco and Nigeria. (Researchers at Stanford University synthesized resiniferatoxin in 1997). Resiniferatoxin is rated at 16 billion Scoville units. That’s right, RTX is 1,000 times hotter than pure capsaicin. And pure capsaicin is at least 5,000 times hotter than your pathetic habanero. Given this potential power against pain, it’s no wonder that clinical trials of RTX for relief of the pain suffered by both surgical patients and those undergoing last stage cancer are underway.
Nociception is the process whereby the nervous system makes the brain/mind aware of physiological pain.
A TRPV1 (pronounced TRIP-vee one) is one of the links in the nociception network. More specifically, a TRPV1 is an ion receptor channel located at the tip of the sensory neurons which relay pain signals to the brain.
Application of RTX to a TRPV1 stuns the ion receptor and props the receptor channel open. This allows calcium and sodium ions to flood into and overload the TRPV1 channel. This process results in the death, or at least the prolonged desensitization, of the sensory neuron. The nociception network is disrupted, and the brain/mind is no longer aware of the pain.
Unlike opioids, which operate in the brain, RTX operates downstream in the nociception network, so widespread adoption of RTX therapy may lessen the need for opioids.
RTX is extremely powerful. It’s also very selective. It is highly specific to TRPV1. “So you gain selectivity because it only acts on TRPV1, only on a certain class of fibers which only transmit pain,” says Tony Yaksh, a researcher at the University of California San Diego who has studied RTX. “Therefore you can selectively knock out pain without knocking out, say, the ability to feel a light touch or the ability to walk.”
The selectivity of RTX therapy has already earned it the title of “the Molecular Scalpel” for chronic pain relief. RTX knocks out pain receptors without affecting the motor, proprioceptive, and other somatosensory functions that are essential for performing the activities of daily living and maintaining quality of life.
RTX’s destruction of TRPV1 ion receptors isn’t necessarily permanent, but it can be quite a while before the receptors regain their sensitivity. This lesson was learned by researchers who have used RTX to abate pain in dogs. “It is profoundly effective, and the relief lasts much longer than I expected, maybe a median of 5 months before the dog’s owners asked for another injection,” says Michael Iadarola, who is studying RTX at the National Institutes of Health. “The animals went from a constant limp to freely running around. One dog was free of pain for 18 months before its owner noticed that the pain had returned.”
RTX is already being tested on humans. Pilot studies for control of post-surgical pain and the pain which afflicts terminal cancer patients are underway.
It is both interesting and satisfying to see medical science learning to utilize natural substances, like hot peppers and cacti, as effective tools in the fight against multiple kinds of pain. We’ll keep you posted as RTX research progresses. Meanwhile, don’t try RTX at home. Stay with your pitifully weak little habanero.
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Read the full article at: www.wired.com
