Resiniferatoxin – the world’s hottest chemical in painkiller research

Resiniferatoxin is a natural substance found in Euphorbia resinifera. This plant grows in Morocco on the slopes of the Atlas Mountains. The milky sap of this plant contains a high concentration of resiniferatoxin.
Resiniferatoxin has a taste that is 500 to 1000 times hotter than capsaicin, which is found in peppers or chili.
On the Scoville scale, resiniferatoxin is considered the harshest chemical in the world, with a value of 16 billion. Even in very low concentrations, contact with the substance immediately causes severe burning pain. 

Neurogenic inflammation and hypothermia

Ingestion causes neurogenic inflammation and hypothermia in mammals. In experiments with rats, a temperature loss of 2-3 K was found within one hour. Resiniferatoxin leads to desensitization to neurogenic inflammation and causes chemical and thermal analgesia. The toxicity of resiniferatoxin is due to the specific stimulation of sensory receptors in the ganglia, particularly heat receptors.
The sensory neurons responsible for the perception of pain are stimulated cell-selectively via the activation of the transient receptor protein TRPV1 (Transient Receptor Potential Vanilloid 1).

TRPV1 is primaril found in sensory neurons that respond to damaging or potentially damaging stimuli, known as nociceptors. It cooperates with another receptor called TRPA1 to mediate the detection of noxius environmental stimuli. Activation of the TRPV1 leads to the sensation of burning heat and pain.

Therapeutic target for pain management

TRPV1 is an ion channel located in the plasma membrane of sensory neurons. Upon activation by various stimuli (such as heat, capsaicin or acid) TRPV1 becomes permeable to Calcium ions. This influx of calcium ions results in neuronal depolarization and subsequent pain signal transmission to the brain. Researchers have validated TRPV1 as a therapeutic target for pain management.
Resiniferatoxin is used in research to study pain mechanisms and to develop painkillers. The therapeutic window of RTX is broad, allowing complete desensitization of pain perception and neurogenic inflammation without causing unacceptable side effects. Therefore, it is a promising candidate for pain therapy.

Resiniferatoxin acts as an agonist at the TRPV1 receptor, it activates TRPV1 and, with prolonged use, causes a decrease in TRPV1 activity (desensitization), resulting in pain relief via the subsequent reduction in TRPV1-mediated release of inflammatory molecules after exposure to noxious stimuli. It leads to desensitization of the receptor.

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