Mescaline - Mode of Action

Mode of Action

Mescaline is produced when products of natural mammalian catecholamine-based neuronal signaling such as dopamine and serotonin are subjected to additional metabolism via methylation, and its hallucinogenic properties stem from these very structural similarities. In plants, this compound may be the end product of a pathway utilizing catecholamines as a method of stress response, similar to how animals may release compounds such as cortisol when stressed. The in vivo function of catecholamines have not been investigated, but they may function as antioxidants, as developmental signals, and as integral cell wall components that resist degradation from pathogens. The deactivation of catecholamines via methylation produces alkaloids such as mescaline.

Mescaline acts similarly to other psychedelic agents. It binds to and activates the serotonin 5-HT_2A receptor with a high affinity as a partial agonist. How activating the 5-HT_2A receptor leads to psychedelia is still unknown, but it likely somehow involves excitation of neurons in the prefrontal cortex. Mescaline is also known to bind to and activate the serotonin 5-HT_2C receptor.

In addition to serotonin receptor activity, mescaline also stimulates the dopamine receptors. Whether mescaline possesses dopamine receptor agonist properties or initiates the release of dopamine remains unclear.

Difluoro and trifluoromescaline have shown to be more potent than their unfluorinated analogue.