Pellotine


Pellotine, also known as peyotline or N-methylanhalonidine, is a tetrahydroisoquinoline alkaloid found in Lophophora species, in particular L. diffusa. It is the second most common alkaloid found in Lophophora williamsii. Pellotine is slightly sedative, and has been used by Native Americans as a constituent of peyote for sacramental purposes. It was reportedly once marketed for use as a sedative. Pellotine has been sold online.

Pharmacology and effects

Doses of 8 to 10mg of isolated pellotine are known to cause convulsions in frogs. When injected subcutaneously to humans, participants have reported drowsiness and a desire not to exert any physical or mental effort, with one study reporting it to have hypnotic effects. It is also reported to lower blood pressure and heart rate. Pellotine produced no hallucinogenic effects in humans at doses of up to 250mg. However, it has been reported to have a calming or sedative effect instead.
Pellotine has been identified as a selective and potent serotonin 5-HT6 receptor weak partial agonist, serotonin 5-HT7 receptor inverse agonist, and serotonin 5-HT1D receptor ligand. In rodents, pellotine dose-dependently produces hypolocomotion, inhibits REM sleep, and promotes sleep fragmentation. The hypnotic effects of pellotine may be mediated by interactions with serotonin receptors.
Side effects of pellotine include dizziness, nausea, vertigo, and vomiting.

Ancient use

Native inhabitants of north-eastern Mexico around 810–1070 CE are thought to have used a number of "mescal buttons" containing mescaline, pellotine, and other related alkaloids. While it is known that the cytisine-containing "mescal beans" were at least ornamental, it is unclear whether "mescal buttons" were ornamental or used for their psychoactive effects.