[1][2] Pellotine is slightly narcotic, and has been used by Native Americans as a constituent of peyote for sacramental purposes.

[3] 8-10 mg of isolated pellotine is known to cause convulsions in frogs.

[4] 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.

[3] It is also reported to lower blood pressure and heart rate.

[3] Native inhabitants of north-eastern Mexico around 810–1070 CE (according to carbon dating) are thought to have used a number of "mescal buttons" (peyote plant material) containing mescaline, pellotine, and other related alkaloids.