Serotonin 5-HT2A, 5-HT2c and 5-HT1A receptor involvement in the acute effects of psilocybin in mice. In vitro pharmacological profile and modulation of thermoregulation and head-twich response
Biomedicine & Pharmacotherapy August 29, 2022 Ines Erkizia-Santamaría, R. Alles-Pascual, Igor Horrillo et al. 108 citations
Psilocybin, a psychedelic drug that activates the 5-HT2A receptor, shows potential for treating neuropsychiatric diseases. In mice, psilocin (the active metabolite) binds with similar affinity to 5-HT2A, 5-HT2C, and 5-HT1A receptors. Psilocybin causes a dose-dependent head-twitch response, a sign of psychosis-like effects, which is blocked by a 5-HT2A antagonist but increased by a 5-HT2C antagonist. Body temperature rises at low doses but falls at higher doses; a 5-HT1A antagonist reverses this drop, causing hyperthermia. These findings clarify the roles of specific serotonin receptors in psilocybin's acute effects, aiding understanding of its therapeutic and side effects.