Psychedelic-like Properties of Quipazine and Its Structural Analogues in Mice.

ABSTRACT: Known classic psychedelic serotonin 2A receptor (5-HT_2AR) agonists retain a tryptamine or phenethylamine at their structural core. However, activation of the 5-HT_2AR can be elicited by drugs lacking these fundamental scaffolds. Such is the case of the N-substituted piperazine quipazine. Here, we show that quipazine bound to and activated 5-HT_2AR as measured by [³H]ketanserin binding displacement, Ca²⁺ mobilization, and accumulation of the canonical G_q/11 signaling pathway mediator inositol monophosphate (IP₁) in vitro and in vivo. Additionally, quipazine induced via 5-HT_2AR an expression pattern of immediate early genes (IEG) in the mouse somatosensory cortex consistent with that of classi

SUBMITTER: de la Fuente Revenga M 

PROVIDER: S-EPMC7933111 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature