Esa R. Korpi

1. Introduction 1.1. GABAA receptors GABAA receptors are a heterogeneous protein family in the nervous system and in non-neuronal tissues. They assemble as transmembrane homo-or heteropentameric anion channels, which specifically conduct bicarbonate and chloride anions and are gated by the endogenous ligand GABA. In most instances, opening of neuronal channels facilitates chloride movement from the extracellular space into the cytoplasm, with a net inhibitory effect (1–3).

Abstract Psychedelics produce fast and persistent antidepressant effects and induce neuroplasticity resembling the effects of clinically approved antidepressants. We recently reported that pharmacologically diverse antidepressants, including fluoxetine and ketamine, act by binding to TrkB, the receptor for BDNF.

1. Introduction Benzodiazepines (BZs) are positive allosteric modulators of γ-aminobutyric acid type A (GABAA) receptors and facilitate the modulation of chloride conductance by GABA (1–3). These drugs are among the most widely prescribed medications for the treatment of anxiety- and sleep-related disorders, but BZs have unwanted side effects including sedation and motor impairment, as well as the potential for abuse (1, 4).