Antidepressants enter cells, organelles, and membranes.

ABSTRACT: We begin by summarizing several examples of antidepressants whose therapeutic actions begin when they encounter their targets in the cytoplasm or in the lumen of an organelle. These actions contrast with the prevailing view that most neuropharmacological actions begin when drugs engage their therapeutic targets at extracellular binding sites of plasma membrane targets-ion channels, receptors, and transporters. We review the chemical, pharmacokinetic, and pharmacodynamic principles underlying the movements of drugs into subcellular compartments. We note the relationship between protonation-deprotonation events and membrane permeation of antidepressant drugs. The key properties relate to charge and hydrophobicity/lipid solubility, summarized by the parameters LogP, pK_a, and LogD

SUBMITTER: Blumenfeld Z 

PROVIDER: S-EPMC10700606 | biostudies-literature | 2024 Jan

REPOSITORIES: biostudies-literature