Irreversible blockade of sigma‐1 receptors by haloperidol and its metabolites in guinea pig brain and SH‐SY5Y human neuroblastoma cells

  title={Irreversible blockade of sigma‐1 receptors by haloperidol and its metabolites in guinea pig brain and SH‐SY5Y human neuroblastoma cells},
  author={Enrique J. Cobos and Esperanza Del Pozo and Jose M. Baeyens},
  journal={Journal of Neurochemistry},
We evaluated the effect of haloperidol (HP) and its metabolites on [3H](+)‐pentazocine binding to σ1 receptors in SH‐SY5Y human neuroblastoma cells and guinea pig brain P1, P2 and P3 subcellular fractions. Three days after a single i.p. injection in guinea pigs of HP (but not of other σ1 antagonists or (−)‐sulpiride), [3H](+)‐pentazocine binding to brain membranes was markedly decreased. Recovery of σ1 receptor density to steady state after HP‐induced inactivation required more than 30 days. HP… 
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