Elsevier

Biological Psychiatry

Volume 41, Issue 10, 15 May 1997, Pages 1010-1019
Biological Psychiatry

Original article
Neuroleptic binding to sigma receptors: Possible involvement in neuroleptic-induced acute dystonia

https://doi.org/10.1016/S0006-3223(96)00264-8Get rights and content

Several antipsychotic drugs, belonging to various chemical classes, were compared for their affinity for the σ, dopamine-D2, and muscarinic receptors. Many neuroleptic drugs were found to bind with high affinity to σ2 receptors, and the binding affinity was clearly different from that observed for dopamine-D2 receptors. The dopaminergic and muscarinic theories for the physiopathology of acute dystonia are not completely satisfactory. Since the σ receptors were reported to play a role in the control of movement, the high affinity of some neuroleptics for these sites suggests their possible involvement in some side effects, such as drug-induced dystonia. There was a correlation between the clinical incidence of neuroleptic-induced acute dystonia and binding affinity of drugs for the σ receptor, except for some drugs, with a lower incidence, displaying significant affinity for the cholinergic muscarinic receptor. Therefore, we conclude that the affinity for the σ receptor might be involved in neuroleptic-induced acute dystonia, but this might be partially corrected by the intrinsic anticholinergic properties of the drug.

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    Part of this work was supported by a grant from the Fonds National de la Recherche Scientifique (FRSM LN 9.4511.89) and by the Ministère de l'Education et de la Recherche Scientifique (Action concertée 89:95135).

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