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, 307 (1), 117-9

Interactions of Selective Serotonin Reuptake Inhibitors With Subtypes of Sigma Receptors in Rat Brain

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Interactions of Selective Serotonin Reuptake Inhibitors With Subtypes of Sigma Receptors in Rat Brain

N Narita et al. Eur J Pharmacol.

Abstract

The interactions of selective serotonin reuptake inhibitors and tricyclic antidepressants with subtypes of sigma receptors were investigated. The rank order of affinity (Ki values) from competition experiments of [3H](+)-pentazocine binding to sigma 1 sites was: fluvoxamine > sertraline > S(+)-fluoxetine > (+/-)-fluoxetine > citalopram > imipramine > paroxetine > desipramine > R(-)-fluoxetine > (+/-)-norfluoxetine. The Ki values of all drugs for sigma 2 sites were more than 1000 nM. Furthermore, all drugs were more potent at sigma 1 sites than at sigma 2 sites. These findings suggest that sigma receptors (sigma 1 site) may play, in some way, a role in the actions of selective serotonin reuptake inhibitors.

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