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.
Publication types
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Antidepressive Agents, Second-Generation / pharmacology
-
Antidepressive Agents, Tricyclic / metabolism
-
Antidepressive Agents, Tricyclic / pharmacology*
-
Brain / drug effects
-
Brain / metabolism
-
Brain / ultrastructure*
-
Desipramine / pharmacology
-
Fluoxetine / analogs & derivatives
-
Fluoxetine / pharmacology
-
Imipramine / pharmacology
-
Male
-
Rats
-
Rats, Sprague-Dawley
-
Receptors, Opioid, delta / classification
-
Receptors, Opioid, delta / drug effects
-
Receptors, Opioid, delta / metabolism*
-
Selective Serotonin Reuptake Inhibitors / metabolism
-
Selective Serotonin Reuptake Inhibitors / pharmacology*
-
Stereoisomerism
Substances
-
Antidepressive Agents, Second-Generation
-
Antidepressive Agents, Tricyclic
-
Receptors, Opioid, delta
-
Serotonin Uptake Inhibitors
-
Fluoxetine
-
norfluoxetine
-
Imipramine
-
Desipramine