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Further evidence for the importance of 5-HT1A autoreceptors in the action of selective serotonin reuptake inhibitors
- Source :
- European Journal of Pharmacology. 260:251-255
- Publication Year :
- 1994
- Publisher :
- Elsevier BV, 1994.
-
Abstract
- The clinical efficacy of antidepressants that block serotonin (5-hydroxytryptamine, 5-HT) reuptake may be restrained by indirect activation of autoreceptors. In vivo microdialysis in rat hippocampus was used to assess the release-inhibitory properties of the 5-HT reuptake inhibitors citalopram and paroxetine. When reuptake was first blocked by infusing citalopram into the hippocampus, systemic administration of citalopram or paroxetine resulted in a 50–70% decrease in hippocampal 5-HT overflow. This presumably reflected the inhibition of 5-HT release subsequent to reuptake blockade in the raphe nuclei and, in turn, activation of somatodendritic autoreceptors. In support, pretreatment with (±)-pindolol or(+)-WAY100135 ((+)-N-tert-butyl-3-(4- (2-methoxyphenyl)piperazine-1-yl)-2-phenylpropanamide dihydrochloride), to block 5-HT1A autoreceptors, abolished the decrease in 5-HT produced by systemic injection of the uptake blockers.
- Subjects :
- Male
medicine.medical_specialty
Microdialysis
Citalopram
Pharmacology
Hippocampus
Piperazines
Reuptake
Rats, Sprague-Dawley
Internal medicine
medicine
Animals
Autoreceptors
Analysis of Variance
Chemistry
Stereoisomerism
Paroxetine
Antidepressive Agents
Rats
Endocrinology
Mechanism of action
Pindolol
Receptors, Serotonin
Raphe Nuclei
Serotonin Antagonists
Serotonin
medicine.symptom
Raphe nuclei
Reuptake inhibitor
Selective Serotonin Reuptake Inhibitors
medicine.drug
Subjects
Details
- ISSN :
- 00142999
- Volume :
- 260
- Database :
- OpenAIRE
- Journal :
- European Journal of Pharmacology
- Accession number :
- edsair.doi.dedup.....a187fb832fce7083c4073ad09172bb1c