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Literature DB >> 7857594

6-Fluoro-serotonin as a substrate for the neuronal serotonin transporter.

E Chanut¹, J J Bonnet, J H Trouvin, M Plat, J Costentin, C Jacquot.

Abstract

6-Fluoro-serotonin (6F-5-HT) was previously identified in the rat brain after peripheral administration of 6-fluoro-DL-tryptophan, a serotonin (5-HT) synthesis inhibitor. These present studies, performed with rat brain synaptosomes show that: i-neuronal 6F-5-HT uptake partly involved the 5-HT transporter since it was inhibited by clomipramine, a 5-HT uptake inhibitor, ii-6F-5-HT blocked the synaptosomal uptake of 3H-5-HT, with an IC50 value of 98 +/- 13 nM, and iii- 6F-5-HT induced 3H-5-HT release from preloaded synaptosomes, with an EC50 value of 95 +/- 6 nM; this release was decreased in the presence of clomipramine, suggesting the involvement of the 5-HT transporter. This release was also reduced when using synaptosomes from reserpinized rats, suggesting that the vesicular pool also participates to the 3H-5-HT release induced by 6F-5-HT. So, 6F-5-HT behaved as a substrate for the 5-HT neuronal transporter.

Entities: Chemical Gene Species

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Year: 1994 PMID： 7857594 DOI： 10.1007/bf01277932

Source DB: PubMed Journal: J Neural Transm Gen Sect

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References

20 in total

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Journal: Psychopharmacology (Berl) Date: 1981 Impact factor: 4.530

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Authors: J J Bonnet; J Costentin
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6-Fluoro-serotonin as a substrate for the neuronal serotonin transporter.

Review 1. Radioligands of the vesicular monoamine transporter and their use as markers of monoamine storage vesicles.

2. Stabilizing effect of sucrose on leakage of cytoplasm from rat brain synaptosomes in saline media.

3. Inhibition of serotonin biosynthesis by 6-halotryptophans in vivo.

4. Inhibition of rat brain tryptophan hydroxylase by 6-halotryptophans.

5. (+)-6-fluorotryptophan, an inhibitor of tryptophan hydroxylase: sleep and wakefulness in the rat.

6. d-Amphetamine as a releaser or reuptake inhibitor of biogenic amines in synaptosomes.

7. Rat brain monoamine metabolism and hypobaric hypoxia: a new approach.

8. Changes in the rat sleep-wake cycle produced by DL-6-fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase.

9. p-Chloroamphetamine induces serotonin release through serotonin transporters.

10. GBR 12783, a potent and selective inhibitor of dopamine uptake: biochemical studies in vivo and ex vivo.