Cat. No. 3350
Chemical Name: 1-[2-[4-(6-Fluoro-1H-indol-3-yl)-3,
Biological ActivityDual 5-HT1B/1D receptor antagonist (pKB values are 9.05 and 8.98 respectively) and 5-HT re-uptake inhibitor (pIC50 = 8.48). Potently antagonizes terminal autoreceptor activity in vitro and increases extracellular 5-HT levels above those evoked by fluoxetine (Cat. No. 0927) in vivo. Also acts as an antagonist at 5-HT2A and 5-HT2B receptors (pKi values are 7.29 and 7.35 respectively).
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Morecroft et al (2005) Functional interactions between 5-hydroxytryptamine receptors and the serotonin transporter in pulmonary arteries. J.Pharmacol.Exp.Ther. 313 539. PMID: 15659538.
Mitchell et al (2001) LY393558, a 5-hydroxytryptamine reuptake inhibitor and 5-HT1B/1D receptor antagonist: effects on extracellular levels of 5-hydroxytryptamine in the guinea pig and rat. Eur.J.Pharmacol. 432 19. PMID: 11734183.
Pullar et al (2001) In vitro activity of LY393558, an inhibitor of the 5-hydroxytryptamine transporter with 5-HT1B/1D/2 receptor antagonist properties. Eur.J.Pharmacol. 432 9. PMID: 11734182.
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