LY 393558

Key Product Details

Product Description

LY 393558 is a dual 5-HT_1B/1D receptor antagonist (pK_B 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-HT_2A and 5-HT_2B receptors (pK_i values are 7.29 and 7.35 respectively).

Product Specifications for LY 393558

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for LY 393558

The following data is based on the product molecular weight 546.68.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.83 mL	9.15 mL	18.29 mL
5 mM	0.37 mL	1.83 mL	3.66 mL
10 mM	0.18 mL	0.91 mL	1.83 mL
50 mM	0.04 mL	0.18 mL	0.37 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Pullar In vitro activity of LY393558, an inhibitor of the 5-hydroxytryptamine transporter with 5-HT_1B/1D/2 receptor antagonist properties. Eur.J.Pharmacol. 2001 PMID: 11734182
• Morecroft Functional interactions between 5-hydroxytryptamine receptors and the serotonin transporter in pulmonary arteries. J.Pharmacol.Exp.Ther. 2005 PMID: 15659538
• Mitchell LY393558, a 5-hydroxytryptamine reuptake inhibitor and 5-HT_1B/1D receptor antagonist: effects on extracellular levels of 5-hydroxytryptamine in the guinea pig and rat. Eur.J.Pharmacol. 2001 PMID: 11734183

Product Documents for LY 393558