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Submit ReviewLY 393558
Description: Dual 5-HT1B and 5-HT1D antagonist; also 5-HT re-uptake inhibitor
Chemical Name: 1-[2-[4-(6-Fluoro-1H-indol-3-yl)-3,6-dihydro-1(2H)-pyridinyl]ethyl]-3,4-dihydro-3-(1-methylethyl)-6-(methylsulfonyl)-1H-2,1,3-benzothiadiazine-2,2-dioxide
Purity: ≥97% (HPLC)
Biological Activity for LY 393558
LY 393558 is a dual 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).
Technical Data for LY 393558
| M. Wt | 546.68 |
| Formula | C26H31FN4O4S2 |
| Storage | Store at -20°C |
| Purity | ≥97% (HPLC) |
| CAS Number | 271780-64-4 |
| PubChem ID | 10347428 |
| InChI Key | QUSLYAPLTMMCFE-UHFFFAOYSA-N |
| Smiles | CC(C)N2S(N(CCN3CC=C(C4=CNC5=C4C=CC(F)=C5)CC3)C1=CC=C(S(=O)(C)=O)C=C1C2)(=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Product Datasheets for LY 393558
References for LY 393558
References are publications that support the biological activity of the product.
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
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
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Citations for LY 393558
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
5-HT Receptors Scientific Review
Written by Nicholas M. Barnes and John F. Neumaier, this review summarizes the various serotonin receptor subtypes and their importance in mediating the role of serotonin in numerous physiological and pharmacological processes. Compounds available from Tocris are listed.
Parkinson's Disease Poster
Parkinson's disease (PD) causes chronic disability and is the second most common neurodegenerative condition. This poster outlines the neurobiology of the disease, as well as highlighting current therapeutic treatments for symptomatic PD, and emerging therapeutic strategies to delay PD onset and progression.