LY 393558

Cat. No. 3350

LY 393558 C26H31FN4O4S2 [271780-64-4]

Price and Availability

For LY 393558 pricing & availability please select your country from the drop down menu:
Submit
By clicking submit you agree to accept a cookie from Tocris Bioscience. For details, please read our privacy and cookie policy.

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

Biological Activity

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

M.Wt:
546.68
Formula:
C26H31FN4O4S2
Solubility:
Soluble to 100 mM in DMSO
Purity:
>97 %
Storage:
Store at -20°C
CAS No:
271780-64-4

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.

If you know of a relevant reference for this product please let us know.

Citations are publications that use Tocris products.

Do you know of a great paper that uses LY 393558 from Tocris? If so please let us know.

View Related Products by Product Action

Keywords: LY 393558, supplier, LY393558, dual, 5-HT1B, 5-HT1D, 5-HT1B/1D, receptors, antagonists, serotonin, reuptake, uptake, SERT, inhibitors, inhibits, transporters, 5-HT1, 5-Hydroxytryptamine, Tocris Bioscience, 5-HT1B Receptor Antagonist products

Quick Order

Find multiple products by catalog number

divider line

GPCR Product Listing

GPCR Product Listing

Highlights over 450 products for GPCRs. Request copy or view PDF today.

divider line

5-HT Review

Written by N. Barnes & J. Neumaler

5-HT Receptors Scientific Review

Our 5-HT review summarizes the serotonin receptor subtypes and highlights their importance in mediating various physiological & pharmacological processes. Request copy or view PDF today.

divider line

Parkinson's disease: Neurobiology and Therapeutic Strategies

Written by Anthony H.V. Schapira

Parkinson's Life Science Poster

Our Parkinson's disease (PD) poster summarizes the neurobiology of the disease, and highlights current therapeutic treatments for symptomatic PD. Request copy or view PDF today.

divider line

Regulation of Vascular Reactivity by GPCRs

Written by J.J. Maguire and A.P. Davenport

Cardiovascular Life Science Poster

Our Cardiovascular poster highlights the key G protein-coupled receptors involved in the regulation of vascular reactivity. Request copy today.

divider line

Bio-Techne Events

One Day Symposium

Bio-Techne Symposium 2017

Epigenetic Regulation of Stem Cell Differentiation

March 1, 2017

Amsterdam, The Netherlands