1-(2-[4-(6-FLUORO-1H-INDOL-3-YL)-3,6-DIHYDRO-2H-PYRIDIN-1-YL]-ETHYL)-3-ISOPROPYL-6-METHANESULFONYL-3,4-DIHYDRO-1H-BENZO[1,2,6]THIADIAZINE 2,2-DIOXIDE Chemical Properties

Boiling point:

785.7±60.0 °C(Predicted)

Density 

1.359±0.06 g/cm3(Predicted)

storage temp. 

Store at +4°C

solubility 

Soluble to 100 mM in DMSO

form 

Powder

pka

16.46±0.30(Predicted)

1-(2-[4-(6-FLUORO-1H-INDOL-3-YL)-3,6-DIHYDRO-2H-PYRIDIN-1-YL]-ETHYL)-3-ISOPROPYL-6-METHANESULFONYL-3,4-DIHYDRO-1H-BENZO[1,2,6]THIADIAZINE 2,2-DIOXIDE Usage And Synthesis

Uses

LY 393558 acts as a 5HT1B/D receptor antagonist which has been shown to limit serotonin reuptake on extracellular levels. Potential use in the treatment of IBS.

Biological Activity

Dual 5-HT 1B/1D receptor antagonist (pK B values are 9.05 and 8.98 respectively) and 5-HT re-uptake inhibitor (pIC 50 = 8.48). Potently antagonizes terminal autoreceptor activity in vitro and increases extracellular 5-HT levels above those evoked by fluoxetine 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).

1-(2-[4-(6-FLUORO-1H-INDOL-3-YL)-3,6-DIHYDRO-2H-PYRIDIN-1-YL]-ETHYL)-3-ISOPROPYL-6-METHANESULFONYL-3,4-DIHYDRO-1H-BENZO[1,2,6]THIADIAZINE 2,2-DIOXIDE(271780-64-4)Related Product Information

• 6-FLUORO-3-(1,2,3,6-TETRAHYDRO-PYRIDIN-4-YL)-1H-INDOLE
• 1-(2-[4-(6-FLUORO-1H-INDOL-3-YL)-3,6-DIHYDRO-2H-PYRIDIN-1-YL]-ETHYL)-3-ISOPROPYL-6-METHANESULFONYL-3,4-DIHYDRO-1H-BENZO[1,2,6]THIADIAZINE 2,2-DIOXIDE