| Identification | Back Directory | [Name]
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 | [CAS]
271780-64-4 | [Synonyms]
LY-393558
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
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
1H-2,1,3-BENZOTHIADIAZINE, 1-[2-[4-(6-FLUORO-1H-INDOL-3-YL)-3,6-DIHYDRO-1(2H)-PYRIDINYL]ETHYL]-3,4-DIHYDRO-3-(1-METHYLETHYL)-6-(METHYLSULFONYL)-, 2,2-DIOXIDE | [Molecular Formula]
C26H31FN4O4S2 | [MDL Number]
MFCD10565930 | [MOL File]
271780-64-4.mol | [Molecular Weight]
546.68 |
| Chemical Properties | Back Directory | [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) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [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). | [in vivo]
LY393558 (1-20 mg/kg; p.o., single) raises extracellular levels of 5-HT to 200-250% at 1 mg/kg in guinea pigs model, while levels of 5-HT to approximately 1500% at the highest dose 20 mg/kg[1].
LY393558 (20 mg/kg; p.o., single) completely abolishes the reduction of levels of 5-HT induced by tetrodotoxin (1μM) in guinea pigs model[1].
LY393558 (1-20 mg/kg; p.o., single) significantly increases extracellular levels of 5-HT in rats model[1].
LY393558 (5 mg/kg/day; p.o., 21 days) can still elicit a further increase in extracellular 5-HT in chronic treatment[1]. | Animal Model: | Female Dunkin Hartley guinea pigs (350-400 g)[1] | | Dosage: | 1-20 mg/kg | | Administration: | p.o., single | | Result: | Extracellular levels of 5-HT reached 200-250% at 1 mg/kg, while levels of 5-HT reached approximately 1500% at the highest dose 20 mg/kg. |
| Animal Model: | Female Dunkin Hartley guinea pigs (350-400 g)[1] | | Dosage: | 20 mg/kg | | Administration: | p.o., single | | Result: | Completely abolished the reduction of levels of 5-HT induced by tetrodotoxin (1μM). |
| Animal Model: | Male Lister Hooded rats (290-320 g)[1] | | Dosage: | 1-20 mg/kg | | Administration: | p.o., single | | Result: | Significantly increased extracellular levels of 5-HT. |
| Animal Model: | Male Lister Hooded rats (290-320 g)[1] | | Dosage: | 5 mg/kg/day | | Administration: | p.o., 21 days | | Result: | Still elicited a further increase in extracellular 5-HT in chronic treatment. |
| [storage]
Store at -20°C |
|
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|