CAS 271780-64-4|LY 393558

Introduction:Basic information about CAS 271780-64-4|LY 393558, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameLY 393558
CAS Number271780-64-4Molecular Weight546.67700
Density/Boiling Point/
Molecular FormulaC26H31FN4O4S2Melting Point/
MSDS/Flash Point/

Names

Name1-[2-[4-(6-fluoro-1H-indol-3-yl)-3,6-dihydro-2H-pyridin-1-yl]ethyl]-6-methylsulfonyl-3-propan-2-yl-4H-2λ6,1,3-benzothiadiazine 2,2-dioxide

LY 393558 BiologicalActivity

DescriptionLY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression[1].
Related CatalogResearch Areas >>Neurological DiseaseSignaling Pathways >>GPCR/G Protein >>5-HT ReceptorSignaling Pathways >>Neuronal Signaling >>5-HT Receptor
In VivoLY393558 (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.
References

[1]. Mitchell SN, et al. 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;432(1):19-27.

Chemical & Physical Properties

Molecular FormulaC26H31FN4O4S2
Molecular Weight546.67700
Exact Mass546.17700
PSA110.55000
LogP5.87740
InChIKeyQUSLYAPLTMMCFE-UHFFFAOYSA-N
SMILESCC(C)N1Cc2cc(S(C)(=O)=O)ccc2N(CCN2CC=C(c3c[nH]c4cc(F)ccc34)CC2)S1(=O)=O
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