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编 号：F300989
分子式：C26H31FN4O4S2
分子量：546.68
分子式：C26H31FN4O4S2
分子量：546.68
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CAS No: 271780-64-4
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生物活性：
LY393558 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.
体内研究：
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.LY393558 (20 mg/kg; p.o., single) completely abolishes the reduction of levels of 5-HT induced by tetrodotoxin (1μM) in guinea pigs model.LY393558 (1-20 mg/kg; p.o., single) significantly increases extracellular levels of 5-HT in rats model.LY393558 (5 mg/kg/day; p.o., 21 days) can still elicit a further increase in extracellular 5-HT in chronic treatment.Animal Model:Female Dunkin Hartley guinea pigs (350-400 g)
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)
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)
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)
Dosage:5 mg/kg/day
Administration:p.o., 21 days
Result:Still elicited a further increase in extracellular 5-HT in chronic treatment.
LY393558 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.
体内研究：
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.LY393558 (20 mg/kg; p.o., single) completely abolishes the reduction of levels of 5-HT induced by tetrodotoxin (1μM) in guinea pigs model.LY393558 (1-20 mg/kg; p.o., single) significantly increases extracellular levels of 5-HT in rats model.LY393558 (5 mg/kg/day; p.o., 21 days) can still elicit a further increase in extracellular 5-HT in chronic treatment.Animal Model:Female Dunkin Hartley guinea pigs (350-400 g)
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)
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)
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)
Dosage:5 mg/kg/day
Administration:p.o., 21 days
Result:Still elicited a further increase in extracellular 5-HT in chronic treatment.
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