A serotonin reuptake inhibitor (IC50 = 3.3 nM in rat cortical synaptosomes); selective for serotonin reuptake over norepinephrine reuptake in rat cortical synaptosomes (IC50 = 2

LY393558 – 1 mg

Brand:
Cayman
CAS:
271780-64-4
Storage:
-20
UN-No:
- /

LY393558 is an inhibitor of serotonin (5-HT) reuptake (IC50 = 3.3 nM in rat cortical synaptosomes).{57349} It is selective for serotonin reuptake over norepinephrine reuptake in rat cortical synaptosomes (IC50 = 2,510 nM) but does inhibit 5-HT-induced [35S]GTPγS binding in cells expressing human 5-HT1B or 5-HT1D receptors (Kbs = 0.89 and 10.4 nM, respectively). LY393558 (30 mg/kg per day) reduces pulmonary vascular remodeling, increases in right ventricular systolic pressure, and the development of right ventricular hypertrophy in a mouse model of pulmonary arterial hypertension induced by overexpression of the serotonin transporter and hypoxia.{57350}  

 

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Description

A serotonin reuptake inhibitor (IC50 = 3.3 nM in rat cortical synaptosomes); selective for serotonin reuptake over norepinephrine reuptake in rat cortical synaptosomes (IC50 = 2,510 nM); inhibits 5-HT-induced [35S]GTPγS binding in cells expressing human 5-HT1B or 5-HT1D receptors (Kbs = 0.89 and 10.4 nM, respectively); reduces pulmonary vascular remodeling, increases in right ventricular systolic pressure, and the development of right ventricular hypertrophy in a mouse model of pulmonary arterial hypertension at 30 mg/kg per day

Formal 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

Synonyms: 

Molecular weight: 546.7

CAS: 271780-64-4

Purity: ≥98%

Formulation: A solid

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