A serotonin reuptake inhibitor
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LY393558

Item No. 32775

Technical Information
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
CAS Number
271780-64-4
Molecular Formula
C26H31FN4O4S2
Formula Weight
Purity
≥98%
A solid
DMSO: 10 mg/mlEthanol: 10 mg/ml
SMILES
CC(C)N1CC2=CC(S(C)(=O)=O)=CC=C2N(CCN3CCC(C4=CNC5=C4C=CC(F)=C5)=CC3)S1(=O)=O
InChi Code
InChI=1S/C26H31FN4O4S2/c1-18(2)31-17-20-14-22(36(3,32)33)5-7-26(20)30(37(31,34)35)13-12-29-10-8-19(9-11-29)24-16-28-25-15-21(27)4-6-23(24)25/h4-8,14-16,18,28H,9-13,17H2,1-3H3
InChi Key
QUSLYAPLTMMCFE-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    LY393558 is an inhibitor of serotonin (5-HT) reuptake (IC50 = 3.3 nM in rat cortical synaptosomes).1 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.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Pullar, I.A., Boot, J.R., Carney, S.L., et al. In vitro activity of LY393558, an inhibitor of the 5-hydroxytryptamine transporter with 5-HT1B/1D/2 receptor antagonist properties. Eur. J. Pharmacol. 432(1), 9-17 (2001).

    2. Morecroft, I., Pang, L., Baranowska, M., et al. In vivo effects of a combined 5-HT1B receptor/SERT antagonist in experimental pulmonary hypertension. Cardiovasc. Res. 85(3), 593-603 (2010).