174635-69-9 (S)-3-甲基-2-苯基-N-(1-苯基丙基)喹啉-4-甲酰胺
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安全说明
运输方式为冰袋运输。危险性质:非危险化学品。WGK Germany:3,存储类别为11 - 可燃固体。
用途与制备
SB-222200 is an effective, selective, oral-active, BBB-permeable NK-3 receptor antagonist developed for CNS disease research. In vitro: inhibits ¹²⁵I-[MePhe⁷]NKB binding to CHO-hNK-3R (Ki 4.4 nM), antagonizes NKB-induced Ca²⁺ mobilization in HEK 293-hNK-3R (IC50 18.4 nM), selective for hNK-3 vs hNK-1 (Ki >100,000 nM) and hNK-2 (Ki 250 nM). In vivo: 5 mg/kg p.o. pretreatment inhibits senktide-induced behavioral responses in mice (57% inhibition); pharmacokinetics: rat T½ ~2 h, plasma clearance 56 mL/min/kg, Vd 3-5 L/kg; oral bioavailability 46% in rats (2.5 mg/kg i.v., 10 mg/kg p.o.).
医药