GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Max) response induced by neurokinin B, indicating insurgable antagonist pharmacology (PA (2)=9.2). GSK256471 may be a promising candidate for the treatment of schizophrenia.
GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Max) response induced by neurokinin B, indicating insurgable antagonist pharmacology (PA (2)=9.2). GSK256471 may be a promising candidate for the treatment of schizophrenia.
GSK256471 is a potent selective NK(3) antagonist that shows a high affinity for recombinant human (PK (I) value 8.9) and native guinea pig (PK (I) value 8.4) tachykinin NK(3) receptors. In vitro functional assessment showed that GSK256471 reduced the E(Max) response induced by neurokinin B, indicating insurgable antagonist pharmacology (PA (2)=9.2). GSK256471 may be a promising candidate for the treatment of schizophrenia.
别名
GSK-256471, GSK 256471
化学信息
分子量
499.62
分子式
C29H29N3O3S
CAS No.
1133706-08-7
密度
1.290 g/cm3 (Predicted)
储存&溶解度
存储
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
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