GSK256471 is a potent and selective NK(3) antagonist. GSK256471 demonstrated 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 evaluations revealed GSK256471 diminished the neurokinin B-induced E(max) response, indicative of non-surmountable antagonist pharmacology (pA(2)=9.2). GSK256471 may be promising drug candidate in the treatment of schizophrenia. References: Dawson LA, Langmead CJ, Dada A, Watson JM, Wu Z, de la Flor R, Jones GA, Cluderay JE, Southam E, Murkitt GS, Hill MD, Jones DN, Davies CH, Hagan JJ, Smith PW. In vitro and in vivo comparison of two non-peptide tachykinin NK3 receptor antagonists: Improvements in efficacy achieved through enhanced brain penetration or altered pharmacological characteristics. Eur J Pharmacol. 2010 Feb 10;627(1-3):106-14. doi: 10.1016/j.ejphar.2009.10.054. Epub 2009 Oct 30. PubMed PMID: 19879867.

纯度：≥98%

CAS：1133706-08-7