GSK256471 is a non-peptide antagonist targeting the tachykinin NK3 receptor, exhibiting a pKi of 8.9 for the human recombinant receptor and 8.4 for the guinea pig native receptor. This compound demonstrates over 100-fold selectivity against NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 irreversibly inhibits neurokinin B (NKB)-induced inositol phosphate accumulation, and has been shown to mitigate wet dog shaking behavior and suppress dopamine release. This compound serves as a valuable tool for studying the pathophysiology of schizophrenia.
GSK256471 is a non-peptide antagonist targeting the tachykinin NK3 receptor, exhibiting a pKi of 8.9 for the human recombinant receptor and 8.4 for the guinea pig native receptor. This compound demonstrates over 100-fold selectivity against NK1 (pKi = 5.2) and NK2 (pKi = 7.3) receptors. GSK256471 irreversibly inhibits neurokinin B (NKB)-induced inositol phosphate accumulation, and has been shown to mitigate wet dog shaking behavior and suppress dopamine release. This compound serves as a valuable tool for studying the pathophysiology of schizophrenia.
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