GSK172981 is a non-peptide tachykinin NK3 receptor antagonist. GSK172981 demonstrated high affinity for recombinant human (pK(i) value 7.7) and native guinea pig (pK(i) value 7.8) tachykinin NK(3) receptors. In vitro functional evaluations revealed GSK172981 to be a competitive antagonist (pA(2)=7.2) at cloned human tachykinin NK(3) receptor. GSK172981 also exhibited a competitive profile in antagonizing neurokinin B-stimulated neuronal activity recorded from the guinea pig medial habenula slices (apparent pK(B)=8.1). GSK172981 is potentially useful in the treatment of schizophrenia.
