A series of analogues of the previously reported NK1 tachykinin antago
nist [Orn6, Glu(OBzl)11]-SP6-11-OBzl has been synthesized and tested i
n order to investigate the effects on antagonistic activity of modific
ations at the C-terminal residue. The biological activity in the guine
a-pig ileum assay (NK1 receptor) indicates that the two aromatic rings
introduced in the C-terminal part of the peptide are both essential f
or the expression of antagonistic activity.