The present invention relates to three parts compounds, and it includes for the regulator part of inner body G-protein-coupling receptor (such as neurokinine-1 receptor), linker and the lipid-anchored object suitable for three parts compound to be anchored into plasma membrane. Pharmaceutical composition the invention further relates to prodrug and comprising the three parts compound and the three parts compound are conducted the purposes of disease or illness that (such as NK1R signal transductions) mediates in treatment by inner body G-protein-coupled receptor signal.