Synthesis, in Vitro Binding Profile, and Autoradiographic Analysis of -cis-3--2-phenylpiperidine, a Highly Potent and Selective Nonpeptide Substance P Receptor Antagonist Radioligand

Article abstract of DOI:10.1021/jm00073a022

The synthesis of a highly potent and selective NK₁ receptor antagonist radioligand, <3H>-cis-3-<(2-methoxybenzyl)amino>-2-phenylpiperidine (6a) is described.The in vitro binding pharmacology and autoradiographic distribution of 6a in guinea pig brain following peripheral administration are also reported.