NTI4F: a non-peptide fluorescent probe selective for functional delta opioid receptors

A non-peptide fluorescent probe, NTI4F, has been developed for the delta (delta) opioid receptor. The probe is a potent delta-antagonist in the mouse vas deferens (MVD) smooth muscle assay and it binds to the delta opioid receptor with high affinity (Ki = 1 nM) and selectivity. Confocal microscopy indicates that the probe binds to Madin-Darby canine kidney (MDCK) cells transfected with the delta opioid receptor. This binding can be blocked by the delta opioid receptor antagonist, naltrindole (NTI), but not by morphine or ethylketazocine (EK) which are mu (mu)- and kappa (kappa)-selective ligands. This fluorescent probe should prove useful in the study of the distribution of the delta opioid receptor.