The opioid antagonist activities of two bivalent ligands, BNI and nor-BNI, have been
evaluated in smooth muscle preparations and in mice. Both ligands are highly potent and …

Previously, we reported on an opioid antagonist, nor-binaltorphimine (nor-BNI), that had
high selectivity for kappa opioid receptors in smooth muscle preparations. In this study, nor …

The structural determinants for the selective binding of the nonpeptide opioid receptor
antagonist nor-binaltorphimine (nor-BNI) to the K-opioid receptor were characterized using a …

The kappa-receptor selectivity of nor-binaltorphimine (nor-BNI), a highly selective kappa-
opioid receptor antagonist in vitro, was examined in vivo by measuring the time course of the …

Progress in opioid research relies heavily on ligands as probes to evaluate selectivity of
action. The design of such ligands using naltrexone as a precursor has afforded a number of …

Buprenorphine was studied for its antagonist activity against the specific κ-opioid agonist U-
50,488 H in pigeons responding under a multiple schedule of grain presentation and in mice …

The indole moiety in the delta-opioid antagonist, naltrindole (2, NTI), was employed as a
scaffold to hold an “address” for interaction with the kappa-opioid receptor. The attachment …

The pharmacological profile of the opioid antagonist norbinaltorphimine has been
characterised in vitro and in vivo. In vitro, norbinaltorphimine reversibly antagonised the …

In an effort to develop selective antagonists for opioid receptors, bivalent ligands that contain
opioid antagonist pharmacophores derived from naltrexone or other morphinans were …

5′-Guanidinonaltrindole (GNTI) possesses 5-fold greater opioid antagonist potency (Ke=
0.04 nM) and an order of magnitude greater selectivity (selectivity ratios> 500) than the …