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Binding of norbinaltorphimine (norBNI) congeners to wild-type and mutant mu and kappa opioid receptors: molecular recognition loci for the pharmacophore and address components of kappa antagonists.
It is suggested that the antagonist pharmacophore is bound within this highly conserved region of the kappa or mutant mu receptor and that an anionic residue at the top of TM6 (E297 or K303E, respectively) provides additional binding affinity. Expand
Binaltorphimine-related bivalent ligands and their kappa opioid receptor antagonist selectivity.
The pharmacologic data suggest that only one antagonist pharmacophore may be required for kappa selectivity and that the other morphinan portion of the molecule confers selectivity by interacting with a unique subsite proximal to the antagonist pharmacphore recognition locus. Expand
Allylprodine analogues as receptor probes. Evidence that phenolic and nonphenolic ligands interact with different subsites on identical opioid receptors.
The m-hydroxy analogues of allylprodine and related structures have been synthesized and tested for narcotic agonist and antagonist activity on the electrically stimulated guinea pig ileum and by theExpand
Opioid agonist and antagonist activities of peripherally selective derivatives of naltrexamine and oxymorphamine.
The present study suggests that zwitterionic groups are highly effective in preventing penetration of ligands into the CNS and may be useful pharmacologic tools for investigation of peripheral opioid mechanisms. Expand
Inhibition of substance P release from spinal cord tissue after pretreatment with capsaicin does not mediate the antinociceptive effect of capsaicin in adult mice
D‐Substance P(1–7), which prevents antinociception, blocked capsaicin‐ and SP(1-7)‐induced decreases in SP release, indicating that these effects are mediated by SP N‐terminal activity. Expand
Synthesis and pharmacologic characterization of an alkylating analogue (chlornaltrexamine) of naltrexone with ultralong-lasting narcotic antagonist properties.
Protection studies in mice suggest that CNA mediates its narcotic antagonist effects by interacting with the same receptors that are occupied by naloxone. Expand
Opioid agonist and antagonist bivalent ligands. The relationship between spacer length and selectivity at multiple opioid receptors.
No correlation between binding and antagonist activity was observed at mu opioid receptors and the peak antagonism of ethylketazocine, a kappa receptor agonist, occurred with the bivalent ligand 9, and it was found that 9 is the most selective kappa antagonist in the series. Expand
Opioid receptor binding characteristics of the non-equilibrium μ antagonist, β-funaltrexamine (β-FNA)☆
Abstract β-Funaltrexamine (β-FNA) bound to mouse brain membranes in a reversible and an irreversible (not removed by washing of the membrane) manner, and a portion of each type of binding wasExpand