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Dopamine transporter site-directed mutations differentially alter substrate transport and cocaine binding.
TLDR
Results demonstrate that aspartate and serine residues lying within the first and seventh hydrophobic putative transmembrane regions are crucial for DAT function and provide identification of residues differentially important for cocaine binding and for dopamine uptake. Expand
Synthesis, opioid receptor binding, and bioassay of naltrindole analogues substituted in the indolic benzene moiety.
TLDR
The results of the present study suggest that morphinan derivatives related to 16 and 14 may provide useful leads for the development of potent nonpeptide ligands possessing delta agonist or mixed delta antagonist/mu agonist activities. Expand
Synthesis, opioid receptor binding, and biological activities of naltrexone-derived pyrido- and pyrimidomorphinans.
TLDR
A series of pyrido- and pyrimidomorphinans synthesized from naltrexone were evaluated for binding and biological activity at the opioid receptors, indicating the existence of a somewhat similar steric constraint at the ligand binding sites of delta, mu, and kappa receptors. Expand
Effect of N-alkyl and N-alkenyl substituents in noroxymorphindole, 17-substituted-6,7-dehydro-4,5alpha-epoxy-3,14-dihydroxy-6,7:2',3'-indolomorphinans, on opioid receptor affinity, selectivity, and
TLDR
Several N-substituted noroxymorphindoles were found to be more mu/delta-selective than naltrindole (NTI) in receptor binding assays and considerably more selective than NTI in the functional assays. Expand
Identification of the first trans-(3R,4R)- dimethyl-4-(3-hydroxyphenyl)piperidine derivative to possess highly potent and selective opioid kappa receptor antagonist activity.
TLDR
A structurally novel opioid kappa receptor selective ligand has been identified and demonstrated high affinity and highly potent and selective kappa antagonism in the [(35)S]GTP-gamma-S assay using cloned opioid receptors. Expand
Investigation of the N-substituent conformation governing potency and mu receptor subtype-selectivity in (+)-(3R, 4R)-dimethyl-4-(3-hydroxyphenyl)piperidine opioid antagonists.
TLDR
It is found that free rotation of the phenyl ring is necessary for high affinity binding and mu receptor subtype selectivity as the planar N-substituted thianaphthylmethyl and benzofuranylmethyl compounds 13 and 14 had significantly lower binding affinities. Expand
Enantiomers of diastereomeric cis-N-[1-(2-hydroxy-2-phenylethyl)- 3-methyl-4-piperidyl]-N-phenylpropanamides: synthesis, X-ray analysis, and biological activities.
TLDR
Using the optical isomers of cis-3-methylfentanyl as reference compounds, the effects on the pharmacological activities of introducing a phenylethyl 2-hydroxyl group into the molecule were analyzed. Expand
In vitro and in vivo characterization of [125I]iodomethyllycaconitine in the rat
TLDR
The results suggest that [125I]iodoMLA will be a useful radioligand to study the α7 nAChR in vitro and in vivo and suggest that it was rapidly cleared and exhibited poor brain penetration in the rat. Expand
Factors influencing agonist potency and selectivity for the opioid delta receptor are revealed in structure-activity relationship studies of the
TLDR
It was determined that mu receptor affinity could be increased while maintaining delta receptor affinity, especially when hydroxyl-substituted compounds are considered, and that ligands of this class will more easily be converted to mu/delta combination agonists compared to the piperazine ligands such as 1. Expand
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