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• W232370915 startingPage "2927" @default.
• W232370915 abstract "We synthesized derivatives of the δ opioid receptor (DOR) antagonists naltrindole (NTI) and compound 1 that were modified with small alkyl or fluorinated ethyl substituents on the 17-nitrogen. Although the derivatives showed decreased binding affinities for the opioid receptors, their selectivities for the DOR were higher than the parent compounds NTI and compound 1. Surprisingly, 17-fluoroethyl NTI derivatives exerted DOR inverse agonistic activities. The DOR inverse agonism of compounds 4c-e was less efficacious but significant, as compared with a standard DOR inverse agonist ICI-174864. On the other hand, compound 1 and its derivatives with small alkyl or monofluoroethyl substituents were partial agonists, but the derivatives having di- or trifluoroethyl group showed neither agonistic nor inverse agonistic activities." @default.
• W232370915 created "2016-06-24" @default.
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• W232370915 date "2015-08-01" @default.
• W232370915 modified "2023-09-27" @default.
• W232370915 title "Naltrindole derivatives with fluorinated ethyl substituents on the 17-nitrogen as δ opioid receptor inverse agonists" @default.
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• W232370915 doi "https://doi.org/10.1016/j.bmcl.2015.05.038" @default.
• W232370915 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/26048798" @default.
• W232370915 hasPublicationYear "2015" @default.
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