Conversion of the Potent δ-Opioid Agonist H-Dmt-Tic-NH-CH(2)-Bid into δ-Opioid Antagonists by N(1)-Benzimidazole Alkylation1

N(1)-Alkylation of 1H-benzimidizole of the δ agonist H-Dmt-Tic-NH-CH(2)-Bid with hydrophobic, aromatic, olefinic, acid, ethyl ester or amide (1–6) became δ antagonists (pA(2) = 8.52–10.14). δ- and μ-Opioid receptor affinities were high (K(i)δ = 0.12–0.36 nM and K(i)μ = 0.44–1.42 nM). Only δ antagoni...

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Main Authors: Balboni, Gianfranco, Guerrini, Remo, Salvadori, Severo, Negri, Lucia, Giannini, Elisa, Bryant, Sharon D., Jinsmaa, Yunden, Lazarus, Lawrence H.
Format: Artigo
Language:Inglês
Published: 2005
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Article
Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC2597450/
https://ncbi.nlm.nih.gov/pubmed/16366592
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm058259l
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