Variation of the net charge, lipophilicity, and side chain flexibility in Dmt(1)-DALDA: Effect on Opioid Activity and Biodistribution

The influence of the side chain charges of the second and fourth amino acid residues in the peptidic μ opioid lead agonist Dmt-d-Arg-Phe-Lys-NH(2) ([Dmt(1)]-DALDA) was examined. Additionally, to increase the overall lipophilicity of [Dmt(1)]-DALDA and to investigate the Phe(3) side chain flexibility...

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Veröffentlicht in:	Journal of medicinal chemistry 2012-11, Vol.55 (22), p.9549
Hauptverfasser:	Novoa, Alexandre, Van Dorpe, Sylvia, Wynendaele, Evelien, Spetea, Mariana, Bracke, Nathalie, Stalmans, Sofie, Betti, Cecilia, Chung, Nga N, Lemieux, Carole, Zuegg, Johannes, Cooper, Matthew A, Tourwé, Dirk, De Spiegeleer, Bart, Schiller, Peter W, Ballet, Steven
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics, Opioid - pharmacology Animals Blood-Brain Barrier Brain - drug effects Mice Molecular Structure Nociception - drug effects Oligopeptides - chemistry Oligopeptides - pharmacokinetics Oligopeptides - pharmacology Opioid Peptides - metabolism Pain Measurement - drug effects Receptors, Opioid - metabolism Structure-Activity Relationship Tissue Distribution
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