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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Bibliographic Details
Main Authors:	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:	Artigo
Language:	Inglês
Published:	2012
Subjects:	Article
Online Access:	https://ncbi.nlm.nih.gov/pmc/articles/PMC3523097/ https://ncbi.nlm.nih.gov/pubmed/23102273 https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm3008079
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Variation of the net charge, lipophilicity and side chain flexibility in Dmt(1)-DALDA: effect on opioid activity and biodistribution

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