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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Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2012
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Article
Accesso online: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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