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Design, synthesis, and evaluation of new endomorphin analogs with enhanced central antinociception after peripheral administration.
Liu, Xin; Zhao, Long; Wang, Yuan; Mou, Lingyun; Yang, Junxian; Zhang, Yixin; Wang, Dan; Wang, Rui.
Afiliação
  • Liu X; Department of pharmacology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Biochemistry and Molecular Biology, School of Basic Medical Sciences, School of Life Science, Lanzhou University, Lanzhou 730000, PR China.
  • Zhao L; Department of pharmacology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Biochemistry and Molecular Biology, School of Basic Medical Sciences, School of Life Science, Lanzhou University, Lanzhou 730000, PR China.
  • Wang Y; Department of pharmacology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Biochemistry and Molecular Biology, School of Basic Medical Sciences, School of Life Science, Lanzhou University, Lanzhou 730000, PR China.
  • Mou L; Department of pharmacology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Biochemistry and Molecular Biology, School of Basic Medical Sciences, School of Life Science, Lanzhou University, Lanzhou 730000, PR China.
  • Yang J; Department of pharmacology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Biochemistry and Molecular Biology, School of Basic Medical Sciences, School of Life Science, Lanzhou University, Lanzhou 730000, PR China.
  • Zhang Y; Department of pharmacology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Biochemistry and Molecular Biology, School of Basic Medical Sciences, School of Life Science, Lanzhou University, Lanzhou 730000, PR China.
  • Wang D; Department of pharmacology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Biochemistry and Molecular Biology, School of Basic Medical Sciences, School of Life Science, Lanzhou University, Lanzhou 730000, PR China.
  • Wang R; Department of pharmacology, Key Laboratory of Preclinical Study for New Drugs of Gansu Province, Institute of Biochemistry and Molecular Biology, School of Basic Medical Sciences, School of Life Science, Lanzhou University, Lanzhou 730000, PR China. Electronic address: wangrui@lzu.edu.cn.
Bioorg Med Chem Lett ; 25(22): 5393-7, 2015 Nov 15.
Article em En | MEDLINE | ID: mdl-26403932
We synthesized two novel endomorphin-1 (EM-1) analogs by substituting the C-terminus residue with (thienyl)-α-methylene-ß-amino acids (Map). Several in vitro and in vivo assays were used to determine the activity of the analogs. The two EM-1 analogs showed subnanomolar binding affinity and functional activity at the µ-opioid receptor in HEK293 cells. Tail-flick and formalin tests further revealed that the EM-1 analogs were very effective after intravenous administration. Our results indicate that compared to endomorphin-1, the (thienyl)Map modified peptides showed improved blood-brain barrier permeability.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oligopeptídeos / Desenho de Fármacos / Receptores Opioides mu Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Oligopeptídeos / Desenho de Fármacos / Receptores Opioides mu Limite: Humans Idioma: En Revista: Bioorg Med Chem Lett Assunto da revista: BIOQUIMICA / QUIMICA Ano de publicação: 2015 Tipo de documento: Article