Studies on Peptides. CL. Syntheses of [D-His2] -Analogs of Enkephalin and Adrenorphin and Several [D-Arg2] enkephalin Analogs

SUSUMU FUNAKOSHI; MINORU KUBOTA; NAOTO KOSUGA; JIAN-PING XU; HARUAKI YAJIMA; WEI LI; SHIGEKI TAMURA; SHUJI KANEKO; MASAMICHI SATOH; HIROSHI TAKAGI

doi:10.1248/cpb.35.2561

Studies on Peptides. CL. Syntheses of [D-His²] -Analogs of Enkephalin and Adrenorphin and Several [D-Arg²] enkephalin Analogs

SUSUMU FUNAKOSHI, MINORU KUBOTA, NAOTO KOSUGA, JIAN-PING XU, HARUAKI YAJIMA, WEI LI, SHIGEKI TAMURA, SHUJI KANEKO, MASAMICHI SATOH, HIROSHI TAKAGI

Author information

SUSUMU FUNAKOSHI
Faculty of Pharmaceutical Sciences, Kyoto University
MINORU KUBOTA
Central Research Institute, Daiichi Seiyaku Co., Ltd.
NAOTO KOSUGA
Faculty of Pharmaceutical Sciences, Kyoto University
JIAN-PING XU
Faculty of Pharmaceutical Sciences, Kyoto University
HARUAKI YAJIMA
Faculty of Pharmaceutical Sciences, Kyoto University
WEI LI
Department of Molecular Biology, Jilin University
SHIGEKI TAMURA
Faculty of Pharmaceutical Sciences, Kyoto University
SHUJI KANEKO
Faculty of Pharmaceutical Sciences, Kyoto University
MASAMICHI SATOH
Faculty of Pharmaceutical Sciences, Kyoto University
HIROSHI TAKAGI
Faculty of Pharmaceutical Sciences, Kyoto University

Keywords: [D-His²] enkephalin, [D-His²] adrenorphin, [D-Arg2] enkephalin analog, μ receptor, guinea-pig ileum assay, trifluoromethanesulfonic acid deprotection, methanesulfonic acid deprotection

JOURNAL FREE ACCESS

1987 Volume 35 Issue 6 Pages 2561-2568

DOI https://doi.org/10.1248/cpb.35.2561

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Abstract

[D-His²] Leu-enkephalin and [D-His²] adrenorphin were synthesized. In addition, eight [D-Arg²] enkephalin-related peptides were synthesized. Their inhibitory effects on electrically stimulated myenteric plexus-longitudinal muscle preparations of guinea-pig ileum were examined.

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