Synthesis of Carboxyl-Terminal Extension Analogs of Dermorphin and Evaluation of Their Opioid Receptor-Binding and Opioid Activities

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概要

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• Eight dermophin (DM) analogs extended at the C-terminus, based on the sequence of prepro-DM deduced from the cDNA, were synthesized by a simultaneous solid-phase method in which a pair of peptides was synthesized in a single vessel. Six peptides (three pairs) were obtained in satisfactory yields (17-37%). In the opioid receptor-binding assay using a rat brain homogenate, the μ-affinities correlated well to the net positive charges of peptides, and DM-Gly-Glu-Ala-Lys-Lys-Ile-Lys-Arg-NH_2 showed the highest μ-affinity, 115-fold that of DM. But, in the guinea pig ileum assay, extension analogs with net positive charge of 2 to 4 exhibited potencies comparable to or slightly lower than that of DM, even though they possessed 2- to 115-fold higher μ-affinities than DM in the receptor-binding assay.

• 社団法人日本薬学会の論文
• 1994-04-15

著者

• 鈴木 謙次

  東北薬科大学

• 安保 明博

  Tohoku College of Pharmacy

• 佐々木 有亮

  Tohoku College of Pharmacy

• 鈴木 謙次

  Tohoku College of Pharmacy

関連論文

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