<Regular article>Opioid Receptor Affinities of Tyrosine ω-Phenylalkyl Esters, Simple Enkephalin Pharmacophore-mimics.

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概要

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• In order to substantiate the hypothesis that the μ-, δ-, or κ-opioid receptor Affinity of opioid peptides can be elicited by an amino-terminus tyrosine residue and the 4th phenylalanine aromatic ring lying in the proper spatial disposition, a series of simple peptide-mimic tyrosine esters, in which tyrosine is linked to aromatic ring separated by a variety of methylene spacers, were prepared and evaluated by in vitro radioligand receptor assay. Compounds having the 6 or 7 methylene spacers were more potent in opioid receptor affinity than those having fewer or more methylene spacers. The N-monomethyl- and N, N-dimethyltyrosine congeners were more potent than the corresponding tyrosine esters. The order of the receptor type selectivity of these compounds was μ>>δ>κ.

• 岐阜薬科大学の論文
• 1997-06-30

著者

• Iwama Tetsuo

  Gifu Pharmaceutical University

• Iwamura T

  Gifu Pharmaceutical Univ. Gifu Jpn

• Niwa Masayuki

  岐阜大学医学部

• IWAMURA TATSUNORI

  岐阜薬科大学

• TSUTSUI HISAYOSHI

  岐阜薬科大学

• KATAOKA TADASHI

  岐阜薬科大学

• HORI MIKIO

  岐阜女子大学

• NOZAKI MASAKATSU

  岐阜大学医学部

• Tsutsui H

  Kumamoto Univ. Kumamoto Jpn

• Nozaki Masakatsu

  Department Of Pharmacology Gifu University School Of Medicine

• Hori M

  Gifu Pharmaceutical Univ. Gifu Jpn

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