Title of article
Rational drug design and synthesis of a selective ε opioid receptor antagonist on the basis of the accessory site concept
Author/Authors
Hideaki Fujii، نويسنده , , Minoru Narita، نويسنده , , Hirokazu Mizoguchi، نويسنده , , Junichi Hirokawa، نويسنده , , Koji Kawai، نويسنده , , Toshiaki Tanaka، نويسنده , , Leon F Tseng، نويسنده , , Hiroshi Nagase، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
3
From page
4241
To page
4243
Abstract
To newly synthesize a selective ε opioid receptor antagonist, 17-(cyclopropylmethyl)-4,5α-epoxy-6β,21-epoxymethano-3-hydroxy-6,14-endoethenomorphinan-7α-(N-phenethyl)carboxamide was first designed from an ε opioid receptor agonist TAN-821 on the basis of the accessory site concept. The designed compound antagonized the agonistic effects induced by an ε opioid receptor agonist β-endorphin on the rat vas deference test. Moreover, the designed compound blocked the antinociception induced by β-endorphin given intracerebroventricularly.
Keywords
Putative e opioid receptor , e Opioid receptor antagonist , Accessory site.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794770
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