Rational drug design and synthesis of a selective opioid receptor antagonist on the basis of the accessory site concept |
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Authors: | Fujii Hideaki Narita Minoru Mizoguchi Hirokazu Hirokawa Junichi Kawai Koji Tanaka Toshiaki Tseng Leon F Nagase Hiroshi |
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Affiliation: | Pharmaceutical Research Laboratories, Toray Industries, Inc., 1111, Tebiro, Kamakura Kanagawa 248-8555, Japan. hideaki_fujii@nts.toray.co.jp |
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Abstract: | To newly synthesize a selective opioid receptor antagonist, 17-(cyclopropylmethyl)-4,5 alpha-epoxy-6 beta,21-epoxymethano-3-hydroxy-6,14-endoethenomorphinan-7 alpha-(N-phenethyl)carboxamide was first designed from an opioid receptor agonist TAN-821 on the basis of the accessory site concept. The designed compound antagonized the agonistic effects induced by an opioid receptor agonist beta-endorphin on the rat vas deference test. Moreover, the designed compound blocked the antinociception induced by beta-endorphin given intracerebroventricularly. |
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