Dihydromorphinones, antagonists

Since a nitro substituent is more electron-withdrawing than a chloro substituent, it was anticipated by Archer and his colleagues that replacing the p-chloro atom on the cinnamoylamino moiety with a p-nitro group would make the cinnamoylamino function a better Michael acceptor [106]. 5/ -Methyl-14/ -(4-nitrocinnamoylamino)-7,8-dihydromorphinone (MET-CAMO, 55) was found to be an irreversible fi selective antagonist, MET-... [Pg.101]

Kotick s group have studied a number of dihydromorphinone derivatives (3) with N-CPM and N-CBM substituents.(32,33) The parent compounds have dual actions, the CPM member being the more potent antagonist and the CBM... [Pg.411]

Pasternak GW, Hahn EF (1980) Long-acting opiate agonists and antagonists 14-hydroxy-dihydromorphinone hydrazones. J Med Chem 23 674-676... [Pg.88]

Jiang Q, Sebastian A, ArcherS, Bidlack JM (1994) 5P-Methyl-14P-(p-nitrocinnamoylamino)-7,8-dihydromorphinone and its corresponding N-cyclopropylmethyl analogue, N-cyclopro-pylmethylnor-5 P-methyl-14P-(p-nitrocinnamoylamino)-7,8-dihydromorphinone mu selective irreversible opioid antagonists. J Pharmacol Exp Ther 268 1107-1113... [Pg.118]

FIGURE 1.7 (a) Dihydromorphinone is more potent than morphine but is equally efficacious, (b) Propranolol is a competitive antagonist at adrenergic receptors. [Pg.9]

Analgesic narcotic antagonists. 1. 8.beta.-Alkyl-, 8.beta.-acyl-, and 8.beta.-(tertiary alcohol)dihydrocodeinones and-dihydromorphinones... [Pg.139]

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