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1: Life Sci. 1987 Dec 28;41(26):2845-9.
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Morphine-6-glucuronide, a potent mu agonist.

Pasternak GW, Bodnar RJ, Clark JA, Inturrisi CE.

Cotzias Laboratory of Neuro-Oncology, Memorial Sloan-Kettering Cancer Center, New York, NY.

The 3- and the 6-glucuronides of morphine have been examined in binding studies and in vivo. The 3-glucuronide had poor affinity in all binding studies whereas the 6-glucuronide potently labeled mu, but not delta or kappa receptors with affinities similar to morphine. Microinjections of the 3-glucuronide directly into the periaqueductal gray were without effect. The 6-glucuronide, on the other hand, was up to 20-fold more potent than morphine following microinjections in the same region. High doses of the 6-glucuronide produced profound seizure activity. All 6-glucuronide actions were sensitive to the opiate antagonist naloxone.

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PMID: 2826951 [PubMed - indexed for MEDLINE]