Affinity profiles of morphine, codeine, dihydrocodeine and their glucuronides at opioid receptor subtypes.

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Mignat C, Wille U, Ziegler A

Affinity profiles of morphine, codeine, dihydrocodeine and their glucuronides at opioid receptor subtypes.

Life Sci. 1995;56(10):793-9.

PubMed ID

7885194 [ View in PubMed

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Abstract

The affinity of morphine, codeine, dihydrocodeine and their glucuronides for mu-, delta-, and kappa-opioid receptors was investigated. Binding was studied on guinea-pig brain homogenates with [3H]DAMGO, [3H]DPDPE, and [3H]U69593. The substitution of the free phenolic group of morphine caused a decrease in binding at opioid receptors without affecting the mu/delta-ratio nor that of mu/kappa. Glucuronidation of the 6-hydroxyl group of morphine, codeine or dihydrocodeine did not affect the affinity to mu-receptors, slightly increased the affinity for delta-receptors and reduced the affinity for kappa-receptors. The 6-glucuronides possess a decreased selectivity for mu-receptors over delta-receptors whereas that for mu- over kappa-receptors was increased. It is concluded that chemical variations at 3- and 6-position of morphine independently affect the affinity to opioid receptor subtypes.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Codeine	Delta-type opioid receptor	Protein	Humans	Yes	Agonist	Details
Codeine	Kappa-type opioid receptor	Protein	Humans	Yes	Agonist	Details