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Evidence from opiate binding studies that heroin acts through its metabolites.
The relative affinity to opiate receptors of heroin, 6-acetylmorphine and morphine was estimated by determining their ability to displace specifically bound 3H-naltrexone from rat brain opiate binding sites. In vitro hydrolysis of heroin to 6-acetylmorphine was monitored in the binding assay filtrate by use of a quantitative HPLC procedure. The rate of heroin hydrolysis was significantly slower at 0 degrees C than at 37 degrees C. The displacement of 1 nM 3H-naltrexone by unlabeled ligand at concentrations ranging from 7 to 500 nM was measured at 0 degrees C for 120 minutes, yielding IC50 values of heroin = 483 nM, 6-acetylmorphine = 73 nM and morphine = 53 nM. When the binding data for heroin were recalculated to include the displacement that could be attributed to the 6-acetylmorphine derived from heroin degradation during the incubation, all of the apparent heroin binding was accounted for by the 6-acetylmorphine. These results are consistent with previous reports of the low binding affinity of morphine congeners (e.g., codeine) that lack a free phenolic 3-hydroxyl group and support the view that heroin is a prodrug which serves to determine the distribution of its intrinsically active metabolites, 6-acetylmorphine and morphine.
PMID: 6319928 [PubMed - indexed for MEDLINE]
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Cited by 3 PubMed Central articles
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Characterizing exons 11 and 1 promoters of the mu opioid receptor (Oprm) gene in transgenic mice.
Xu J, Xu M, Pan YX.
BMC Mol Biol. 2006 Nov 13; 7:41. Epub 2006 Nov 13.
[BMC Mol Biol. 2006]
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Morphine kinetics after diamorphine infusion in premature neonates.
Barrett DA, Elias-Jones AC, Rutter N, Shaw PN, Davis SS.
Br J Clin Pharmacol. 1991 Jul; 32(1):31-7.
[Br J Clin Pharmacol. 1991]
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Diamorphine infusion in the preterm neonate.
Elias-Jones AC, Barrett DA, Rutter N, Shaw PN, Davis SS.
Arch Dis Child. 1991 Oct; 66(10 Spec No):1155-7.
[Arch Dis Child. 1991]
Patient Drug Information
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Codeine (Brontex® , Capital and Codeine® , Cheracol® with Codeine Syrup, ...)
Codeine is used to relieve mild to moderate pain. It is also used, usually in combination with other medications, to reduce coughing. Combination products that contain codeine and promethazine should not be used in child...
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