2011
DOI: 10.1111/j.1369-1600.2010.00298.x View full text |Buy / Rent full text
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Abstract: High blood-brain permeability and effective delivery of morphine to the brain have been considered as explanations for the high potency of heroin. Results from Andersen et al. indicate that 6-monoacetylmorphine (6-MAM), and not morphine, is the active metabolite responsible for the acute effects observed for heroin. Here, we use pharmacokinetic modeling on data from the aforementioned study to calculate parameters of the distribution of heroin, 6-MAM and morphine in blood and brain tissue after subcutaneous he… Show more

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“…Moreover, the maximal increase in the NAc-Muscle differential was at ~20 min, the time interval when locomotor hypoactivity is inverted into hyperactivity. Interestingly, at this time the levels of the primary heroin metabolite (6-MAM), which has high affinity to μ-opioid receptors (Boix et al, 2013; Gottas et al, 2013), are on descending curve after their peaks at ~5 min but levels of morphine, another heroin’s metabolite, are at their peaks (Gottas et al, 2013). …”
Section: Discussionmentioning
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“…Moreover, the maximal increase in the NAc-Muscle differential was at ~20 min, the time interval when locomotor hypoactivity is inverted into hyperactivity. Interestingly, at this time the levels of the primary heroin metabolite (6-MAM), which has high affinity to μ-opioid receptors (Boix et al, 2013; Gottas et al, 2013), are on descending curve after their peaks at ~5 min but levels of morphine, another heroin’s metabolite, are at their peaks (Gottas et al, 2013). …”
Section: Discussionmentioning
“…This decrease in HDAC expression was accompanied by increased acetylation of H4, and altered emotional phenotypes and responsivity to an antidepressant. Other labs have also demonstrated a relationship between ELS and HDAC expression (Tesone-Coelho et al, 2013). Additionally, ELS decreased nucleus accumbens DNMT expression rates, which were associated with hyper-methylation of neuronal plasticity genes (Anier et al, 2013).…”
Section: Els and Epigenetic Effectsmentioning
“…There are major differences in the presence of heroin-metabolizing enzymes in human and rodent blood (Berry et al, 2009;Bahar et al, 2012), which may complicate the extrapolation of opioid metabolism data across species. Despite these differences, the in vivo half-lives of heroin in rodents and humans have been shown to be remarkably similar (t 1/2 ∼2.5-4 minutes) (Way et al, 1960;Rook et al, 2006b;Boix et al, 2013;Gottas et al, 2013;Raleigh et al, 2013). Fig.…”
Section: An Antibody Against 6-mam Impairs Heroin Effectsmentioning