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- W2000990574 abstract "Brain levels of Δ1-tetrahydrocannabinol (Δ1-THC) and its major metabolite (7-hydroxy-Δ1-THC) following intravenous injection of tritium-labelled Δ1-THC into mice were measured and correlated with inhibition of spontaneous motor activity. Metabolism of Δ1-THC to 7-hydroxy-Δ1-THC was fast and both substances rapidly penetrated the C.N.S. Peak brain levels of both compounds occurred within 20 min of injection and the correlation between pharmacological response and brain concentration of either compound was equally good. Twenty min after injection more than 50 per cent of the radioactivity in blood was irreversibly bound, whereas only 12 per cent of the activity in brain was unextractable. SKF 525A (25 mg/kg i.p.) produced only a slight increase in the brain level of Δ1-THC but the level of 7-hydroxy-Δ1-THC was increased nearly three-fold, presumably due to the inhibition of subsequent metabolic reactions. Piperonyl butoxide (100 mg/kg i.p.) produced an increase in the brain level of Δ1-THC but no change in the level of 7-hydroxy-Δ1-THC. Higher doses of either inhibitor produced behavioural changes in the absence of Δ1-THC. It is concluded that 7-hydroxy-Δ1-THC is centrally active, but that it has not yet been demonstrated that the effects of injected Δ1-THC are due solely to its primary metabolite." @default.
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- W2000990574 title "Brain levels of Δ1-tetrahydrocannabinol and its metabolites in mice—correlation with behaviour, and the effect of the metabolic inhibitors SKF 525A and piperonyl butoxide" @default.
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- W2000990574 doi "https://doi.org/10.1016/0006-2952(72)90039-1" @default.
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