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The uptake of [3H]flunitrazepam ([3H]FLTZ), [3H]diazepam ([3H]DZP) and [3H]muscimol ([3H]MUS) was studied in isolated interstitial cells from adult rat testis. Uptake of [3H]FLTZ, [3H]DZP, and [3H]MUS was temperature dependent, saturable and inhibited by various organic anions, suggesting that the uptake is mediated by active transport mechanisms. The apparent Km for [3H]FLTZ and [3H]DZP was 0.15 mumol/l and 0.20 mumol/l, and the Vmax at 10 min was 2.4 pmol/h/10(6) cells and 2.2 pmol/h/10(6) cells, respectively. Initial uptake rates of [3H]FLTZ and [3H]DZP were greater than that of [3H]MUS. Higher concentrations of the three ligands caused a marked reduction in the initial uptake rate of the three ligands. Intracellular accumulation of ligands was demonstrated with [3H]DZP, showing the highest accumulation at the 20-min time point. The predominant distribution was to the nuclear fraction at the 1- and 2-h time points. Accumulation of [3H]FLTZ and [3H]MUS was predominantly to the mitochondrial fraction at the 1-h time point, while the accumulation of [3H]DZP was predominantly to the nuclear fraction, with a low amount of the ligand found in the mitochondrial fraction. None of the ligands displayed significant photolabile effects. These results are in agreement with the reported distribution of benzodiazepine receptor subtypes in rat testis. The [3H]DZP uptake rate in testicular interstitial cells is greater than that in rat cerebral cortex.An article published by Austin Business Journal earlier this year addressed the notion of the ‘affordable luxury’
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