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note
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Minimizations and energy calculations were carried out using MedChem Explorer (Accelerys) using a CFF force field.
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27444438090
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note
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3H] oxytocin was made up in buffer containing 100 mg/mL HSA. HSA was obtained from Sigma (Poole, Dorset, U.K.).
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28
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27444447980
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note
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50 is the serum concentration for 50% inhibition of uterine contractility response to oxytocin in an OT induced rat uterus contraction model (see ref 15).
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29
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27444439651
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note
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-1 i.v.) 18 h after pretreatment with diethylstilbestrol (250 ug/kg ip). Arterial blood pressure was recorded from a femoral artery. The left uterine horn was anchored in the abdominal cavity at the ovarian end, and uterine contractility was recorded via a ligature tied approximately 2 cm distally and connected to a strain gauge under 1-2 g resting tension. Two consecutive two-point dose-response curves to either iv OT were constructed and uterine contractile responses quantified by recording the area under the contractile response for the 10 min period immediately postdose. Cumulative doses of antagonist or vehicle were then injected iv, and oxytocin dose-response curves were repeated 15 min later. Dose ratios were calculated for each dose of antagonist by comparison with the second agonist dose-response curve and the DR10 (antagonist dose required to shift the agonist dose-response curve 10-fold), calculated by linear interpolation of log-(DR-1) plotted against dose (mg/kg).
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Stereoselective benzylic hydroxylation of 2-substituted indanes using toluene dioxygenase as biocatalyst
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