Donald B. Bennett

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Many 3-aryl-4-(1,2,3,4-tetrahydro[1,4]diazepino[6,7,1-hi]indol-7-yl)maleimides exhibit potent GSK3 inhibitory activity (<100 nM IC(50)), although few show significant selectivity (>100x) versus CDK2, CDK4, or PKCbetaII. However, combining 3-(imidazo[1,2-a]pyridin-3-yl), 3-(pyrazolo[1,5-a]pyridin-3-yl) or aza-analogs with a(More)
To gauge the experimental variability associated with Biacore analysis, 36 different investigators analyzed a small molecule/enzyme interaction under similar conditions. Acetazolamide (222 g/mol) binding to carbonic anhydrase II (CAII; 30000 Da) was chosen as a model system. Both reagents were stable and their interaction posed a challenge to measure(More)
Pulmonary delivery of the decapeptide detirelix was studied in briefly anesthetized dogs and the pharmacokinetics were examined following intravenous administration, intratracheal instillation, and aerosol inhalation. Detirelix administrations to the lung gave plasma profiles that were extended over two days, and that differed markedly from those of(More)
Prazosin, an antihypertensive drug with postsynaptic alpha 1-adrenergic blocking activity, has been coupled to poly-N5-(3-hydroxypropyl-L-glutamine) (PHPG) via a carbamate linkage. PHPG was activated by p-nitrophenyl chloroformate and then reacted with prazosin to form p(HPG-prazosin carbamate) conjugate. Drug loading was 23.9% (w/w). Activated polymer and(More)
The unanesthetized awake sheep was employed as large animal model for the determination of bioavailability and pharmacokinetics following the pulmonary instillation of the decapeptide detirelix. After intratracheal administration of a 80 micrograms/kg dose, the average t1/2 of elimination was 9.8 +/- 1.3 hours (n = 5) which was similar to the elimination(More)
The narcotic antagonist naltrexone (I) was modified at the 3 and 14 hydroxyl positions and covalently coupled to a biodegradable poly(alpha-amino acid) backbone through a labile bond. Selective acetylation of I with acetic anhydride gave naltrexone-3-acetate (II), which was subsequently succinoylated to naltrexone-3-acetate-14-hemisuccinate (III) with(More)
The concentrations of 210Pb and its states of equilibrium with 238U, 234U and 230Th in U miners' lungs obtained at autopsy are reported. The concentration of 210Pb ranged from 0.63 to 123 Bq/kg wet weight with an average of 32.7 Bq/kg. The 210Pb concentrations were almost seven times higher than the concentrations of 238U, 234U and 230Th. The radiation dose(More)
Argonne National Laboratory (ANL) exhumed the remains of two individuals who had received Pu by intravenous injection, performed Pu analysis on these remains, and then sent portions of individual bones to our laboratory. We analyzed these bone samples to determine the macro-distribution of naturally occurring alpha-emitting isotopes of U (234U and 238U). We(More)
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