Reduction of mitomycin C is catalysed by human recombinant NRH:quinone oxidoreductase 2 using reduced nicotinamide adenine dinucleotide as an electron donating co-factor.

NRH:Quinone Oxidoreductase 2 (NQO2) has been described as having no enzymatic activity with nicotinamide adenine dinucleotide (NADH) or NADPH as electron donating cosubstrates. Mitomycin C (MMC) is both a substrate for and a mechanistic inhibitor of the NQO2 homologue NQO1. NRH:quinone oxidoreductase 2 catalysed the reduction of MMC at pH 5.

Impact of biological and economic variables on optimal parity for replacement in swine breed-to-wean herds.

Voluntary and involuntary culling practices determine the average parity when sows are replaced in a herd. Underlying these practices is the economic effect of replacing a sow at different parities. A dynamic programming model was used to find the optimal parity and net present value in breed-to-wean swine herds.

A store-operated Ca(2+) influx pathway in the bag cell neurons of Aplysia.

Although store-operated Ca(2+) influx has been well-studied in nonneuronal cells, an understanding of its nature in neurons remains poor. In the bag cell neurons of Aplysia californica, prior work has suggested that a Ca(2+) entry pathway can be activated by Ca(2+) store depletion. Using fura-based imaging of intracellular Ca(2+) in cultured bag cell neurons, we now characterize this pathway as store-operated Ca(2+) influx.

NRH:quinone oxidoreductase 2 (NQO2) catalyzes metabolic activation of quinones and anti-tumor drugs.

NRH:quinone oxidoreductase 2 (NQO2) is a cytosolic flavoprotein that utilizes NRH as electron donor. The present studies investigate the role of NQO2 in metabolic detoxification/activation of quinones and quinone based anti-tumor drugs. Chinese hamster ovary (CHO) cells stably overexpressing cDNA derived mouse NQO2 and mouse keratinocytes from DMBA-induced skin tumors in wild-type and NQO2-null mice were generated.

Evaluation of methodology for administration of porcine FSH for use in estrus induction and for increasing ovulation rate in prepubertal gilts.

Ovulation rate influences production efficiency of oocytes and embryos and depends upon the amount of gonadotropin administered and the ratio of FSH:LH activity. In Experiment 1, gilts (n=135) were assigned to receive 10 or 15 Armour units (AU) of porcine FSH containing 6%, 10%, or 15% LH, whereas controls received PG600. Gilts received 1/6th the FSH dose in six sc administrations at 8-h intervals.

Effect of altering dose of PG600 on reproductive performance responses in prepubertal gilts and weaned sows.

This study evaluated the effects of altering dose of PG600 on estrus and ovulation responses in prepubertal gilts and weaned sows. Experiment 1 tested the effects of one (1.0x, 400IU eCG+200IU hCG, n=74), one and a half (1.

Field demonstration of surfactant-enhanced solubilization of DNAPL at Dover Air Force Base, Delaware.

This study reports on a surfactant-based flood for tetrachloroethylene (PCE) removal from a control test cell at the Dover National Test Site. The surfactant formulation (sodium dihexyl sulfosuccinate (Aerosol-MA or AMA), isopropanol and calcium chloride) was able to achieve a high concentration of PCE in swollen micelles (supersolubilization) without vertical PCE migration. The hydraulic system included eight screened wells that were operated in both vertical circulation and line drive configurations.

Design of aquifer remediation systems: (2) estimating site-specific performance and benefits of partial source removal.

A Lagrangian stochastic model is proposed as a tool that can be utilized in forecasting remedial performance and estimating the benefits (in terms of flux and mass reduction) derived from a source zone remedial effort. The stochastic functional relationships that describe the hydraulic "structure" and non-aqueous phase liquid (NAPL) "architecture" have been described in a companion paper (Enfield, C.G.

Effect of PG600 and adjusted mating times on reproductive performance in weaned sows.

The administration of PG600 to sows at weaning induces >90% of sows to return to estrus within a week, but farrowing rate and litter size are often not improved. This study evaluated the effects of adjusted artificial insemination (AI) times based on weaning to estrus interval (WEI) and estrus to ovulation interval (EOI) following PG600. All sows were given PG600 at weaning and allotted to adjusted (ADJ, n=47) or non-adjusted (NA, n=46) mating times after the onset of estrus.

Recruitment and selection of ovarian follicles for determination of ovulation rate in the pig.

Gonadotropins determine the follicle selection and ovulation rate. Follicle growth is independent of gonadotropins until antrum formation, at which time recruitment occurs. Once recruited, follicles will continue to grow or degenerate.

Targeting enzymes to cancers--new developments.

Two methods of using tumour located enzymes have been described. These are antibody directed enzyme prodrug therapy (ADEPT) and macromolecule directed enzyme prodrug therapy (MDEPT), where the tumour located enzyme converts a non-toxic prodrug into a cytotoxic drug at tumour sites. The alternative use of tumour located enzymes is to inactivate rescue agents that protect cells from antimetabolite action, and is described as 'Antimetabolite with inactivation of rescue agent at cancer sites' (AMIRACS).

Effect of age and physical or fence-line boar exposure on estrus and ovulation response in prepubertal gilts administered PG600.

Boar exposure has been used for estrus induction of prepubertal gilts, but has limited effect on estrus synchronization within 7 d of introduction. In contrast, PG600 (400 IU of PMSG and 200 IU of hCG; Intervet, Millsboro, DE) is effective for induction of synchronized estrus, but the response is often variable. It is unknown whether boar exposure before PG600 administration might improve the efficiency of estrus induction of prepubertal gilts.

A thallium-sensitive, fluorescence-based assay for detecting and characterizing potassium channel modulators in mammalian cells.

Potassium channels have been identified as targets for a large number of therapeutic indications. The ability to use a high-throughput functional assay for the detection and characterization of small-molecule modulators of potassium channels is very desirable. However, present techniques capable of screening very large chemical libraries are limited in terms of data quality, temporal resolution, ease of use, and requirements for specialized instrumentation.

BL-1249 [(5,6,7,8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine]: a putative potassium channel opener with bladder-relaxant properties.

BL-1249 [(5,6,7,8-tetrahydro-naphthalen-1-yl)-[2-(1H-tetrazol-5-yl)-phenyl]-amine] produced a concentration-dependent membrane hyperpolarization of cultured human bladder myocytes, assessed as either a reduction in fluorescence of the voltage-sensitive dye bis-(1,2-dibutylbarbituric acid)trimethine oxonol (EC50 = 1.26 +/- 0.6 microM) or by direct electrophysiological measurement (EC50 = 1.

(S,E)-N-[1-(3-heteroarylphenyl)ethyl]-3-(2-fluorophenyl)acrylamides: synthesis and KCNQ2 potassium channel opener activity.

Replacement of the morpholinyl moiety in (S,E)-N-[1-(3-morpholinophenyl)ethyl]-3-phenylacrylamide (1) with heteroaryl groups led to the identification of (S,E)-N-1-[3-(6-fluoropyridin-3-yl)phenyl]ethyl-3-(2-fluorophenyl)acrylamide (5) as a potent KCNQ2 potassium channel opener. Among this series of heteroaryl substituted acrylamides, (S,E)-N-1-[3-(1H-pyrazol-1-yl)phenyl]ethyl-3-(2-fluorophenyl)acrylamide (9) exhibits balanced potency and efficacy. The syntheses and the KCNQ2 opener activity of this series of acrylamides are described.

Effect of housing system and boar exposure on estrus expression in weaned sows.

Reproductive efficiency depends on detection of estrus, which may be influenced by housing and boar exposure. This experiment investigated the effects of housing system and boar contact on measures of estrus in weaned sows. Mixed-parity sows were randomly assigned to be weaned into gestation crates away from boars (AWC, n = 45), into pens away from boars (AWP, n = 42), or into pens adjacent to a mature boar (ADJ, n = 46).

Synthesis and KCNQ2 opener activity of N-(1-benzo[1,3]dioxol-5-yl-ethyl, N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl, and N-[1-(2,3-dihydro-1H-indol-5-yl)-ethyl acrylamides.

Bioisosteric replacement studies led to the identification of N-(1-benzo[1,3]dioxol-5-yl-ethyl)-3-(2-chloro-phenyl)-acrylamide ((S)-3) as a highly potent KCNQ2 opener, and 3-(2,6-difluoro-phenyl)-N-[1-(2,3-dihydro-benzofuran-5-yl)-ethyl]-acrylamide ((S)-4), and N-[1-(2,3-dihydro-1H-indol-5-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide ((S)-5) as highly efficacious KCNQ2 openers. In contrast, their respective R enantiomers showed significantly less or no appreciable KCNQ2 opener activity even at the highest concentration tested (10 microM). Because of its high potency and moderate efficacy as well as its convenient synthesis, (+/-)-3 was selected as a reference compound for analyzing efficacies of KCNQ openers in electrophysiology studies.

Activation of a calcium entry pathway by sodium pyrithione in the bag cell neurons of Aplysia.

The ability of sodium pyrithione (NaP), an agent that produces delayed neuropathy in some species, to alter neuronal physiology was accessed using ratiometric imaging of cytosolic free Ca(2+) concentration ([Ca(2+)](i)) in fura PE-filled cultured Aplysia bag cell neurons. Bath-application of NaP evoked a [Ca(2+)](i) elevation in both somata and neurites with an EC(50) of approximately 300 nM and a Hill coefficient of approximately 1. The response required the presence of external Ca(2+), had an onset of 3-5 min, and generally reached a maximum within 30 min.

Improving the extraction of tetrachloroethylene from soil columns using surfactant gradient systems.

In this work, we extend the recently developed gradient approach for surfactant-enhanced remediation of dense non-aqueous phase liquid (DNAPL)-impacted sites. The goal of the gradient approach is to maximize the DNAPL solubilization capacity in swollen micelles (Type I aqueous microemulsions) while at the same time minimizing the potential for DNAPL mobilization. In this work, we introduce a modified version of the capillary/trapping curve that we refer to as the gradient curve to help interpret and/or design the gradient approach.

(S)-N-[1-(4-cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide is a potent and efficacious KCNQ2 opener which inhibits induced hyperexcitability of rat hippocampal neurons.

(S)-N-[1-(4-Cyclopropylmethyl-3,4-dihydro-2H-benzo[1,4]oxazin-6-yl)-ethyl]-3-(2-fluoro-phenyl)-acrylamide ((S)-2) was identified as a potent and efficacious KCNQ2 opener. This compound demonstrated significant activity in reducing neuronal hyperexcitability in rat hippocampal slices, and the inhibition mediated by (S)-2 was reversed by the KCNQ blocker linopirdine.

Effect of estrogen formulation and its site of deposition on serum PGFM concentrations, uterine contractility, and time of ovulation in artificially inseminated weaned sows.

At the time of artificial insemination, 48 mixed parity sows were assigned by parity to receive 25 microg estradiol-17beta either in oil deposited onto the vaginal mucosa (E-oil), or dissolved in extended semen (E-semen), or received no estrogen and served as controls. All sows were inseminated transcervically 24 h after detection of estrus. The time of ovulation was determined in 15 sows per treatment by transrectal ultrasonography.

Bioeconomic evaluation of sow longevity and profitability.

Sow production indicators, including litter size, litter weight, and the length of time that sows remained in the herd (sow longevity), were used to characterize sow performance and profitability. Sow longevity and production records from 148,568 sows in 32 commercial herds from Central Illinois from January 1995 to May 2001 were analyzed using survival and repeatability models, respectively. The factors studied included sow genetics (32 genetic lines), with eight major lines present in multiple herds, and the combination of herd and year of entry in the herd.