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Biomedical subjects

G Brown

Publications and source records attributed to G Brown.

At least 163 records · Page 9Linked to original sources

RX871024 induces Ca2+ mobilization from thapsigargin-sensitive stores in mouse pancreatic beta-cells.

The effects of RX871024, a compound with an imidazoline structure, on cytoplasmic-free Ca2+ concentration ([Ca2+]i) in mouse pancreatic beta-cells were studied. RX871024 modulates [Ca2+]i by at least two mechanisms. One mechanism involves closure of ATP-regulated K+ channels, resulting in membrane depolarization, opening of voltage-gated L-type Ca2+ channels, and a subsequent increase in [Ca2+]i. Another mechanism, reported here for the first time, deals with RX871024-induced mobilization of Ca2+ from nonmitochondrial thapsigargin-sensitive intracellular stores. Reduced glutathione, inhibitors of cytochrome P-450, and monoaminooxidases A and B blocked this Ca2+ mobilization. It is concluded that the mechanism of RX871024-induced Ca2+ mobilization from intracellular stores involves changes in the oxidation/reduction state of the pancreatic beta-cell and may be controlled by cytochrome P-450.

Adenosine Triphosphate↗

Effects of repeated withdrawal from chronic ethanol on oral self-administration of ethanol on a progressive ratio schedule.

Male hooded Lister rats were trained using a sucrose-fading technique, to perform an operant lever press response to obtain ethanol. Initial training, using an FR4 schedule in which each reinforcement required four lever presses, included varying the concentration of ethanol in the liquid reinforcer. Changes in reinforcer concentration between 7 and 15% (vol/vol) had little effect on either numbers of lever pressing responses, or reinforcers obtained during the 3h session. Increasing the reinforcer concentration to 20% caused a decline in responding. The effects of varying reinforcer concentration (0-20% ethanol) were also studied in the same animals performing a progressive ratio schedule, in which the number of responses required to obtain a reinforcer was successively increased during the session. In these experiments the point at which rats ceased to respond (breaking point) was taken as a measure of their motivation to obtain ethanol. The function describing the relationship between ethanol concentration and number of responses, and number of reinforcers obtained in a session was an inverted U, with the maximum values occurring at an ethanol concentration of 10%. The value of the breaking point (highest ratio achieved) depended on the criterion used to define cessation of responding, but was between 15 and 22. Rats performing for ethanol showed higher breaking points than when responding for water, but there was no statistically reliable effect of ethanol concentration on the breaking point parameter. The effects of feeding the rats a liquid diet containing ethanol, and its subsequent withdrawal, on progressive ratio responding for 5% ethanol, were studied over four cycles of exposure and withdrawal. Intakes of ethanol of 11 g/kg/day had no effect on the animals' breaking point on the progressive ratio schedule, but withdrawal from the ethanol diet resulted in breaking points significantly higher than those in a control group pair-fed a nutritionally equivalent, ethanol-free diet. Although there was no further effect of repeated exposure and withdrawal on responding during the acute withdrawal phase, baseline levels of responding were elevated in the animals which had received multiple cycles of ethanol diet and withdrawal. These results are discussed in the context of the consequences of sensitization to repeated withdrawal from ethanol in dependent animals and humans.

Administration, Oral↗

An assessment of a sedative algorithm for sleep in an intensive care unit.

The difficulty for intensive care unit (ICU) patients to obtain frequent and extensive sleep has been well-documented. This project assessed the benefit of an algorithm of pharmacological assistance (lorazepam and methotrimeprazine) on sedation level and sleep duration in the ICU. The setting was a 15-bed closed ICU dealing with medical and surgical patients in a tertiary care, teaching hospital. Desired and actual levels of sedation for individual patients were determined hourly by the bedside nurse. Medications could be administered to facilitate achieving the desired level of sedation. Our results should no difference occurred in the achievement of the target sedation or duration of sleep with the implementation of the sedation algorithm. The amount of additional medication required during the night did change with the implementation of the sedation algorithm. A reduction in the amount of diazepam, morphine, and additional methotrimeprazine was noted. Efforts to change nursing practice will be required to improve the quality and quantity of sleep in ICU patients. This clinical evaluation demonstrates that the implementation of an algorithm for medication use is not effective alone in obtaining the desired level and duration of sleep in ICU patients. Nursing practice should continue to look at non-pharmacological factors, such as environmental noise, patient interruptions, and patient care practice to determine strategies in addition to medications which would aid the critically ill patient in achieving adequate sleep.

Algorithms↗

Upgrading clinical decision support with published evidence: what can make the biggest difference?

BACKGROUND: To enhance clinical decision support, presented messages are increasingly supplemented with information from the medical literature. The goal of this study was to identify types of evidence that can lead to the biggest difference. METHODS: Seven versions of a questionnaire were mailed to randomly selected active family practice physicians and internists across the United States. They were asked about the perceived values of evidence from randomized controlled trials, locally developed recommendations, no evidence, cost-effectiveness studies, expert opinion, epidemiologic studies, and clinical studies. Analysis of variance and pairwise comparisons were used for statistical testing. RESULTS: Seventy-six (52%) physicians responded. On a Likert scale from one to six, randomized controlled clinical trial was the highest rated evidence (mean 5.07, SD +/- 1.14). Such evidence was significantly superior to locally developed recommendations and no evidence at all (P < .05). The interaction was also strong between the types of evidence and clinical areas (P = .0001). CONCLUSION: While most health care organizations present data without interpretation or simply try to enforce locally developed recommendations, such approaches appear to be inferior to techniques of reporting data with pertinent controlled evidence from the literature. Investigating physicians' perceptions is likely to benefit the design of computer generated messages.

Adult↗

Deletion mutants of the herpes simplex virus type 1 UL8 protein: effect on DNA synthesis and ability to interact with and influence the intracellular localization of the UL5 and UL52 proteins.

The herpes simplex virus type 1 (HSV-1) helicase-primase, an essential component of the viral DNA replication machinery, is a trimeric complex of the virus-coded UL5, UL8, and UL52 proteins. An assembly of the UL5 and UL52 subunits retains both enzymic activities, and the UL8 protein has been implicated in modulating these functions, facilitating efficient nuclear uptake of the complex and interacting with other viral DNA replication proteins. To further our understanding of UL8, we have constructed plasmids expressing mutant proteins, truncated at their N- or C-termini or lacking amino acids internally, under the control of the human cytomegalovirus major immediate-early promoter. Deletion of 23 amino acids from the N-terminus or 33 from the C-terminus abolished the ability of UL8 to support DNA replication in transient transfection assays. None of the UL8 mutants tested exhibited a strong dominant negative phenotype in the presence of the wild-type product, although some inhibition of replication was observed with mutants lacking 165 N-terminal or 497 C-terminal amino acids. The ability of the UL8 mutants to facilitate efficient nuclear localization of UL52 in the presence of coexpressed UL5 was examined by immunofluorescence. Selected mutants were also expressed by recombinant baculoviruses and tested for interaction with UL5 and UL52 in immunoprecipitation assays. The replicative ability of the mutants was found to correlate with their ability to localize UL52 to the nucleus, but not their interaction with UL5 and UL52. This property precluded the identification of any region of UL8 important for its presumed nuclear functions.

Animals↗

Fighting malaria.

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Global Health↗

Studies on the metabolism of the novel antitumor agent [N-methyl-11C]N-[2-(dimethylamino)ethyl]acridine-4-carboxamide in rats and humans prior to phase I clinical trials.

This study reports on the biodistribution and metabolism of the 11C-labeled novel antitumor agent N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) (also known as NSC 601316) in rats (plasma and tissues) and humans (plasma). Information on plasma metabolites was uniquely obtained in humans prior to Phase I clinical trial following i.v. injection of [11C]DACA at tracer dose. DACA was labeled in the N-methyl position using no-carrier-added [11C]iodomethane. Rapid high-performance liquid chromatography methods were developed for metabolite analysis of [11C]DACA. The metabolism of [11C]DACA was investigated in patients by plasma sampling. The biodistribution and metabolism of [11C]DACA was investigated in rats by plasma sampling, sacrifice experiments with tissue analyses, and imaging using positron emission tomography scanning. Analysis of human plasma demonstrated rapid and extensive metabolism of [11C]DACA. The levels of [11C]DACA changed from 77 +/- 8% (SD) at 5 min to 25 +/- 5% at 45 min postinjection. Seven radioactive metabolites were observed in human plasma, and one was identified as [11C]DACA-N-oxide. Rapid clearance of 11C radioactivity from rat blood, plasma, and major organs was observed. The half-life of 11C radioactivity clearance in rat blood between 15 and 90 min was calculated to be 3.2 h; the levels of [11C]DACA in rat plasma decreased from 69 +/- 3% (SD) at 2 min to 29 +/- 1.5% at 25 min. The number of radioactive metabolites in rat plasma was the same as in human plasma except that the proportions differed. Again, one metabolite was identified as the [11C]DACA-N-oxide. Analysis of rat tissues showed rapid and extensive metabolism in tissues, particularly liver and kidney; however, [11C]DACA (i.e., the parent compound) was the major radioactive component in the lung, heart, and brain over 40 min. Positron emission tomography scanning using [11C]DACA in the rat showed little retention of 11C radioactivity in major organs with rapid excretion via gut and kidney. The rat data were consistent with animal (mouse and rat) preclinical data obtained with preexisting techniques with longer-lived isotopes. Labeling of potential anticancer drugs with positron-emitting radionuclides and performing in vivo preclinical evaluation at tracer doses in animals and humans prior to Phase I clinical trials provides unique information that could speed up the assessment of the drug and could potentially assist drug development programs. In this example, there was no unexpected interspecies difference in metabolism of DACA that would have alerted us to make a change in the planned Phase I study.

Acridines↗

Binding characteristics of [125I]TTA 386, ETA-selective antagonist.

The data presented in this manuscript describe the binding characteristics of the ETA-selective antagonist, [125I]TTA 386 (hexamethylenelmino carbonyl-Leu-Tri-Ala-beta-Ala-Tyr-Phe). This radioligand bound with high affinity and specificity to cloned human ETA receptors and rat mesenteric artery ETA receptors. The apparent dissociation constants (KdS) and maximum binding capacities were 1.0 nM and 8.5 pmol/mg for cloned human ETA receptors and 0.8 nM and 170 fmol/mg for rat mesenteric artery membranes respectively. Binding of [125I]TTA 386 was fast reaching equilibrium by 45 min and 15 min for human ETA and rat mesenteric artery membrane, respectively. Addition of excess unlabeled ligand resulted in the dissociation of bound radioligand from both preparations. Competition of [125I]TTA 386 binding by unlabeled ET-1, ET-3, TTA 386 and BQ123 revealed appropriate ETA pharmacology. This radioligand did not display any binding to cloned human ETB receptors.

Animals↗

Triiodothyronine blocks potentiation of HL60 monocyte differentiation by anti-inflammatory agents and by steroids and induces apoptosis of all-trans retinoic acid "primed" cells.

Sensitivity of the human promyeloid cell line HL60 to physiological differentiating agents [e.g. all-trans retinoic acid (all-trans RA) and 1 alpha, 25-dihydroxyvitamin (D3)] is increased by exposure of cells to "anti-inflammatory agents" (e.g. indomethacin) and to steroids [e.g. medroxyprogesterone acetate (MPA)] and post "priming" with a low dose (10(-8) M) of all-trans RA. Co-treatment of serum free-grown HL60 cells (HL60-ITS) with indomethacin and D3 reduces the dose of D3 required for monocyte differentiation from 10(-7) to 6.25 x 10(-9) M. This potentiating effect was observed to be almost absent when experiments where undertaken using serum-grown HL60 cells (HL60-FCS). The agent present in serum that interferes with indomethacin- and MPA-potentiation of the sensitivity of HL60 cells to D3 has been identified as the thyroid hormone 3,5,3'-L-triiodothyronine (T3). "Priming" of HL60-ITS cells with a low dose of all-trans RA reduces the amount of D3 required for the induction of monocyte differentiation to the same degree as co-treatment with either indomethacin or MPA (to 5 x 10(-9) M). However, the combined effect of all-trans RA "priming" and T3 treatment of HL60-ITS cells was induction of apoptosis. Treatment with either agent alone did not result in increased levels of apoptotic cells. These data reveal that T3 has an important influence on the capacity of HL60 cells to undergo differentiation and can promote apoptosis of these cells. Drug combinations, such as a differentiation potentiating agent, for example, indomethacin or MPA, and a differentiation inducer, for example, all-trans RA or D3, may have important therapeutic significance. Serum levels of T3 would be anticipated to influence the outcome.

Anti-Inflammatory Agents, Non-Steroidal↗

Carbon-11 labelling of the antitumour agent N-[2-(dimethylamino)ethyl]acridine-4-carboxamide (DACA) and determination of plasma metabolites in man.

The potential anti-cancer agent N-[2-(dimethylamino)ethyl] acridine-4-carboxamide, DACA has been labelled with carbon-11. N-[2-11C-methyl]DACA was produced in 73% radiochemical yield from [11C]iodomethane in 40 min from EOB. The average radiochemical yield was 3.2 GBq with specific radioactivity of 41.5 GBq mumol-1 at EOS, corresponding to 24 micrograms of stable DACA. The position of labelling was confirmed by co-labelling with [11/13C]iodomethane. PET studies in patients have been performed prior to Phase I trial of DACA and during Phase I trial of DACA. Analysis of serial plasma samples showed that the metabolism of N-[2-11C-methyl]DACA is rapid and extensive in patient plasma.

Acridines↗

Cloning and expression of human V-genes derived from phage display libraries as fully assembled human anti-TNF alpha monoclonal antibodies.

BACKGROUND: With the advent of phage antibody libraries, access to completely human antibody fragments is feasible, either by direct selection from human antibody libraries, or by guided selection. After selection, Fabs and scFvs may need to be expressed as complete antibodies in mammalian cells for further characterisation, or if effector functions are required. OBJECTIVES: To rebuild and express the human anti-TNF alpha antibody Fab-P3A2 (isolated as a Fab fragment from phage display libraries by guided selection) as a fully assembled, functional human antibody (gamma-1, lambda) in Sp2/0 myeloma cells, and to perform preliminary characterisation studies of the secreted IgG1 molecule. A further objective was to investigate the kinetics of human antibody production and the stability of antibody secretion in transfectomas cultured in various media formulations. STUDY DESIGN: A tripartite strategy was employed for cloning heavy chain gene (VH)-P3 and light chain gene V lambda-A2-C lambda into mammalian cell expression vectors p alpha Lys-30 and p alpha Lys-17 respectively. The cell line P3A2.B5 was isolated after co-transfection of Sp2/0 mouse myelomas with the constructs, expanded and weaned into a protein free medium. Fully assembled Ig-P3A2 antibody was purified by Protein A affinity chromatography and characterised with respect to size of antibody chains, and affinity for human TNF alpha. Stability of secretion was investigated by extended serial sub-culture and analysis of P3A2.B5 sub-clones. Strategies of media enrichment were tested for any effect on antibody productivity by selected P3A2.B5 sub-clones. RESULTS: The cell line P3A2.B5 secreted an assembled, human antibody Ig-P3A2, with heavy and light chains of molecular weight 55 and 28 KD respectively. Equilibrium capture studies showed Ig-P3A2 to have a dissociation constant of approximately 1.5 x 10(-8) M. The mean specific productivity of the cell line increased from 1.2 pg/cell/day to 7.8 pg/cell/day by a combination of medium enrichment and serum reduction. Prolonged serial sub-culture of P3A2.B5 showed the cell line to be unstable with respect to antibody secretion. CONCLUSIONS: We have outlined a method for expression of human V genes as assembled antibodies in Sp2/0 myeloma cells. A cloning strategy for the stable expression of scFv or Fab genes isolated from phage display libraries as assembled human antibodies of the IgGl subclass in Sp2/0 myeloma cells has been described. For maximising specific productivity of antibody-producing cell lines, supplementation of culture media with glucose, glutamine and amino acids increases antibody yield significantly compared to that in conventional media, indicating the latter is stoichiometrically limiting for production purposes.

Animals↗

Cognitive impairment in the Amish: a four county survey.

BACKGROUND: The prevalence of probable dementia was determined in a rural, homogeneous community of Amish individuals in the Midwestern USA. The Amish are a genetically isolated group with a low level of formal education (< or = 8 years) and few exposures to modern life, who live in intergenerational setting and have strong social support networks. METHODS: Using community directories, trained interviewers administered the Mini Mental State Examination (MMSE) and a medical history survey to all Amish over 64 years old in a four county area. Individuals with scores < 27 (out of a maximum of 30 points) were given additional neuropsychological tests. Results were reviewed by a neuropsychologist and subjects were classified with regard to probable cognitive impairment. RESULTS: The MMSE scores were inversely related with age and directly with education. The Amish have higher MMSE scores than reported for the general US population. The overall prevalence of probable cognitive impairment for those over 64 years was 6.4%. The prevalence increased with age and lower education and was lowest among married individuals. CONCLUSIONS: The MMSE scores among the Amish were higher than the general population despite their low level of formal education. The lower level of cognitive impairment among the Amish could reflect a lack of inherited susceptibility to dementing diseases, or environmental factors characteristic of their traditional lifestyle. Even among this population with < or = 8 years of formal education, education may protect against cognitive impairment.

Age Distribution↗

An evaluation of empiric vs. nomogram-based dosing of heparin in an intensive care unit.

OBJECTIVE: To compare the time to achieve therapeutic anticoagulation with heparin using two dosing methods. DESIGN: A retrospective before and after time series. SETTING: An 11-bed medical-surgical intensive care unit of a tertiary, teaching hospital. PATIENTS: Critically ill patients who required full dose anticoagulation as part of treatment of hemodynamic or respiratory failure. INTERVENTION: The use of a weight-based dosing nomogram with independent adjustment of infusion rates by nursing staff utilizing the nomogram dosing directions. This nomogram was compared with prior empiric heparin dosing by physicians. MEASUREMENTS AND MAIN RESULTS: The time to achieve a therapeutic activated partial thromboplastin time (PTT) (> 60 secs) was significantly less during use of the nomogram than during use of the empiric dosing method. The number of adjustments required to achieve the therapeutic PTT was less during use of the nomogram. Heparin dosing using the nomogram resulted in larger initial heparin infusion rates (unit/kg) and significantly higher initial PTT results. There was no difference in the initial bolus dose, time to first measured PTT, number of PTT measurements outside the therapeutic range, or signs of toxicity from subtherapeutic or supratherapeutic anticoagulation. CONCLUSIONS: Use of a weight-based heparin dosing nomogram by intensive care unit nursing staff can shorten the time to achieve therapeutic anticoagulation compared with empiric dosing by physicians.

Anticoagulants↗

Palindrome resolution and recombination in the mammalian germ line.

Genetic instability is promoted by unusual sequence arrangements and DNA structures. Hairpin DNA structures can form from palindromes and from triplet repeats, and they are also intermediates in V(D)J recombination. We have measured the genetic stability of a large palindrome which has the potential to form a one-stranded hairpin or a two-stranded cruciform structure and have analyzed recombinants at the molecular level. A palindrome of 15.3 kb introduced as a transgene was found to be transmitted at a normal Mendelian ratio in mice, in striking contrast to the profound instability of large palindromes in prokaryotic systems. In a significant number of progeny mice, however, the palindromic transgene is rearranged; between 15 and 56% of progeny contain rearrangements. Rearrangements within the palindromic repeat occur both by illegitimate and homologous, reciprocal recombination. Gene conversion within the transgene locus, as quantitated by a novel sperm fluorescence assay, is also elevated. Illegitimate events often take the form of an asymmetric deletion that eliminates the central symmetry of the palindrome. Such asymmetric transgene deletions, including those that maintain one complete half of the palindromic repeat, are stabilized so that they cannot undergo further illegitimate rearrangements, and they also exhibit reduced levels of gene conversion. By contrast, transgene rearrangements that maintain the central symmetry continue to be unstable. Based on the observed events, we propose that one mechanism promoting the instability of the palindrome may involve breaks generated at the hairpin structure by a hairpin-nicking activity, as previously detected in somatic cells. Because mammalian cells are capable of efficiently repairing chromosome breaks through nonhomologous processes, the resealing of such breaks introduces a stabilizing asymmetry at the center of the palindrome. We propose that the ability of mammalian cells to eliminate the perfect symmetry in a palindromic sequence may be an important DNA repair pathway, with implications regarding the metabolism of palindromic repeats, the mutability of quasipalindromic triplet repeats, and the early steps in gene amplification events.

Animals↗

Gestational resistance to the pulmonary vasoconstrictor effect of the TxA2 mimetic U-46619: possible mechanism.

Pregnancy is associated with the reduction of vascular sensitivity to vasoconstrictor compounds. We have examined whether pregnancy in rabbits induces hyposensitivity of the pulmonary vascular system to U-46619. Anesthetized, mechanically ventilated nonpregnant (NP; n = 7) and late-pregnant (P; n = 7) rabbits were studied. The intravenous injection of 0.03, 0.1, and 0.3 microgram/kg U-46619 led to a dose-dependent elevation of mean pulmonary arterial pressure (MPAP) in NP rabbits from a baseline value of 15 +/- 1 to 22 +/- 1 mgHg. There was no significant MPAP response to intravenous administration of U-46619 in P rabbits. The pulmonary arterial pressure response of isolated, ventilated, and buffer-perfused lungs of P rabbits was also blunted (P < 0.001 vs. NP). Pulmonary arterial membrane binding of [125I]BOP, another thromboxane (Tx)A2 analog, indicated 48 +/- 16 fmol receptors/mg protein in P rabbits and 193 +/- 48 fmol receptors/mg protein in NP samples (P < 0.025). Receptor affinity [1/dissociation constant (KD)] was also lower in the tissue of P rabbits (P < 0.01 vs. NP). The urinary excretion of the stable TxA2 metabolite 11-dehydro-TxB2 was lower in P than in NP rabbits (P < 0.02), which made homologous desensitization an unlikely explanation for the changes of vascular TxA2 receptors. These results show that, in late gestation, rabbit pulmonary vascular sensitivity to U-46619 is reduced simultaneously with, and as a possible consequence of, downregulation of specific receptors.

15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5↗