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At least 19 recordsLinked to original sources

PubMed1993

Influence of (-)-S-Bay K 8644, (+/-)-Bay W 5035 and (+/-)-Bay T 5006 on hemodynamics and FITC-dextran 3 elution kinetics in isolated rat hearts.

1. We investigated the effects of the new calcium-agonists (+/-)-Bay W 5035 and (+/-)-Bay T 5006 in comparison to (-)-S-Bay K 8644 on hemodynamics and epimyocardial perfusion in Langendorff rat hearts. 2. At equieffective inotropic concentration, vasoconstriction of coronary resistance vessels was significantly less after (+/-)-Bay W 5035 or (+/-)-Bay T 5006 than after (-)-S-Bay K 8644 application. 3. FITC-Dextran 3 elution kinetics indicated that the epimyocardial vascular volume was significantly reduced only by (-)-S-Bay K 8644. 4. Moreover, (-)-S-Bay K 8644 enhanced transcoronary exchange more markedly than (+/-)-Bay W 5035 or (+/-)-Bay T 5006, reflecting the differences in coronary constrictor activity. 5. We conclude that in comparison to (-)-S-Bay K 8644 the relation between inotropy and vasoconstriction is more favorable for (+/-)-Bay W 5035 or (+/-)-Bay T 5006.

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethy↗

PubMed1994

Comparative effects of the dihydropyridine-type calcium-agonists (-)-S-Bay K 8644, (+/-)-Bay-W 5035 and (+/-)-Bay-T 5006 on human platelet aggregability.

1. Human platelet aggregation induced by collagen is concentration-dependently inhibited by dihydropyridine (DHP)-type calcium(Ca)-agonists. 2. There was no significant difference between the maximal anti-aggregatory effects or the anti-aggregatory potencies of (-)-S-Bay-K 8644 (EC50: 5.3 +/- 1.5 x 10(-5) M), (+/-)-Bay-W 5035 (EC50: 14.9 +/- 8.8 x 10(-5) M) or (+/-)-Bay-T 5006 (EC50: 2.7 +/- 1.9 x 10(-5) M) (P > 0.05). 3. Antiaggregatory effects of DHP-type Ca-agonists seem to be independent of Ca-channel activation.

3-Pyridinecarboxylic acid, 1,4-dihydro-2,6-dimethy↗

PubMed1997

Pharmacology of the 5-lipoxygenase inhibitors BAY Y 1015 and BAY X 1005 in the horse.

Calcium ionophore A23187 induced time and concentration dependent production of immunoreactive leukotriene (LT) B4 by equine heparinized whole blood in vitro. Time dependent production of immunoreactive LTB4 by equine neutrophils and immunoreactive LTC4 by equine eosinophils in vitro was also demonstrated. The 5-lipoxygenase activating protein (FLAP) inhibitors, BAY X 1005 and BAY Y 1015, produced concentration dependent inhibition of ionophore-induced LTB4 synthesis by equine whole blood (mean +/- SEM IC50s n = 5; 6.14 +/- 0.28 microM vs. 12.30 +/- 0.75 microM for BAY Y 1015 and BAY X 1005, respectively) and neutrophils (mean +/- SEM IC50s n = 5; 0.003 +/- 0.001 microM vs. 0.045 +/- 0.021 microM for BAY Y 1015 and BAY X 1005, respectively) and LTC4 synthesis by equine eosinophils (mean +/- SEM IC50s n = 5; 0.0036 +/- 0.0002 microM and 0.108 +/- 0.023 microM for BAY Y 1015 and BAY X 1005, respectively) in vitro. In all three assays, BAY Y 1015 was more potent than BAY X 1005, and for both compounds much higher concentrations were required to inhibit LT synthesis by whole blood compared to isolated neutrophils and eosinophils. Plasma concentration-time relationships and pharmacokinetic parameters for BAY Y 1015 administered intravenously and orally to six horses at a dosage of 10 mg/kg in a two period cross-over study were established. The study also evaluated the anti-inflammatory properties of BAY Y 1015 and its ability to inhibit ex vivo whole blood LTB4 synthesis and in vivo LTB4 synthesis in a tissue cage model of acute inflammation. At this dosage, BAY Y 1015 failed to significantly inhibit immunoreactive LTB4 synthesis or the oedema produced by intradermal injection of the mild irritant, carrageenan.

Administration, Oral↗

PubMed1999

Role of a polycyclic aromatic hydrocarbon bay region ring in modulating DNA adduct structure: the non-bay region (8S,9R,10S, 11R)-N(6)-[11-(8,9,10,11-tetrahydro-8,9, 10-trihydroxybenz[a]anthracenyl)]-2'-deoxyadenosyl adduct in codon 61 of the human N-ras protooncogene.

The structure of the non-bay region (8S,9R,10S,11R)-N(6)-[11-(8,9,10, 11-tetrahydro-8,9,10-trihydroxybenz[a]anthracenyl)]-2'-de oxyadenosyl adduct at X(6) of 5'-d(CGGACXAGAAG)-3'.5'-d(CTTCTTGTCCG)-3', incorporating codons 60, 61 (underlined), and 62 of the human N-ras protooncogene, was determined. Molecular dynamics simulations were restrained by 475 NOEs from (1)H NMR. The benz[a]anthracene moiety intercalated above the 5'-face of the modified base pair and from the major groove. The duplex suffered distortion at and immediately adjacent to the adduct site. This was evidenced by the disruption of the Watson-Crick base pairing for X(6) x T(17) and A(7) x T(16) and the increased rise of 7.7 A between base pairs C(5) x G(18) and X(6) x T(17). Increased disorder was observed as excess line width of proton resonances near the lesion site. Comparison with the bay region benzo[a]pyrene [Zegar, I. S., Kim, S. J., Johansen, T. N., Horton, P. J., Harris, C. M., Harris, T. M., and Stone, M. P. (1996) Biochemistry 35, 6212-6224] and bay region benz[a]anthracene [Li, Z., Mao, H., Kim, H.-Y., Tamura, P. J., Harris, C. M., Harris, T. M., and Stone, M. P. (1999) Biochemistry 38, 2969-2981] adducts with the corresponding stereochemistry and at the same site shows that this non-bay region benz[a]anthracene lesion assumes different base pair geometry, in addition to exhibiting greater disorder. These differences are attributed to the loss of the bay region ring. The results suggest the bay region ring contributes to base stacking interactions at the lesion site. These structural differences between the non-bay and bay region lesions are correlated with site-specific mutagenesis data. The bay region benzo[a]pyrene and bay region benz[a]anthracene adducts were poorly replicated in vivo, and induced A --> G mutations. In contrast, the non-bay region benz[a]anthracene adduct was easily bypassed in vivo and was nonmutagenic.

Bay-Region, Polycyclic Aromatic Hydrocarbon↗

PubMed2001

Selectivity of blocking of low- versus high-voltage activated calcium currents by the dihydropyridine derivatives Bay E5759 and Bay A4339 in neuroblastoma--glioma NG 108-15 cells.

Beneficial therapeutic effects of dihydropyridine derivatives in cardiovascular and neurological disorders are often associated with selective L-type Ca(2+)channel blockade. Here the new dihydropyridine derivatives Bay E5759 (1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid ethyl-1-methylethyl ester) and Bay A4339 (1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridinedicarboxylic acid dimethyl-ester) were tested for their potency and selectivity of blocking of Ba(2+)currents mediated by low-(LVACC)vs high-voltage activated Ca(2+)channels (HVACC) in neuroblastoma-glioma hybrid cells. Nisoldipine and mibefradil served as reference compounds. Bay E5759 and Bay A4339 blocked HVACC at low nanomolar concentrations, whereas LVACC was hardly reduced at up to 10 microM. The order of potency for blockade of HVACC was Bay E5759 (IC(50): 0.4 nM) > Bay A4339 (2.5 nM) approximately = nisoldipine (4 nM) >> mibefradil (3.8 microM). Thus Bay E5759 and Bay A4339 are highly potent and selective blockers of HVACC, presumably L-type Ca(2+)channels.

Animals↗

PubMed1986

Effect of alpha-glycohydrolase inhibitors (Bay m1099 and Bay o1248) on sucrose metabolism in normal men.

The inhibitory effect of N- beta-(4-ethoxycarbonylphenoxy-ethyl-1-desoxynojirimycin (BAY o1248) and of N-hydroxyethyl-1-desoxynojirimycin (BAY o1099) was studied in normal men. Nine healthy volunteers (weight range of 82% to 117% of their ideal body weight) ingested a 50 g sucrose load together with placebo, 50 mg BAY m1099, or 10 mg BAY of o1248. Their substrate oxidation rate was measured by continuous indirect calorimetry during four hours. The plasma glucose and plasma insulin peaks were both significantly blunted and the late fall of glycemia reduced. Mean plasma glucose, fructose, and insulin were reduced by both drugs during the first two hours following the sucrose load and led to a decrease of the suprabasal glucose oxidation (oxidation above baseline) during the first two hours of the test. However, the total suprabasal glucose oxidation during the four hours of the test was not significantly different from that of the control. Breath hydrogen, as an index of malabsorption, was shown to increase with both 50 mg BAY m1099 and 10 mg BAY o1248, starting from the third hour. These findings are consistent with a significant delay of sucrose absorption induced by these new alpha-glycohydrolase inhibitors.

1-Deoxynojirimycin↗

PubMed1983

Comparison of ketoconazole, Bay N7133, and Bay L9139 in the treatment of experimental vaginal candidiasis.

The efficacies of ketoconazole and two new imidazole preparations, Bay N7133 and Bay L9139, were compared in a rat model of experimental candida vaginitis. With a dosage regimen of 10 mg/kg by gavage for 5 days, the cure rate for ketoconazole was 96% as compared with rates of 23 and 29% for Bay N7133 and Bay L9139, respectively (P less than 0.001). Follow-up vaginal cultures at 30 days revealed a relapse in only 1 of 27 rats treated with ketoconazole. Our subsequent experiment in which ketoconazole regimens of 10 mg/kg were compared with Bay N7133 and Bay L9139 regimens of 25 mg/kg demonstrated cure rates of 100, 15, and 82% for the respective agents.

Animals↗

PubMed1979

Comparative study of the aerobic, heterotrophic bacterial flora of Chesapeake Bay and Tokyo Bay.

A comparative study of the bacterial flora of the water of Chesapeake Bay and Tokyo Bay was undertaken to assess similarities and differences between the autochthonous flora of the two geographical sites and to test the hypothesis that, given similarities in environmental parameters, similar bacterial populations will be found, despite extreme geographic distance between locations. A total of 195 aerobic, heterotrophic bacterial strains isolated from Chesapeake Bay and Tokyo Bay water were examined for 115 biochemical, cultural, morphological, nutritional, and physiological characters. The data were analyzed by the methods of numerical taxonomy. From sorted similarity matrices, 77% of the isolates could be grouped into 30 phena and presumptively identified as Acinetobacter-Moraxella, Caulobacter, coryneforms, Pseudomonas, and Vibrio spp. Vibrio and Acinetobacter species were found to be common in the estuarine waters of Chesapeake Bay, whereas Acinetobacter-Moraxella and Caulobacter predominated in Tokyo Bay waters, at the sites sampled in the study.

Aerobiosis↗

PubMed1968

Possible origin of the high incidence of Clostridium botulinum type E in an inland bay (Green Bay of Lake Michigan).

Bottom and shoreline sediments of Green Bay, northern Lake Michigan, and rivers of the Green Bay drainage basin, as well as soils of the surrounding land mass, were examined for Clostridium botulinum type E. Detection was based on identification of type E toxin in enrichment cultures and was influenced by many factors. Testing smaller amounts of sample in multiple cultures was more productive than examining large inocula in fewer cultures. Incubation at 30 C was unsatisfactory, but 14 days at 20 C or 7 days at 25 C gave good results. Mild heating (60 C for 30 min) of specimens reduced the incidence of positive findings. Freezing enrichment cultures prior to testing for toxicity eliminated many nonbotulinal toxic substances that killed mice. A control culture inoculated with type E spores was employed to show whether a specimen contained factors which could mask the presence of type E. Samples from 708 stations were tested in 2,446 cultures. Type E was found in nearly all underwater specimens of Green Bay and northern Lake Michigan but was present less frequently in samples taken along their shores. The incidence was still lower in the rivers emptying into Green Bay with the organism being rare on the shores of these rivers and in the soils of the land mass proper. Samples from the upper reaches of the rivers practically never contained type E. Runoff could deposit type E spores in Green Bay, but this is not considered to be the major factor in the high incidence of the organism. Multiplication in the bay itself is indicated.

Animals↗

PubMedDate not supplied

Innovations in bayes and empirical bayes methods: estimating parameters, populations and ranks.

By formalizing the relation among components and 'borrowing information' among them, Bayes and empirical Bayes methods can produce more valid, efficient and informative statistical evaluations than those based on traditional methods. In addition, Bayesian structuring of complicated models and goals guides development of appropriate statistical approaches and generates summaries which properly account for sampling and modelling uncertainty. Computing innovations enable implementation of complex and relevant models, thereby substantially increasing the role of Bayes/empirical Bayes methods in important statistical assessments. Policy-relevant statistical assessments involve synthesis of information from a set of related components such as medical clinics, geographic regions or research studies. Typical assessments include inference for individual parameters, synthesis over the collection of components (for example, the parameter histogram) and comparisons among parameters (for example, ranks). The relative importance of these goals depends on the context. Bayesian structuring provides a guide to valid inference. For example, while posterior means are the 'obvious' and optimal estimates for individual components under squared error loss, their empirical distribution function (EDF) is underdispersed and never valid for estimating the EDF of the true, underlying parameters. Effective histogram estimates result from optimizing a loss function based in a distance between the histogram and its estimate. Similarly, ranking observed data usually produces poor estimates and ranking posterior means can be inappropriate. Effective estimates should be based on a loss function that caters directly to ranks. Using examples of 'borrowing information', shrinkage and the variance/bias trade-off we motivate Bayes and empirical Bayes analysis. Then, we outline the formal approach and discuss 'triple-goal' estimates with values that when ranked produce optimal ranks, for which the EDF is an optimal estimate of the parameter EDF and such that the values themselves are effective estimates of co-ordinate-specific parameters. We use basic models and data analysis examples to highlight the conceptual and structural issues.

Animals↗

PubMedDate not supplied

Empirical-Bayes and semi-Bayes approaches to occupational and environmental hazard surveillance.

Empirical-Bayes methods offer potentially dramatic improvements in statistical accuracy over conventional statistical methods. We provide an elementary introduction to empirical-Bayes analysis of occupational and environmental hazard surveillance data. Such analyses are especially well suited to situations in which many associations must be examined, but few or none can be estimated precisely. Statistical issues in hazard surveillance are reviewed, followed by a discussion of the rationale and methods for empirical-Bayes analyses, using a study of occupational exposures and cancer mortality to illustrate key concepts. Finally, the assumptions underlying empirical-Bayes analyses are discussed critically, with special attention to the "exchangeability" assumptions that distinguish empirical-Bayes from conventional methods.

Bayes Theorem↗

PubMed1986

The effect of new alpha-glucosidase inhibitors (BAY m 1099 and BAY o 1248) on meal-stimulated increases in glucose and insulin levels in man.

To confirm findings obtained from animal experiments demonstrating the metabolic effect of two new glucosidase inhibitors, 7 single blind cross-over studies with 42 healthy male volunteers were performed. In each group 6 subjects received 25, 50, 100 and 200 mg BAY m 1099 and 10, 20, and 40 mg BAY o 1248 or placebo with a standardized breakfast. Blood glucose and serum insulin were measured in venous blood before and 30, 60, 90, 120 and 180 min after each of 3 meals. ECG, blood pressure, body weight, monitor ECG and haematological and clinico-chemical parameters were also examined. The postprandial increase in blood glucose and serum insulin after breakfast were significantly and dose-dependently reduced by BAY m 1099. 10 and 20 mg BAY o 1248 not only reduced the increases in blood glucose and serum insulin after breakfast, but also after lunch (10 mg). 40 mg BAY o 1248 prevented the postprandial increase in both metabolic parameters after breakfast (p less than 0.05), an effect which was sustained after lunch. Intestinal problems occurred (flatulence, meteorism, diarrhoea) in 25 of 42 volunteers. Objective tolerability was good. The results of these first clinical pharmacological studies with two new glucosidase inhibitors justify studies on patients with diabetes mellitus.

1-Deoxynojirimycin↗

PubMed1983

In-vitro inhibitory activities of 2 new orally absorbable imidazole derivatives: BAY n 7133 and BAY 1 9139.

The inhibitory activities of 2 new orally absorbed antifungal imidazole derivatives, BAY n 7133 and BAY 1 9139, were compared in vitro with those of ketoconazole and miconazole. Clinical isolates of pathogenic fungi tested included 35 yeasts, 62 dimorphic fungal pathogens, 37 filamentous fungi and 31 dermatophytes. LY 121019, a semisynthetic analog of echinocandin B, was included in tests with the pathogenic yeasts. Both BAY n 7133 and BAY 1 9139 were found to be broad spectrum antifungal agents. The spectra of these newer compounds were comparable to those of ketoconazole and miconazole; however only BAY n 7133 resembled these latter 2 imidazoles quantitatively in terms of the degree of antifungal activity as indicated by measurable MICs. In contrast, the spectrum of LY 121019 appeared to be confirmed only to isolates of Candida.

Antifungal Agents↗

PubMedDate not supplied

Off Bayes: effect of verification bias on posterior probabilities calculated using Bayes' theorem.

Estimates of sensitivity and specificity can be biased by the preferential referral of patients with positive test responses or ancillary clinical abnormalities (the "concomitant information vector") for diagnostic verification. When these biased estimates are analyzed by Bayes' theorem, the resultant posterior disease probabilities (positive and negative predictive accuracies) are similarly biased. Accordingly, a series of computer simulations was performed to quantify the effects of various degrees of verification bias on the calculation of predictive accuracy using Bayes' theorem. The magnitudes of the errors in the observed true-positive rate (sensitivity) and false-positive rate (the complement of specificity) ranged from +11% and +23%, respectively (when the test response and the concomitant information vector were conditionally independent), to +16% and +48% (when they were conditionally non-independent). These errors produced absolute underestimations as high as 22% in positive predictive accuracy, and as high as 14% in negative predictive accuracy, when analyzed by Bayes' theorem at a base rate of 50%. Mathematical correction for biased verification based on the test response using a previously published algorithm significantly reduced these errors by as much as 20%. These data indicate 1) that selection bias significantly distorts the determination of predictive accuracies calculated by Bayes' theorem, and 2) that these distortions can be significantly offset by a correction algorithm.

Algorithms↗

PubMed1984

In vitro antifungal activities of Bay n 7133 and Bay L 9139, two new orally absorbed antifungal imidazole derivatives, against pathogenic yeasts.

Bay n 7133 and Bay L 9139 (Bayer AG, Wuppertal, Fed. Rep. Germany) are new, orally absorbable, antifungal imidazole derivatives. In vitro, Bay n 7133 was comparable to ketoconazole and miconazole when tested against isolates of Candida albicans and Cryptococcus neoformans. Bay L 9139 also was active against these organisms but to a lesser degree than the other imidazoles. LY 121019, an analog of echinocandin B, was also tested. It proved to be the most active antimycotic against C. albicans but the least active against C. neoformans. Optimal results were obtained in tests employing Kimmig's agar, a medium previously described for use in susceptibility tests with antifungal agents.

Antifungal Agents↗

PubMed1985

Activity of BAY n 7133 and BAY 1 9139 in vitro and in experimental murine coccidioidomycosis.

The activity of two new antifungal azoles, BAY n 7133 and BAY 1 9139, against Coccidioides immitis was compared with that of ketoconazole in vitro and in experimental murine coccidioidomycosis. Daily intravenous injections were given for 30 days. All mice were autopsied and suspensions of lung, liver and spleen cultured. BAY n 7133 was as active as ketoconazole while Bay 1 9139 was les active. All three drugs were coccidioidostatic only both in vitro and in vivo.

Animals↗

PubMed1984

The metabolic activation of dibenzo[a,e]fluoranthene in vitro. Evidence that its bay-region and pseudo-bay-region diol-epoxides react preferentially with guanosine.

Dibenzo[a,e]fluoranthene ( DBF ), a non- alternant carcinogenic polycyclic aromatic hydrocarbon (PAH), binds covalently to DNA. The main adducts were characterized as covalent additions of its bay-region and pseudo-bay-region diol-epoxides. The structure of these 2 adducts was analyzed by mass spectrometry using their persilyl derivatives. 3,4-Dihydroxy-1,2-epoxy-1,2,3,4-tetrahydro- DBF (3,4-diol-1,2-epoxy- DBF ) and 12,13-dihydroxy-10,11-epoxy-10,11,12,13-tetrahydro- DBF (12, 13-diol-10,11-epoxy- DBF ) obtained by synthesis were allowed to react in vitro with calf thymus DNA or with poly(G). The comigration of DNA and poly(G) adducts isolated after acid hydrolysis of DNA and poly(G) was in good agreement with mass spectroscopic results: both bay-region and pseudo-bay-region DBF diol-epoxides reacted with guanine residues.

Biotransformation↗

PubMed2000

Detection of localized methylmercury contamination by use of the mussel adductor muscle in Minamata Bay and Kagoshima Bay, Japan.

Based on our previous finding that the concentrations of total mercury in mussel adductor muscle approximated those of methylmercury, we compared concentrations of total mercury in the adductor muscle of the mussel Mytilus galloprovincialis, collected from four sites around Minamata City from 1993 to 1995 and four sites in Kagoshima Bay from 1997 to 1998, to assess the level of localized methylmercury contamination. Though the input of mercury from the chemical plant had stopped by around 1970, concentrations of total mercury in the mussel adductor muscle were higher at two sites (26-121 ng/g, n = 135) near the main fallout of wastewater from the chemical plant in Minamata Bay than at the other sites, i.e. two sites 1-5 km from the former sites in Minamata City (6-28 ng/g, n = 52), and all sites in Kagoshima Bay (2-30 ng/g, n = 287). The localized methylmercury contamination around the chemical plant in Minamata Bay was documented also by our sensitive analysis of mercury concentrations in seawater and sediment samples. The survey of concentrations of total mercury in the mussel adductor muscle seems to be useful for monitoring the methylmercury contamination in coastal areas.

Animals↗