Adaptation level effects in discrimination of flicker frequency

Pigeons accustomed to food reinforcement for responding in the presence of a 25-Hz flickering light were exposed to several sets of flicker-frequency stimuli arranged as increasing and decreasing series. In the first experiment, food was occasionally delivered for key pecks during 30-s periods of 25-Hz flicker appearing at the beginning, midway, and at the end of an ascending and descending series of nine frequencies, ranging from 13 to 37 Hz. These stimuli appeared for 15-s periods with no food available (extinction). Gradients of responding to flicker values in the ascending series differed from those in the descending series, showing displacements in peak responding toward the lower and higher frequency values, respectively. The same effects occurred when the sequence was changed so that a descending series was followed by an ascending series of frequencies. These effects are consonant with an adaptation level (AL) interpretation and were replicated in a second experiment in which durations of the extinction presentations were increased to 30s. In a final condition, only a descending series was presented and displacement of peak responding from 25 Hz to a higher frequency stimulus, 28 Hz, was observed.     

Biphenyl amide p38 kinase inhibitors 2: Optimisation and SAR

The biphenyl amides are a novel series of p38 MAP kinase inhibitors. Structure-activity relationships of the series against p38alpha are discussed with reference to the X-ray crystal structure of an example. The series was optimised rapidly to a compound showing oral activity in an in vivo disease model.     

Discovery of a novel series of quinoxalines as inhibitors of c-Met kinase

A series of quinoxaline inhibitors of c-Met kinase is described. The postulated binding mode was confirmed by an X-ray crystal structure and optimisation of the series was performed on the basis of this structure. Future directions for development of the series are discussed together with the identification of a novel quinoline scaffold.     

Competition between plant populations with different rooting depths II. Pot experiments

Summary In a previous paper in this series a model was proposed lor the competition between plant populations with different rooting depths. This model predicts that in mixtures of plant populations with different rooting depths the Relative Yield Total will exceed unity. Secondly it predicts that in these mixtures the relative crowding coefficient of the deep rooting population with respect to the shallow rooting one will decrease with increasing plant frequency. Two competition experiments in deep pots are carried out to test these predictions. In the first experiment a comparison is made between a series in which nutrients limited plant growth severely and a series in which nutrients were applied in a quantity that allowed high productivity. In the nutrient poor series the Relative Yield Total exceeded unity by about twenty per cent, while in the nutrient rich series only a small deviation from one was observed. The second experiment was divided into a series of deep pots in which different rooting depths were possible and a series of shallow pots in which the two species were forced to share the same space. In the series of shallow pots the relative crowding coefficient of the two species was found to be independent of plant frequency. In the series of deep pots the relative corowding coefficient of the two species with respect to each other did decrease significantly with increasing frequency.The observed frequency-dependence for the shallow rooting species could be explained by an extension of the theory presented previously. In the spacing series used in the same experiment a decrease of the shoot to root ratio with increasing plant density was observed. Furthermore, in the replacement series the shoot to root ratio in mixture was found to be lower than in monoculture. The consequences of these phenomena for the estimation of the relative crowding coefficient and the Relative Yield Total on the basis of shoot weights are discussed. However, it is argued that the fact that shoot to root ratios change with plant frequency does not provide an alternative explanation for the frequency-dependence observed.Grassland Research Group Publication No. 33     

Temporal variation in phenetic affinity of early Upper Egyptian male cranial series

We carried out an exploratory historical biology study using temporally distinguished groups of predynastic-Early Dynastic male crania from the region of Upper Egypt. The objectives were, first, to determine the overall pattern of phenetic affinity between temporally sequential series and in relation to the earliest series and, second, to explore the possible meanings of the pattern of relationship to sociohistorical change. The cranial series were designated early predynastic, late predynastic, terminal predynastic, and Dynasty I. Craniometric phenetic affinity was ascertained using Mahalanobis distances; a 5% level of probability was chosen for significance. The distance matrix values were ordered into hierarchies of dissimilarity from each series (distance hierarchies) and tabulated for time-successive groups, including the temporally earliest series (i.e., serialized by time). The principal observations were as follows. The overall pattern was not one in which the values between all series were statistically insignificant; nor was it one of consistent sequential increase of biological distance from the earliest series. There was a notable and statistically significant distance between the early and late predynastic groups, with the late and terminal predynastic groups mutually having the lowest and statistically insignificant distances with each other. The value between the terminal predynastic and Dynasty I series was generally larger than the values between other groups and was statistically significant. The overall pattern is possibly consistent with archeological interpretations that postulate increasing intraregional interactions during the late and terminal predynastic periods and the rise of an Egyptian state that eventually included northern Egypt.     

Synthesis and SAR of tetrahydroisoquinolines as Rev-erbα agonists

The design and synthesis of a novel series of Rev-erbα agonists is described. The development and optimization of the tetrahydroisoquinoline series was carried out from an earlier acyclic series of Rev-erbα agonists. Through the optimization of the scaffold 1, several potent compounds with good in vivo profiles were discovered.     

The Role of Hemispheric Functional Specialization in the Analysis of the Relationship between Signal and Nonsignal Information during Image-Shape Classification

The effect of additional information on image shape classification was studied in seven-year-old children. The classified images were either dissimilar in the axis ratio of the basic oval (F) or had an additional element (F + E). In one series of experiments, the additional element was oriented towards a longer axis of the oval, which was a discriminative sign (situation 1, matching); in another series it was rotated by 90° (situation 2, mismatching). The analysis of the successful image classification in series 1 and 2 showed that images with an additional element that mismatches a discriminative sign were classified as being significantly worse than those with matching information. The analysis of the event-related potentials (ERP) from different cortical areas revealed a specific role of the frontal and temporo-parieto-occipital cortical areas in the classification of additional sensory information. The analysis of additional matching information (series 1) was associated with the right hemisphere and evidenced by an increase in N200 wave amplitude in the frontal area and by a negative shift during the development of a late positive complex (250–550 ms) in the temporo-parieto-occipital area. The analysis of additional information mismatching a discriminative sign (series 2) was associated with the left hemisphere and evidenced by an early positive component (P100) in the frontal area, negative components N200–N250, and a further negative shift during the development of late positive complex in the temporo-parieto-occipital area.     

Plant phenological records in northern Finland since the 18th century as retrieved from databases, archives and diaries for biometeorological research

Plant phenological data from northern Finland, compiled from several sources, were examined as potential biometeorological indicators of climate change since the 18th century. A common feature of individual series was their sporadic nature. In addition to waning enthusiasm, wartime hardships and crop failures had caused gaps in recording observations during the 18th and 19th centuries. The present study’s challenge was to combine separate records, as retrieved from several historical archives and personal diaries, into a single continuous series. To avoid possible biases due to the variability of data availability each year, each phenomenon-specific mean series was transformed into normalized site-specific index series. These series were compared to each other and to a regional instrumental temperature series (years 1802–2011). The inter-phenomena correlations were high. Moreover, a strong biometeorological response of the phenological series, most especially to monthly mean temperature in May, and seasonally to the April through June temperatures, was identified. This response focused on slightly later spring months compared to the responses in an earlier study conducted for southern Finland. The findings encouraged us to compute a total phenological index series as an average of all available phenomenon-specific index series for northern Finland. The earliest phenological springs were found as a cluster in the recent end of the record, whereas the anomalously-late phenological spring could be found through the centuries. This finding could indicate that potential future warming could result in an earlier onset of phenological springs (i.e. as experienced by the plants), with a remaining possibility of late phenological springs. To conclude, it was shown that the indices are reliable biometeorological indicators of the April through June temperature variations and thus of the climate variability in the region.     

Synthesis and SAR of 2-phenoxypyridines as novel c-Jun N-terminal kinase inhibitors

The design and synthesis of a novel series of c-jun N-terminal kinase (JNK3) inhibitors is described. The development and optimization of the 2-phenoxypyridine series was carried out from an earlier pyrimidine series of JNK1 inhibitors. Through the optimization of the scaffold 2, several potent compounds with good in vivo profiles were discovered.     

Effect of plant fill ratio on water temperature in constructed wetlands

An existing free-water-surface constructed wetland system at the Auburn University Poultry Science Unit was used to evaluate the effect of plant fill ratio on water temperature. Each wetland consisted of two cells in series. One series was operated with an approximate 10% fill of Sagittaria lancifolia (duck-potato). A second series contained Phragmites australis (common reed) and Scirpus spp. (bulrush) with an approximate 5% fill of plants. A third series was unvegetated and acted as a control. Water temperature was measured using thermographs placed at the midpoint of each cell with temperature readings taken hourly from July 1995 until June 1996. Water temperature was compared between each cell by using paired t-tests for the hourly temperature data. The unvegetated cells had significantly higher temperatures than the vegetated cells year round. The approximate 10% fill ratio series had significantly higher temperatures than the 5% fill ratio during the winter months. The unvegetated cells were significantly warmer than the vegetated cells for 75 of 80 instances. The unvegetated cells also exhibited greater daily variation in temperature than did the vegetated cells.     

Influenza neuraminidase inhibitors: structure-based design of a novel inhibitor series

Combinatorial and structure-based medicinal chemistry strategies were used together to advance a lead compound with an activity of K(i) = 58 microM via a potency enhancement of >70 000-fold to an analogue with an activity of K(i) = 0.8 nM against influenza neuraminidase (A/Tokyo/67). Lead optimization was initiated using molecular modeling and combinatorial chemistry. Protein crystal structures revealed that inconsistent structure-activity relationship (SAR) data resulted from different binding orientations of the inhibitor core five-membered rings from one series to another. Binding modes for a series of compounds showed up to a 180 degrees variation in orientation of the five-membered ring within the active site. Potent analogues were only achieved with chemical series that were observed to bind in the same orientation and yielded consistent SAR. In one series, consistent binding was obtained by an unprecedented occupation of a negatively charged binding pocket by a neutral methyl ester unit. The structural rationale for this novel SAR variation, based on protein crystallographic data, is given.     

Synthesis and in vitro antitumor activity of asperphenamate derivatives as autophagy inducer

In an effort to improve the aqueous solubility and the antitumor activity of natural product asperphenamate, we have designed and synthesized three series of asperphenamate derivatives, including series I (simplifying molecular skeleton series), series II (introducing a hydroxyl group to A-phenyl ring series) and series III (disrupting molecular planarity series). All derivatives have displayed a significantly increased solubility compared with asperphenamate. Their growth inhibitory activities in vitro were screened by the standard MTT method in MCF-7, HeLa, and BEL-7402 cell lines. With the exception of the derivatives in series I, most of derivatives in series II and series III showed growth inhibitory activity. Among all derivatives, IM23b in series III showed the greatest potency in human breast cancer MCF-7 cells. The cellular potency of IM23b was approximately 1.5-fold more potent than that of cisplatin. The mechanism of cell death induced by IM23b in human breast cancer MCF-7 cells was further investigated. We concluded that the cell death was induced by autophagy instead of apoptosis or cell cycle arrest.     

Structure-activity relationships in a series of NPY Y5 antagonists: 3-amido-9-ethylcarbazoles,core-modified analogues and amide isosteres

Beginning with carbazole 1a, the amide and alkyl substituents were optimized to maintain potency while adding solubilizing groups. Efforts to replace the 3-amino-9-ethylcarbazole core, a known carcinogen, used the SAR generated in the carbazole series for guidance and led to the synthesis of a number of core-modified analogues. In addition, an isosteric series, in which the amide was replaced with an imidazole, was prepared. Two potent new series lacking the putative toxicophore were identified from these endeavors.     

Synthesis and SAR of 4-(pyrazol-3-yl)-pyridines as novel c-jun N-terminal kinase inhibitors

The design and synthesis of a novel series of c-jun N-terminal kinase (JNK) inhibitors is described. The development of the 4-(pyrazol-3-yl)-pyridine series was discovered from an earlier pyrimidine series of JNK inhibitors. Through the optimization of the scaffold 2, several potent compounds with good in vivo profiles were discovered.     

Activation of brain structures by fMRI data when viewing the video clips and recall of shown actions

In 10 healthy volunteers, brain tomograms were recorded using an fMRI scanner with a 3T-field magnet. Emotionally neutral and emotionally involving videos were used for stimulation. Registration consisted of seven series: two series of viewing a fixation point and two kinds of video clips, one series of viewing of a succession of two types of video clips, two series of watching videos with subsequent recall, and two series of viewing the fixation point followed by recall of content online. Viewing content online caused the greatest degree of metabolism increase localized in the visual cortex. This activation was more pronounced during the presentation of an emotionally involving video clip. In addition to the occipital lobe, it actively involved the temporal, parietal and, to a lesser extent, the frontal cortex. Activation of the motor cortex was detected only in some subjects. The "interference" effect in which the increase in metabolism was minimal was observed during a consequent demonstration of video-clips. Immediate recall of video-clips after viewing caused the greatest activation of the posterior frontal and motor cortex. Delayed recall activated mostly the anterior frontal cortex. There was a decrease of metabolism in the visual cortex during the recall. The greatest reduction in the visual cortex was observed during immediate recall. Immediate and delayed recall activated the structures associated with the maintenance of consciousness, memory and a system of mirror neurons.     

Changes in evoked potentials during systematic exposure to a series of similar signals with variable intersignal intervals]

Series of clicks, standard by the number of stimuli and greatly varying by the length of interstimuli intervals in each series, were systematically presented to dogs without reinforcement. Evoked potentiale (EP) in the cortical auditory zone were recorded. It has been found that a typical U-shaped distribution of amplitude values of averaged EP is elaborated in the series in the course of repeated presentations; a maximal amplitude is observed in response to the first and last clicks, and a minimal, in the middle of the series. Such a regularity was previously found for the action of standard series with a constant interstimuli interval. It is assumed that an estimation may take place in the dog CNS of the number of signals used in a series, whose mechanism is not necessarily based on the time factor. The ability to estimate the number of signals in the series may be regarded as an elementary model of counting in the dogs' CNS.     

Structural and functional mapping of geosigmeta in Atlantic coastal marshes (France) using a satellite time series

Geosynphytosociology deals with the study of combinations of vegetation series – or geosigmeta – within landscape. Its main advantage is to assess conservation status based on vegetation dynamics. However, this field-based approach has not been widely applied, because local surveys are not representative of spatio-temporal landscape complexity, which leads to uncertainties and errors for geosigmeta structural and functional mapping. In this context, satellite time series appear as relevant data for monitoring vegetation dynamics. This article aims to assess the contribution of an annual satellite time series for geosigmeta structural and functional mapping. The study area, which focuses on the French Atlantic coast (4630 km²), includes salt, brackish, sub-brackish and fresh marshes. A structural vegetation map was derived from the classification of an annual time series of 38 MODIS images validated with field surveys. The functional vegetation map was derived from the annual Integral of Normalized Difference Vegetation Index (NDVI-I), as an indicator of above-ground net primary production. Results show that geosigmeta were successfully mapped at a scale of 1:250,000 with an overall accuracy of 82.9%. The geosigmeta functional map highlights a strong gradient from the lowest NDVI-I values in salt marshes to the highest values in fresh marshes.     

The relationship between nutrient availability,shoot biomass and species richness in grassland and wetland communities

The relationship was studied between shoot biomass, nutrient concentration in the soil and number of species per unit area. The study was carried out in two different parts of the Netherlands, the Gelderse Vallei (east of Amersfoort) and the Westbroekse Zodden (northwest of Utrecht). Four series of vegetation and soil samples were taken: one series in grassland and wetland communities, one series in grassland communities, one series in fen communities and one series in only one wetland community. The two series in grassland communities show a negative correlation between shoot biomass and species number and a positive correlation between shoot biomass and nutrient concentration in the soil. The opposite was found in the series in the fen communities: there was a positive correlation between species number and shoot biomass and a negative correlation between shoot biomass and nutrient concentrations. The series of samples that had been taken in only one wetland community showed an optimum curve for the relation between shoot biomass and number of species. It is concluded that in the plant communities studied the species richness per unit area increases with increasing productivity at low production levels (< 400–500 g/m²) and decreases with increasing productivity at higher production levels (> 400–500 g/m²).     

Power series expansion and structural analysis for life cycle assessment

Goal, Scope and Background The usefulness of power series expansion for an LCA system has often been doubted, as those systems may not possess the unique properties that enable power series expansion and analyses based on the power series. This paper surveys the existing literature on power series expansion of monetary input-output system and discusses how the power series expansion can be utilized for more general systems including the LCA model. Methods The inherent properties of matrices that are capable of producing power series forms for their inverse and, further, can utilize structural path analysis are analyzed. Using these analyses, the way how a matrix that is not eligible for structural analyses is converted into an eligible form is investigated. A numerical example is presented to demonstrate the findings. Results The necessary and sufficient condition for an indecomposable, real square technology matrix can be expressed using power series was identified. Two additional conditions for a technology matrix to be utilized for structural analyses using power series expansion are discussed as well. It was also shown that an LCA system that fulfills the Hawkins-Simon condition can be easily converted into the form that is eligible for structural analysis by rescaling the columns and rows. Discussion As a numerical example, an application of accumulative structural path analysis for an LCA system is shown. The implications of the results are discussed in a more plain language as well. Conclusions The survey presented in this paper provides not only the conditions under which a linear system is expressed using a power series form but also the way to appropriately convert a system to utilize the rich analytical tools using power series expansion for structural analyses. Recommendations and Perspectives Widely used LCA databases and software tools have employed the linear systems approach as the basis. Much of these developments in the domain of LCA have been made, however, in isolation of the rich findings of IOA. There will be much to benefit LCA through an active dialogue between the two disciplines. There are rich analytical tools available through the use of power series expansion. The current survey will help software developers and LCA practitioners to apply such tools in LCA.     

Testosterone propionate treatment of an XY gonadal dysgenetic chacma baboon

Behavioral studies of an XY gonadal dysgenetic chacma baboon prior to and during testosterone propionate treatment were carried out. The orchidectomized dysgenetic individual, two intact males, a castrate male, and two ovariectomized females were pair-tested with a group of eight ovariectomized stimulus females prior to and during their treatment with estradiol benzoate. Three test series were carried out. One series occurred prior to any treatment of the agonadal focal subject animals. During this series it was only the intact males who showed behavior change during their testing with the estrogen treated females. A second test series occurred after a month of daily testosterone propionate injections (1 mg/kg/day) had been given to the four agonadal subjects. During this test series the castrate male ejaculated once with one of the estrogen-treated females. All of the treated subjects showed increases in their frequency of yawning. Upon completion of this test series the androgen dosage was increased (2 mg/kg/day) and 2 weeks later a third test series was carried out. During this series the castrate male ejaculated with five of his eight estrogen-treated partners. The yawning of all the treated subjects continued. As had been the case in the second series the XY gonadal dysgenetic individual continued to behave as did the ovariectomized females. None of these animals showed any increase in any measure of male sexual behavior. This study establishes the fact that a genetic male primate deprived of in utero exposure to testicular hormones will go on to develop as a normal genetic female and will fail to exhibit increased levels of male sexual behavior during androgen treatment.