7-Azaindole-3-acetic acid derivatives: Potent and selective CRTh2 receptor antagonists

High throughput screening identified a 7-azaindole-3-acetic acid scaffold as a novel CRTh2 receptor antagonist chemotype, which could be optimised to furnish a highly selective compound with good functional potency for inhibition of human eosinophil shape change in whole blood and oral bioavailability in the rat.     

Identifying Space Use at Foraging Arena Scale within the Home Ranges of Large Herbivores

An intermediate spatiotemporal scale of food procurement by large herbivores is evident within annual or seasonal home ranges. It takes the form of settlement periods spanning several days or weeks during which foraging activity is confined to spatially discrete foraging arenas, separated by roaming interludes. Extended by areas occupied for other activities, these foraging arenas contribute towards generating the home range structure. We delineated and compared the foraging arenas exploited by two African large herbivores, sable antelope (a ruminant) and plains zebra (a non-ruminant), using GPS-derived movement data. We developed a novel approach to specifically delineate foraging arenas based on local change points in distance relative to adjoining clusters of locations, and compared its output with modifications of two published methods developed for home range estimation and residence time estimation respectively. We compared how these herbivore species responded to seasonal variation in food resources and how they differed in their spatial patterns of resource utilization. Sable antelope herds tended to concentrate their space use locally, while zebra herds moved more opportunistically over a wider set of foraging arenas. The amalgamated extent of the foraging arenas exploited by sable herds amounted to 12-30 km², compared with 22-100 km² for the zebra herds. Half-day displacement distances differed between settlement periods and roaming interludes, and zebra herds generally shifted further over 12h than sable herds. Foraging arenas of sable herds tended to be smaller than those of zebra, and were occupied for period twice as long, and hence exploited more intensively in days spent per unit area than the foraging arenas of zebra. For sable both the intensity of utilization of foraging arenas and proportion of days spent in foraging arenas relative to roaming interludes declined as food resources diminished seasonally, while zebra showed no seasonal variation in these metrics. Identifying patterns of space use at foraging arena scale helps reveal mechanisms generating the home range extent, and in turn the local population density. Thereby it helps forge links between behavioural ecology, movement ecology and population ecology.     

Phosphoramidites of [180] Chiral (Rp)- and (Sp)-Configurated Dimer-Blocks and their Use in Automated Oligonucleotide Synthesis

Abstract

The N,N-diisopropylphosphoramidites 1 and 2 of appropriately protected chiral diastereoisomers of d(T-[P-180]-A) (6a and 6o, resp.) have been synthesized. They were employed in solid-phase synthesis to yield the octamers d(GAGT-(Rp)-[P180]-ACTC) and d(GAGT-(Sp)-[P180]-ACTC).     

Ramet Demography of a Clonal Invader, <Emphasis Type="Italic">Arundo donax</Emphasis> (Poaceae), in Southern California

Arundo donax L. is a rhizomatous perennial, asexually reproducing species that has invaded riparian habitats throughout Mediterranean climate zones. This research evaluated ramet demography of A. donax in two California riparian communities that differed in nitrogen availability. Quadrats were established along 100 m transects at each site and oriented across the advancing fronts of established populations. Morphology and phenology were assessed monthly over 1 year for calculation of demographic parameters and rhizomes were excavated and mapped at the end of the experiment. A. donax exhibited seasonal patterns of recruitment but no dormancy at the high nitrogen site, while at the low nitrogen site no recruitment occurred in the winter and maximum recruitment was delayed by a month relative to the high nitrogen site. Spread of A. donax was delayed until spring and lower overall in the low nitrogen site compared to the high nitrogen site, where lower initial density, greater production of shoots, and higher linear and areal addition indicated that this population was spreading more rapidly. Temperature and precipitation influenced seasonality and amount of recruitment of A. donax in this study. Several recently established, immature clumps were found in gaps at the low nitrogen site, likely due to flood-mediated dispersal of propagules. Recruitment in these clumps occurred from shoot buds, in contrast to the mature populations that reproduced from rhizome buds. Ecologically based management strategies for A. donax and other exotic species should account for differences such as those described here and be tailored to local conditions where the species occurs.     

The impacts of flow on chemical communication strategies and fight dynamics of crayfish

Signal transmission is influenced by the physics of an environment. Consequently, a physical effect on sensory signals can influence how animals send or sample sensory information. Habitat-specific physics may constrain or enhance signal transmission (e.g. sound transmission in a flowing river versus a still pond) and provide a mechanism for the evolution of sensory biases. This study investigated how the transmission of chemically mediated social signals in crayfish is influenced by two different aquatic environments. Agonistic bouts between crayfish were performed under lotic (flowing water) and lentic (nonflowing, still water) conditions. When crayfish (Orconectes rusticus) collected from a lotic system (river) interacted under lotic conditions, we noted that dominant O. rusticus spent more time upstream than subordinate O. rusticus. Orconectes rusticus positioned themselves randomly and spent equal amounts of time with respect to upstream and downstream in the nonflowing environment. We tested another species, Orconectes virilis, collected from a nonflowing environment (lake) and they showed no positional preference when tested in flow. Additionally, both O. rusticus and O. virilis took longer to reach high fight intensities under flow conditions. It was possible to visualize O. rusticus urine release, and they released urine more often when upstream of an opponent in a flow environment during these agonistic bouts. These results suggest that O. rusticus collected from lotic environments release urine to maximize the transmission of chemical cues to a fight opponent. It appears that crayfish may adapt their signalling processes based upon their long-term ambient environments.     

Retinol-binding protein 4 is expressed in chondrocytes of developing mouse long bones: implications for a local role in formation of the secondary ossification center

Retinol-binding protein 4 (Rbp4) is the major carrier of retinol in the bloodstream, a retinoid whose metabolites influence osteogenesis, chondrogenesis and adipogenesis. Rbp4 is mainly produced in the liver where it mobilizes hepatic retinol stores to supply other tissues. However, Rbp4 is also expressed in several extrahepatic tissues, including limbs, where its role is largely unknown. This study aimed to identify the cellular localization of Rbp4 to gain insight into its involvement in limb development and bone growth. Using immunohistochemistry, we discovered that Rbp4 was present in a variety of locations in developing embryonic and postnatal mouse hindlimbs. Rbp4 was present in a restricted population of epiphyseal chondrocytes and perichondral cells correlating to the future region of secondary ossification. With the onset of secondary ossification, Rbp4 was detected in chondrocytes of the resting zone and in chondrocytes that bordered invading cartilage canals and the expanding front of ossification. Rbp4 was less abundant in proliferating chondrocytes involved in primary ossification. Our data implicate the involvement of chondrocytic Rbp4 in bone growth, particularly in the formation of the secondary ossification center of the limb.