Dipyridyl amides: potent metabotropic glutamate subtype 5 (mGlu5) receptor antagonists

The mGlu5 receptor has been implicated in a number of CNS disorders. Herein, we report on the discovery, synthesis, and biological evaluation of dipyridyl amides as small molecules mGluR5 antagonists.     

Effect of testosterone propionate on fine structure and gonadotrophin content of the female rat and hamster anterior pituitary

Summary The effect of long-term testosterone propionate treatment on the adult female rat and hamster anterior pituitary was investigated by means of combined bioassay and electron microscopy. In the rat, a marked hypertrophy and enhancement of secretory activity of FSH cells occurred which correlated well with a marked increase of follicle stimulating hormone (FSH) stores. A moderate decrease of luteinizing hormone (LH) stores was not accompanied by changes in so-called LH cells. Alterations in acidophilic cell types were also observed. Somatotrophs were atrophic and showed evidence of decreased secretory activity, while lactotrophs appeared to be stimulated by testosterone treatment. There were similar changes in the hamster.     

Family resemblance for anthropometric and blood pressure measurements in Black Caribs and Creoles from St. Vincent Island

This paper examines family resemblance for five anthropometric measurements (height, weight, triceps skinfold, upper arm circumference relaxed [UACR] and flexed [UACF] and for systolic and diastolic blood pressure in a group of adult Caribbean islanders of primarily African ancestry. Six hypotheses about family resemblance are tested by using path analysis and likelihood ratios. Significant intergenerational transmission is found only for height and UACR. For weight, UACF, and diastolic blood pressure, non-transmissible sibling resemblance is the primary component of family resemblance, although significant marital resemblance exists for diastolic blood pressure. Triceps skinfold and systolic blood pressure show no evidence of any family resemblance. Although results for highly heritable traits such as height are comparable to reports from other populations, measurements with a large contribution from common family environment or residual environmental effects, such as triceps skinfold or blood pressure, have much lower family resemblance in this population than in other populations. We hypothesize that this difference is due to the fact that adult children and their parents do not share a common household in this culture and to the presence of major nonfamilial environmental factors contributing to obesity and hypertension in this population.     

Human fibroblast stromelysin catalytic domain: expression, purification, and characterization of a C-terminally truncated form.

Stromelysin-1 is a member of a tissue metalloproteinase family whose members are all capable of degrading extracellular matrix components. A truncated form of human fibroblast prostromelysin 1 lacking the C-terminal, hemopexin-like domain has been expressed in Escherichia coli and purified to homogeneity. Treatment of this short form of prostromelysin with (aminophenyl)mercuric acetate resulted in activation and loss of the propeptide in a manner identical with the wild-type, full-length protein. Kinetic comparisons using Nle11-substance P as a substrate showed that the wild-type stromelysin and the truncated form of the enzyme had similar kcat and Km values. Likewise, both enzymes displayed similar Ki values for a hydroxamate-containing peptide inhibitor. Taken together, these results indicate that the C-terminal portion of stromelysin is not required for proper folding of the catalytic domain, maintenance of the enzyme in a latent form, activation with an organomercurial, cleavage of a peptide substrate, or interaction with an inhibitor. Moreover, the active short form of stromelysin displayed a reduction in the C-terminal heterogeneity, a characteristic degradation of the full-length stromelysin, and thereby provides a more suitable protein for future structural studies.     

Stable isotope analyses of collagen in fish scales: limitations set by scale architecture

Comparisons between the stable isotope composition of carbon in collagen excized from juvenile (freshwater) and adult (marine) portions of scales from Atlantic salmon Salmo salar demonstrated that c. 75% of carbon analysed in the 'juvenile' portion of the scale derives from later formed collagen. Scale collagen analyses were effectively restricted to the last season of growth.     

Activities in Crude Porcine Pancreatic Lipase: Enantioselectivity in Hydrolysis of the Diacetate of 2-Phenylpropane-1,3-Diol

The hydrolysis of a prochiral diacetate by porcine pancreatic lipase is catalysed by the purified enzyme, not by an enzyme present in the crude enzyme but absent from the purified enzyme, as previously reported.     

Temporal and spatial patterns in fire occurrence during the establishment of mixed‐oak forests in eastern North America

Question: What was the role of fire during the establishment of the current overstory (ca. 1870–1940) in mixed‐oak forests of eastern North America? Location: Nine sites representing a 240‐km latitudinal gradient on the Allegheny and Cumberland Plateaus of eastern North America. Methods: Basal cross‐sections were collected from 225 trees. Samples were surfaced, and fire scars were dated. Fire history diagrams were constructed and fire return intervals were calculated for each site. Geographic patterns of fire occurrence, and fire‐climate relationships were assessed. Results: Fire was a frequent and widespread occurrence during the formation of mixed‐oak forests, which initiated after large‐scale land clearing in the region ca. 1870. Fire return ranged from 1.7 to 11.1 years during a period of frequent burning from 1875 to 1936. Fires were widespread during this period, sometimes occurring across the study region in the same year. Fires occurred in a variety of climate conditions, including both drought and non‐drought years. Fires were rare from 1936 to the present. Conclusions: A variety of fire regime characteristics were discerned. First, a period of frequent fire lasted approximately 60 years during the establishment of the current oak overstory. Second, fire occurred during a variety of climate conditions, including wet climates and extreme drought. Finally, there was within‐site temporal variability in fire occurrence. These reference conditions could be mimicked in ongoing oak restoration activities, improving the likelihood of restoration success.