11 research outputs found

    Correlation of size parameters.

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    <p>Red: <i>Phoenix dactylifera</i>, black: all <i>Phoenix</i> except <i>P</i>. <i>dactylifera</i>, in mm. Each pair of correlations is plotted on the lower left side while the coefficients of correlation <i>r</i> are given on the upper right-hand side: <i>r</i><sub><i>1</i></sub> corresponds to the correlation coefficients when all <i>Phoenix</i> species are included while <i>r</i><sub><i>2</i></sub> were calculated after discarding the date palm <i>P</i>. <i>dactylifera</i>.</p

    <i>Phoenix dactylifera</i> seed samples for morphometric analyses.

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    <p>When different from the country of sampling, the country of origin of the cultivar is given in parenthesis. Acc. Nb.: Accession number; Nb. seed: Number of seeds.</p

    Variability of seed dimensions and shape within <i>Phoenix</i> species.

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    <p>It is calculated as the dispersion of seeds around the related species’ centroid in two PCA spaces obtained from size parameters (Size Var.) and 64 Fourier coefficients related to dorsal and lateral seed shapes (Shape Var.) using the rarefaction method. The values are the average over the mean distance between 20 randomly sampled seeds in one hundred replicates and the standard deviation over the one hundred replicates. The groups derived from Tukey’s test are given into parentheses.</p

    Identification, Optimization, and Pharmacology of Acylurea GHS-R1a Inverse Agonists

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    Ghrelin plays a major physiological role in the control of food intake, and inverse agonists of the ghrelin receptor (GHS-R1a) are widely considered to offer utility as antiobesity agents by lowering the set-point for hunger between meals. We identified an acylurea series of ghrelin modulators from high throughput screening and optimized binding affinity through structure–activity relationship studies. Furthermore, we identified specific substructural changes, which switched partial agonist activity to inverse agonist activity, and optimized physicochemical and DMPK properties to afford the non-CNS penetrant inverse agonist <b>22</b> (AZ-GHS-22) and the CNS penetrant inverse agonist <b>38</b> (AZ-GHS-38). Free feeding efficacy experiments showed that CNS exposure was necessary to obtain reduced food intake in mice, and it was demonstrated using GHS-R1a null and wild-type mice that this effect operates through a mechanism involving GHS-R1a
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