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The high degree of similarity between the mouse and human genomes is demonstrated through analysis of the sequence of mouse chromosome 16 (Mmu 16), which was obtained as part of a whole-genome shotgun assembly of the mouse genome. The mouse genome is about 10% smaller than the human genome, owing to a lower repetitive DNA content. Comparison of the(More)
Peripheral corticotropin-releasing factor (CRF) receptor ligands inhibit gastric acid secretion and emptying while stimulating gastric mucosal blood flow in rats. Endogenous CRF ligands are expressed in the upper gastrointestinal (GI) tissues pointing to local expression of CRF receptors. We mapped the distribution of CRF receptor type 1 (CRF1) and 2 (CRF2)(More)
The encapsulated form of hepatocellular carcinoma (HCC) is a pathologic subtype that has been found to occur with variable frequency in typical HCC in Japanese radiological, surgical, and autopsy series. It is a well-differentiated tumor that tends to grow slowly and noninvasively, and has a better prognosis than other gross forms of HCC. Among the 73 cases(More)
4-Amino-N-arylpiperidines serve as effective bioisosteres for N-arylpiperazines in the series of dihydropyridine NPY1 receptor antagonists. These were prepared by a ZnCl2-mediated reductive amination reaction between elaborated primary amines, 2 or 5, and 4-arylpiperidones.
Partial tears of the peroneal tendons are rare. Partial longitudinal tears of the peroneus longus tendon are even more rare. We report on 2 professional basketball players who had partial peroneus longus tendon tears beneath the cuboid. A literature review and discussion of treatment is included.
The radiographic findings in the stomach in the upper gastrointestinal examination in 11 patients with the Acquired Immune Deficiency Syndrome (AIDS) were reviewed. Four cases of Kaposi's sarcoma (KS) showed multiple submucosal nodular filling defects; in one of these cases, ulceration of some of the nodules was present. Gastric lymphoma occurred in two(More)
The orexigenic peptide ghrelin has been shown to have prokinetic activity in the gastrointestinal (GI) system of several species, including humans. In this series of experiments, we have evaluated the prokinetic activity of novel, small-molecule ghrelin receptor (GhrR) agonists after parenteral and peroral dosing in mice and rats. Gastric emptying, small(More)
Incorporation of substituted phenyl piperazine privileged structures into a known MC4 specific dipeptoid consensus sequence resulted in a series of potent (EC(50)=24 nM) and selective MC4-R agonists. We report the SAR of this series of compounds using in vitro cAMP functional assays in cells transfected with the MC4 or other melancortin receptors.
1H-tetrazole-1-alkanenitrile SR-9g exhibits a >10-fold in vivo potency enhancement over the lead nitrile 1 and has acceptable oral bioavailability in rats and dogs. An enantiospecific synthesis of 1H-tetrazole-1-alkanenitrile nitriles 9 has been developed.