Enhancement of the liver on dynamic MDCT: investigation among three groups consisting of noncirrhotic patients and cirrhotic patients with and without a large portosystemic shunt.

Purpose: The aim of this study was to determine any difference in hepatic enhancement values on dynamic multidetector row computed tomography (MDCT) among three groups: noncirrhotic patients and cirrhotic patients with and without a large portosystemic shunt.

Materials And Methods: A group of 20 noncirrhotic patients (group A), 43 cirrhotic patients without a large shunt (group B), and 20 cirrhotic patients with a large shunt (group C) underwent dynamic MDCT of the liver using a standard concentration (300 mg I/ml) and volume (100 ml) of contrast material. The attenuation values of the liver were measured during arterial, portal, and late phases.

Dynamic contrast-enhanced MDCT of the liver: analysis of the effect of different iodine concentrations with the same total iodine dose in the same chronic liver disease patients.

Purpose: To evaluate the effect of aortic and hepatic enhancement in patients with chronic liver disease who underwent dynamic MDCT using a higher concentration of contrast material within the same total iodine dose (80 mL of 370 mgI/mL), compared with a standard iodine concentration (100 mL of 300 mgI/mL).

Materials And Methods: Dynamic MDCT of the liver was performed in 35 patients using different prefilled syringes (300 mgI/mL = group A, 370 mgI/mL = group B) during follow-up periods. The bolus-tracking program was used to automatically start the arterial phase scan.

[Clinical usefulness of B-flow imaging in the diagnosis of superficial soft tissue tumors].

B-flow imaging is a recently developed ultrasound technique that extends the B-mode imaging quality of blood flow, including high-frame-rate and high-spatial-resolution imaging. The purpose of the present study was to clarify the usefulness of B-flow for evaluation of the hemodynamics of superficial soft tissue tumors. All 33 cases of superficial soft tissue tumors were examined by both B-flow and Color/Power Doppler methods on the same plane.

Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent.

The p38 mitogen-activated protein (MAP) kinase has been implicated in the proinflammatory cytokine signal pathway, and its inhibitors are potentially useful for the treatment of chronic inflammatory diseases such as rheumatoid arthritis (RA) and inflammatory bowel disease. To develop a new drug for RA, we synthesized a novel series of 4-phenyl-5-pyridyl-1,3-thiazoles and evaluated their inhibition of p38 MAP kinase, lipopolysaccharide (LPS)-stimulated release of tumor necrosis factor-alpha (TNF-alpha) from human monocytic THP-1 cells in vitro, and LPS-induced TNF-alpha production in vivo in mice. During the course of the study, we found that these compounds risk the inhibition of cytochrome P450 (CYP) isoforms by coordination of the 4-pyridyl nitrogen with heme iron.

Synthesis and biological activities of 4-phenyl-5-pyridyl-1,3-thiazole derivatives as p38 MAP kinase inhibitors.

A novel series of 4-phenyl-5-pyridyl-1,3-thiazole analogues possessing potent in vitro inhibitory activity against p38 mitogen-activated protein kinase and the release of tumor necrosis factor-alpha (TNF-alpha) from human monocytic THP-1 cells stimulated by lipopolysaccharide has been identified. Subsequent structure-activity relationship (SAR) studies and optimization for absorption, distribution, metabolism, and elimination (ADME) profiles led to the identification of compounds 7 g and 10b as orally active lead candidates that block the in vivo production of proinflammatory cytokine (TNF-alpha). In pharmacokinetic studies, compound 10b showed good oral administration in mice and demonstrated significant in vivo anti-inflammatory activity in an anti-collagen monoclonal antibody-induced arthritis mouse model (minimum effective dose (MED)=30 mg/kg).