(3R,4R)-4-Amino-1-((4-((3-methoxyphenyl)amino)pyrrolo[2,1-f][1,2,4]triazin-5-yl)methyl)-3-piperidinol (BMS-690514), an oral selective inhibitor of human epidermal growth factor receptors 1 (or epidermal growth factor receptor), 2, and 4, and vascular endothelial growth factor receptors 1, 2, and 3, is being developed as a treatment for patients with non-small-cell lung cancer and metastatic bre...

UNLABELLED In PET, transmission scanning for attenuation correction has most commonly been performed with an external positron-emitting radionuclide source, such as (68)Ge. More recently, combined PET/CT scanners have been developed in which the CT data can be used for both anatometabolic image formation and attenuation correction of the PET data. The purpose of this study was to assess the qua...

The pharmacokinetics, metabolism, and excretion of a new antipsychotic drug, ziprasidone, were studied in four normal male volunteers after oral administration of a single 20 mg dose of a mixture of 14C- and 3H-labeled ziprasidone. Blood, urine, and feces were collected at various intervals for determination of total radioactivity and metabolic profiles. Eleven days after the dose, 20.3 +/- 1% ...

The use of radioactively labelled proteins for studying proteolysis is well established (Schneider et al., 1965), as are techniques for radiolabelling proteins, which have been developed mainly for radioimmunassay procedures (Yalow & Berson, 1966). 1311 has been the favoured isotope for such work, although it has a short half-life (8.04 days). "'I has a longer half-life (60 days) and can be eff...

In eight anaesthetized post-absorptive dogs we measured the concentration and specific radioactivity of phenylalanine and leucine in arterial and femoral-venous plasma, together with hindlimb flow during a continuous infusion of L-[ring-2,6-3H]phenylalanine and [1-14C]leucine. The femoral-venous plasma concentration was greater than arterial for both phenylalanine and leucine (P less than 0.05 ...

The biliary excretion and blood/plasma ratios of four novel 5-bromo-6-alkoxy- 5,6-dihydro prodrugs to S-ethyl-2'-deoxyuridine (EDU) including (-)-trans-(5S, 6S)-S-bromo-S-ethyl-6-methoxy-S, 6-dihydro-2'-deoxyuridine (BMEDU), (+ )-trans( SR, 6R)-S-bromo-S-ethyl-6-ethoxy-S, 6-deoxyuridine (BEEDU), (+ )-trans-(SR, 6R)-5-bromo-5-ethyl-6-ethoxy -S, 6-dihydro-S '-O-valeryl-2 ':.deoxyuridine (VBE...

Background: The natural radioactivity level and the radon concentration of soil were measured at four important geothermal area located in Dikili geothermal region, Turkey. Materials and Methods: The natural radionuclide content of soil samples were measured by NaI(Tl) gamma spectrometer system and the soil radon concentration were determined using Kodak-Pethe LR-115 Type II Solid State Nuclear...

The disposition and metabolism of tafluprost, an ester prodrug of the 15,15-difluoro-prostaglandin F(2alpha) antiglaucoma agent, have been studied in rats after ocular administration. Radioactivity was absorbed very rapidly into the eye and systemic circulation after a single ocular dose of 0.005% [(3)H]tafluprost ophthalmic solution, with maximum levels in plasma and most eye tissues occurring...