Results: The nucleophilic Selleckchem PF-573228 substitution reaction proceeded efficiently in acetonitrile at 150 degrees C, giving the Final product in an average yield of 42% and an average specific activity of 30 GBq/mu mol. In vitro, high-SA [I-131]IAZGP was incorporated
into the tumor cells with similar kinetics and oxygen dependence to low-SA [I-131]IAZGP. In HT29 tumor-bearing mice, biodistributions of high- and low-SA [I-131]IAZGP were equivalent. Ex vivo autoradiography revealed heterogeneous intraturnor localization of high-SA [I-131]IAZGP corresponding closely to distributions of other exogenous and enclogenous hypoxia markers. Comparable rnicroregional distribution patterns were observed with low-SA [I-131]IAZGP.
Conclusions: Angiogenesis inhibitor Radiolabeled IAZGP produced via nucleophilic Substitution is validated as an exogenous hypoxia marker. Specific activity does not appear to influence the in vivo hypoxia-mapping ability of the radiotracer. (C) 2009 Elsevier Inc. All rights reserved.”
“Erythropoiesis-stimulating
agents (ESAs) remain the first-line treatment of anemia in lower risk myelodysplastic syndromes (MDS) without 5q deletion. A preliminary report suggested that adding all-trans retinoic acid (ATRA) to ESAs may improve their erythroid response, particularly in patients with high endogenous erythropoietin (EPO) level, and may improve other cytopenias. We conducted a prospective multicenter study of EPO-beta and ATRA in anemic MDS patients with marrow blasts <10% and either previous ESA failure or relapse, endogenous EPO >500 U/l or other cytopenia(s) (absolute neutrophilic count <1.0 G/l or platelets <50 G/l). A total of 59 patients were evaluable after 12 weeks of treatment. The erythroid response
rates according to IWG 2000 and 2006 criteria, respectively, were as follows: overall: 49 and 36%; patients with previous ESA failure (n=28): 43 and 32%; patients with endogenous EPO Piperacetam >500 U/l (n=18): 11 and 19%; patients transfused 42 red blood cells units/month (n=28) 43 and 39%. Only one neutrophil, but no platelet response, and no major side effect were observed. EPO-beta-ATRA combination appears a possible therapeutic option in anemia of MDS having failed an ESA alone, but not in patients with high endogenous EPO level, and does not improve neutropenia and thrombocytopenia.”
“Introduction: The regional brain distribution of (2R,3R)-5-[F-18]fluoroethoxy-benzovesamicol ((-)-[F-18]FEOBV), a radioligand for the vesicular acetylcholine transporter (VAChT), was examined in vivo in mice, rats and rhesus monkeys.
Methods: Regional brain distributions of (-)-[F-18]FEOBV in mice were determined using ex vivo dissection. MicroPET imaging was used to determine the regional brain pharmacokinetics of the radioligand in rat and rhesus monkey brains.