Conjugated Polyelectrolyte Blend with Polyethyleneimine Ethoxylated for Thickness-Insensitive Electron Injection Layers in Organic Light-Emitting Devices.

Electron injection layers (EILs) based on a simple polymer blend of polyethyleneimine ethoxylated (PEIE) and poly[(9,9-bis(3'-(( N, N-dimethyl)- N-ethylammonium)-propyl)-2,7-fluorene)- alt-2,7-(9,9-dioctylfluorene)] (PFN-Br) can suppress the dependence of organic light-emitting device (OLED) performance on thickness variation compared with single PEIE or PFN-Br EILs. PEIE and PFN-Br were compatible with each other and PFN-Br uniformly mixed in the PEIE matrix. PFN-Br in PEIE formed more fluorene-fluorene pairs than PFN-Br alone.

Air-Stable and High-Performance Solution-Processed Organic Light-Emitting Devices Based on Hydrophobic Polymeric Ionic Liquid Carrier-Injection Layers.

A lot of research, mostly using electron-injection layers (EILs) composed of alkali-metal compounds has been reported with a view to increase the efficiency of solution-processed organic light-emitting devices (OLEDs). However, these materials have intractable properties, such as a strong affinity for moisture, which cause the degradation of OLEDs. Consequently, optimal EIL materials should exhibit high electron-injection efficiency as well as be stable in air.

A chiral BINOL-bridged imidazole dimer possessing sub-millisecond fast photochromism.

We developed a chiral 1,1'-bi-2-naphthol-bridged imidazole dimer possessing 100 μs fast photochromism and high fatigue resistance. It offers great opportunities for the practical applications to fast photoresponsive chiral dopants, invisible security materials and optical trigger molecules to induce the dynamic structural changes in biological matters.

A real-time dynamic holographic material using a fast photochromic molecule.

We have developed a real-time, dynamic holographic material that exhibits rapid colouration upon irradiation with UV light and successive fast thermal bleaching within tens of milliseconds at room temperature. Photochromic polymer films were prepared by a simple solution-casting method from the benzene solution of the mixture of the photochromic molecule, poly(ethyl acrylate), and poly(phenoxyethyl acrylate). The real-time control of holographic images using the photochromic polymer film yields a speed equivalent to the time resolution of the human eye.

Calcitonin gene-related peptide is an important regulator of cutaneous immunity: effect on dendritic cell and T cell functions.

Some cutaneous inflammations are induced by percutaneous exposure to foreign Ags, and many chemical mediators regulate this inflammation process. One of these mediators, calcitonin gene-related peptide (CGRP), is a neuropeptide released from nerve endings in the skin. CGRP binds to its receptors composed of receptor activity-modifying protein 1 and calcitonin receptor-like receptor to modulate immune cell function.

Identification of an orally active opioid receptor-like 1 (ORL1) receptor antagonist 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine as clinical candidate.

Our efforts to optimize prototype opioid receptor-like 1 (ORL1) antagonist 1 led to the discovery of 4-{3-[(2R)-2,3-dihydroxypropyl]-2-oxo-2,3-dihydro-1H-benzimidazol-1-yl}-1-[(1S,3S,4R)-spiro[bicyclo[2.2.1]heptane-2,1'-cyclopropan]-3-ylmethyl]piperidine 10.

Optimization of benzimidazole series as opioid receptor-like 1 (ORL1) antagonists: SAR study directed toward improvement of selectivity over hERG activity.

A structure-activity relationship (SAR) study on the benzimidazole series of opioid receptor-like 1 (ORL1) antagonists related to 1 is described. Optimization of 1 by introduction of a hydrophilic substituent into the thioether part resulted in identification of potent ORL1 antagonists with high selectivity over binding affinity for hERG and other opioid receptors.

2-Cyclohexylcarbonylbenzimidazoles as potent, orally available and brain-penetrable opioid receptor-like 1 (ORL1) antagonists.

The synthesis and biological evaluation of new potent opioid receptor-like 1 (ORL1) antagonists are presented. Conversion of the thioether linkage of the prototype [It is reported prior to this communication as a consecutive series.: Kobayashi, K.

A novel class of cycloalkano[b]pyridines as potent and orally active opioid receptor-like 1 antagonists with minimal binding affinity to the hERG K+ channel.

A series of compounds based on 7-{[4-(2-methylphenyl)piperidin-1-yl]methyl}-6,7,8,9-tetrahydro-5 H-cyclohepta[ b]pyridine-9-ol ( (-)-8b), a potent and selective opioid receptor-like 1 (ORL1) antagonist, was prepared and evaluated using structure-activity relationship studies with the aim of removing its affinity to human ether-a-go-go related gene (hERG) K (+) channel. From these studies, 10l was identified as an optimized structure with respect to ORL1 antagonist activity, and affinity to the hERG K (+)channel. Furthermore, 10l showed good in vivo antagonism with a wide therapeutic index in regards to adverse cardiovascular effects.

Identification of novel benzimidazole series of potent and selective ORL1 antagonists.

Structure-activity studies on benzimidazole lead 1 obtained from library screening led to the discovery of potent and selective ORL1 antagonist 28, 5-chloro-2-[(1-ethyl-1-methylpropyl)thio]-6-[4-(2-hydroxyethyl)piperazin-1-yl]-1H-benzimidazole, which is structurally distinct from conventional non-peptide antagonists known to date.

Formation of acylruthenium promoted by coordination of AlMe(3) to (eta(4)-cyclopentadienone)Ru(CO)(3).

The reaction of AlMe(3) with (eta(4)-tetraphenylcyclopentadienone)Ru(CO)(3) leads to rapid and quantitative formation of an adduct arising from coordination of the enone oxygen to aluminium, which undergoes alkylation at the Ru(CO)(3) moiety to give (eta(5)-C(4)Ph(4)C(OAlMe(2)))Ru(CO)(2)(COMe) concomitant with a change of hapticity of the dienone ligand.

Removal of thiobencarb in aqueous solution by zero valent iron.

A cost-effective method with zero valent iron (ZVI) powder was developed for the purification of thiobencarb (TB)-contaminated water. The removal treatment was performed in the batch system. A sample solution of 10 ml containing 10 microg ml(-1) of TB could be almost completely treated by 100mg of ZVI at 25 degrees C for 12h of treatment time.

Hypertension and dysregulated proinflammatory cytokine production in receptor activity-modifying protein 1-deficient mice.

Calcitonin gene-related peptide (CGRP) is thought to be a prominent neuropeptide in cardiovascular regulation and neuroimmune modulation. There are two isoforms of CGRP (alphaCGRP and betaCGRP), and the main CGRP receptors are probably composed of a calcitonin receptor-like receptor (CLR) and a receptor activity-modifying protein (RAMP)1. However, the physiological functions of CGRP that are mediated through the CLR/RAMP1 receptors remain to be clarified.

Design, synthesis, and biological evaluation of indole derivatives as novel nociceptin/orphanin FQ (N/OFQ) receptor antagonists.

A novel series of 2-(1,2,4-oxadiazol-5-yl)-1H-indole derivatives as nociceptin/orphanin FQ (N/OFQ) receptor antagonists was discovered. Systematic modification of our original lead by changing the pendant functional groups, linker, heterocyclic core, and basic side chain revealed the structure-activity requirements for this novel template and resulted in the identification of more potent analog with improved potency as compared to the parent compound.

Statin blocks Rho/Rho-kinase signalling and disrupts the actin cytoskeleton: relationship to enhancement of LPS-mediated nitric oxide synthesis in vascular smooth muscle cells.

We previously demonstrated statins to enhance cytokine-mediated nitric oxide (NO) synthesis in vascular smooth muscle cells (VSMC). To clarify the mechanism by which this occurs, we evaluated the effects of fluvastatin in lipopolysaccharide (LPS)-stimulated VSMC. NO production induced by LPS was dose-dependently enhanced by fluvastatin, as were iNOS mRNA levels and iNOS protein expression.

Risk factors for vitamin D deficiency in patients with Crohn's disease.

Background: Although the pathogenesis of osteopenia in Crohn's disease is not established, vitamin D deficiency is thought to be an important risk factor. However, little is known about the prevalence of vitamin D deficiency in patients with Crohn's disease in Japan. This study aimed to clarify the prevalence of vitamin D deficiency in patients with Crohn's disease in Japan and to examine the possible causes of the deficiency.

Sabellaria tottoriensis n. sp. (Annelida: Polychaeta: Sabellariidae) from shallow water off Tottori, the Sea of Japan.

A new species of the genus Sabellaria Lamarck, 1812 (Annelida: Polychaeta: Sabellariidae), is described from shallow water off Tottori, the Sea of Japan. Sabellaria tottoriensis n. sp.

Endoscopic diagnosis and staging of mucinous cystic neoplasms and intraductal papillary-mucinous tumors.

Background/purpose: The number of patients with cystic neoplasms of the pancreas as detected using various types of imaging techniques has been steadily increasing. Among the cystic neoplasms, mucinous cystic neoplasms (MCNs) and intraductal papillary-mucinous tumors (IPMTs) were comparatively more frequently encountered. We used imaging techniques to focus on the differential diagnosis of MCNs and IPMTs, and tumor staging.

[Effect of angiotensin II type 1 receptor antagonist on oxidative stress markers in type 2 diabetic patients with hypertension].

Oxidative stress may play a critical role in the pathogenesis of endothelial dysfunction in patients with diabetes or hypertension. An angiotensin II type 1 receptor(AT1) antagonist candesartan is now a widely used antihypertesive drug, and AT1 activation is a predominant source of oxidative stress. We studied the effect of a 12-week treatment of candesartan(4-12 mg-day) on oxidative stress markers [lipid peroxidation(LPO), malondialdehyde-modified LDL(MDA-LDL), 8-epi-PGF2 alpha, and the generation of superoxide anion by monocytes(CLA-DCL)] in 30 type 2 diabetic patients with hypertension (> 140/85 mmHg).

A two-step method for marking polypectomy sites in the colon and rectum.

Background: Intraoperative localization of polypectomy sites is critical for laparoscopic and open surgery, but conventional methods of marking the colorectum are sometimes unreliable. A new two-step method for marking polypectomy sites for identification during laparoscopic and open operations is described.

Methods: Eighteen patients with postpolypectomy lesions necessitating preoperative marking were enrolled in this study.