Synthesis of some dibenzodiazepinone derivatives as potent and m2-selective antimuscarinic compounds

Two series of 5-[[4-[4-(dialkylamino)butyl]-l-cyclohexyl]acetyl], and 5-[(dialkylamino)acyl]-10,11-dihydro-5H- dibenzo[b,e][1,4]diazepin-11-ones were synthesized as potential m2-selective ligands 1,2. Their affinity and selectivity for the muscarinic cholinergic receptor m-AChR subtypes were determined. Replacing a nitrogen with CH in the piperidine ring of 5-[[4-[4-(dialkylamino)butyl]-l-piperidinyl]acetyl]-10,11-dihydro-5H-dibenzo-[b,e][1,4]diazepin-11-ones 3 significantly altered the affinity and selectivity to the muscarinic receptor subtypes.     

Chemical Biological Sensors Based on Advances in Conducting Electroactive Polymers

Advances in conducting electroactive polymers (CEPs) have driven the design of novel chemical and biochemical sensors. The redox properties of CEPs have been intensely studied for more than two decades with emphasis on their synthesis and characterization. Little attention has been paid to the importance of mechanism in sensor designs. However, in order to design robust and stable sensors, it is important to understand how the polymer structure, morphology, adhesion properties and microenvironment affect sensor performance. This work describes how chemical and biological sensors have been designed, fabricated, characterized and tested based on the fundamental understanding in CEPs. The use of photopolymerized conducting polymers in sensor designs is described. Four focus areas are presented in which the electronic properties of CEPs have enabled the design of novel sensors for organics, nucleic acids, biological molecules, vapors and metal ions.     

High-spin 52 117 Te: Rotational bands? Noncollective oblate

¹¹⁷Te has been studied via⁸²Se(⁴⁰Ar,5n)¹¹⁷Te, and a new, substantially extended level scheme is proposed to I53/2. Our TRS calculations suggest rotational bands, but with an experimental sensitivity of 2%, we see none. Our results differ from those of Sharma, et al, who report two isolated E2 bands. We find them less band-like, being joined at the top and changed in content and order. We suggest a noncollective oblate shape for a new 39/2^– level.This work is supported in part by the Department of Energy under Contract No.DE-AC03-76SF0098(LBL).     

Self-assembly of peptides into a beta-barrel motif

We report the results of a study of the self-assembly of four minimalist peptide strands with a native beta-barrel structure. Using a soft-well potential to mimic cellular crowding, molecular dynamics simulations were performed in confining spheres of varying radii. By utilizing a previously introduced scaling factor lambda for the non-native hydrophobic interactions (0相似文献   

The use of pyridine-2-azo-p-dimethylaniline as an indicator in glacial acetic acid

Pyridine-2-azo-p-dimethylaniline is suggested as an indicator in the titration of amines (aniline, butylamine, p-phenylenediamine and ethylenediamine) with perchloric acid in glacialacetic acid medium. The precision obtainable is much better than that with crystal violet indicator. The pyridine dye can also be used satisfactorily in the titration of sodium carbonate and sodium acetate.     

Ultraviolet B radiation induces upregulation of calcitonin gene-related peptide levels in human Finn chamber skin samples

One of the neuropeptides that plays a role in UVB-induced immunomodulation is calcitonin gene-related peptide (CGRP), as demonstrated in several animal studies. CGRP can be detected in human skin, but effects of UVB exposure on CGRP levels in human skin are not known. We determined CGRP levels in human Finn chamber skin samples of 15 UVB-irradiated and 10 control volunteers. Filter samples were collected prior to and immediately after a UVB exposure protocol (5 consecutive days, with one personally determined minimal erythema dose (MED(jp)) per day). CGRP levels in filter samples were determined using a commercially available radioimmunoassay kit. CGRP could be detected in the filter samples and volunteers showed statistically significantly increased levels after UVB exposure. In addition, the CGRP levels of UVB-exposed volunteers were positively correlated with the dose of UVB in J/m(2) that they received on 5 consecutive days. In other words, higher UVB doses resulted in higher CGRP levels. In summary, CGRP, a mediator in UVB-induced immunomodulation, could be detected in human Finn chamber skin samples, and was significantly increased after UVB exposure. The CGRP level appeared to depend on the amount of UVB the volunteers received.     

Parallel transformations of cyclohexene mediated by the Cp*W(NO) fragment

Hydrogenolysis of Cp*W(NO)(CH2CMe3)2 at room temperature in cyclohexene results in the formation of the intermediate 16e organometallic complex, [Cp*W(NO)(eta2-cyclohexene)]. This intermediate leads to three parallel transformations of cyclohexene, namely (a) C-H activation of cyclohexene to form an eta3-cyclohexenyl hydrido complex, (b) combination of cyclohexene and H2 to form a cyclohexyl hydrido complex, and (c) coupling of two molecules of cyclohexene with concomitant loss of two hydrogen atoms to form a complex containing a novel eta1,eta3-(cyclohexyl)cyclohexenyl ligand. Single-crystal X-ray crystallographic analyses of products resulting from transformations (b) and (c) have been effected.