Rearrangement of 4,5α-epoxymorphinan derivatives with carbamoylepoxy rings provide novel oxazatricyclodecane structures

We describe the rearrangement of a carbamoylepoxy 4,5α-epoxymorphinan derivative that provided a novel 4,5α-epoxymorphinan derivative with an oxazatricyclodecane structure via an oxabicyclo[2.2.2]octane intermediate. We proposed the mechanism of the rearrangement reaction based on results observed in different deprotonation conditions. Epimerization occurred during rearrangement under reversible, but not irreversible, deprotonation conditions. The rearrangement product had a novel fundamental structure with moderate affinities for opioid receptors (K_i (μ)=47.7 nM, K_i (δ)=174.6 nM, and K_i (κ)=248.1 nM). Thus, the rearrangement products might have high potency as opioid ligands.     

1H and 13C NMR Determination of the Enantiomeric Purity of Substituted 4-Amino-3- (thien-2-Yl)-Butyric Acids and 4-Amino-3-(Benzo[b]Furan-2-yl)-Butyric Acids,Ligands of the GabaB Receptor.

The enantiomeric composition and absolute configuration of 4-Amino-3-(benzo[b]furan-2-yl)-Butanoic Acids and of 4-Amino-3-(thien-2-yl)-Butanoic Acids 1 may be accurately determined by ¹H and ¹³C nuclear magnetic resonance analysis of the corresponding derivatives 3 prepared by reaction with chiral reagents. Correlation with HPLC is signaled.     

Characterization of Compounds Acting on the α1A Adrenergic Receptor from Caulis spatholobi by Cell Membrane Chromatography with Possible Application for Treatment of Benign Prostatic Hyperplasia

Tamsulosin hydrochloride is a commonly used drug for treatment of benign prostatic hyperplasia which is a disease affecting elderly men. However, adverse reactions may occur when tamsulosin hydrochloride is used for long-term treatment. Caulis spatholobi is a traditional Chinese medicine with many pharmacological effects. In this study, a cell membrane chromatography column was combined with high-performance liquid chromatography–mass spectrometry to determine the active compounds acting on α1A adrenergic receptor from Caulis spatholobi. Formononetin was shown to be active on the α1A adrenergic receptor. This was investigated by a competitive binding assay that demonstrated that tamsulosin hydrochloride and formononetin employ the same binding sites. Thus, formononetin is a potential α1A adrenergic receptor antagonist for treating benign prostatic hyperplasia.     

Association of UCP3, APN,and TNF-a Gene Polymorphisms with Type 2 Diabetes in a Population of Northern Chinese Han Patients

We observed the polymorphism distribution and coaction of uncoupling protein 3(UCP3)-55C/T,adiponectin(APN)+45T/G and tumor necrosis factor(TNF)-a-308G/A on the onset and development of T2DM in a North...     

Remarks on the formula for γ-interior

The paper presents a formula for the γ-interior of a set under special conditions for , more general than those in the previous paper [Acta Math. Hungar. 80 (1998) 89-93]. There are also some applications.     

Efficient synthesis of optically active α-substituted glutamate analogs possessing α-hydroxymethyl and α-alkoxymethyl groups

Highly enantioselective synthesis of (2R)-α-(hydroxymethyl)glutamate (1), a selective agonist of mGluR2 and 3, was achieved in short steps using an asymmetric version of the Strecker synthesis. This was converted into its α-methoxymethyl- and α-benzyloxymethyl derivatives 2 and 3, possible ligands as tools to investigate glutamate receptors, via protection of the sterically hindered amino group by means of phase transfer catalyst.     

CaWO4晶体中F型色心电子结构的研究

运用相对论的密度泛函离散变分法(DV-Xα)研究了CaWO₄晶体中F型色心的电子结构. 计算结果表明，F和F⁺心在禁带中引入了新的施主能级；分析了晶体内可能存在的光学跃迁模式，并通过过渡态的方法计算了F，F⁺心跃迁到导带底的能量分别为1.92eV和2.42eV. 因此，从理论上推断了F和F⁺心在CaWO₄晶体中可能引起650nm和515nm的吸收，由此说明CaWO₄晶体中650nm和515nm吸收带起源于晶体中的F和F⁺心. 关键词： 4晶体')" href="#">CaWO₄晶体 +心')" href="#">F和F⁺心 DV-Xα     

Crystal structure of ethene-/α-olefin copolymers with various long comonomers (C8–C26)

Ethene-/α-olefin copolymers having a wide range of comonomers between 8 and 26 carbon atoms in length were characterized by wide angle X-ray diffraction (WAXD). It was found that the crystallinities for the shorter comonomers (C₈, C₁₂) matched fairly well with the crystallinities from DSC and volumetric measurements, while for the longer comonomers (C₁₈, C₂₆) distinct differences between the three methods were found. This was explained by the presence of an additional crystalline phase of the side chains slightly deforming the amorphous peak.