Synthesis,structure, in vitro pharmacology,and in vivo activity of trans-3,4-dichloro-N-[[1-(dimethylamino)-4-phenylcyclohexyl]methyl]-benzamide (AP01; 4-phenyl-AH-7921), a novel mixed μ-/κ-opioid

Analogs of non-fentanyl novel synthetic opioids (NSO) with modifications that fall outside of established structure–activity relationships (SARs) for that class of drugs create the question whether or not it should be considered an analog, as defined by 21 U.S.C. §802(32)(A), which is important for its inclusion in the US system of drug scheduling. AH-7921 is a US Schedule I drug and an example of the 1-benzamidomethyl-1-cyclohexyldialkylamine class of NSO. The SARs regarding substitution of the central cyclohexyl ring have not been well characterized in the literature. Therefore, in order to expand the SAR surrounding AH-7921 analogs, trans-3,4-dichloro-N-[[1-(dimethylamino)-4-phenylcyclohexyl]methyl]-benzamide (AP01; 4-phenyl-AH-7921) has been synthesized, analytically characterized, and tested in vitro and in vivo pharmacologically. Using methods described in the original patents for this class of NSO, it was found that the single trans geometric isomer was obtained. The proton nuclear magnetic resonance, mass spectrum, infrared spectrum, and Raman spectrum are reported along with the melting point of the hydrochloride salt. In vitro binding to a battery of 43 central nervous system receptors showed it to be a high-affinity μ-opioid receptor (MOR) and κ-opioid receptor (KOR) ligand (60 nM and 34 nM, respectively). AP01 also had a 4 nM affinity for the serotonin transporter (SERT), which is a higher level of potency at this receptor than most other opioids. In rats, it exhibited antinociception in the acetic acid writhing test. Therefore, the 4-phenyl modification results in an active NSO, but carries with it potential toxicities beyond those expected for currently approved opioid drugs.     

Pressure sensitive adhesives and paper spray-mass spectrometry for the collection and analysis of fentanyl-related compounds from shipping materials

The rise of fentanyl and fentanyl analogs in the drug supply pose serious threats to public health. Much of these compounds enter the United States through shipping routes. Here we provide a method for fentanyl screening and analysis that utilizes pressure-sensitive adhesive (PSA) lined paper to recover drug residues from parcel-related surfaces. The paper used is commercially available repositionable notes (also called post-it or sticky notes). From this paper, mass spectra were obtained by paper spray-mass spectrometry (PS-MS), where PSA paper served as both a sampling and analysis substrate. Seven fentanyl-related compounds were analyzed: fentanyl, 4-anilino-N-phenethylpiperidine (4-ANPP), N,1-diphenethyl-N-phenylpiperidin-4-amine (phenethyl-4-ANPP), valerylfentanyl, 4-fluoroisobutyrylfentanyl (4-FIBF), carfentanil, and p-fluorofentanyl. These compounds were recovered by PSA paper and identified by PS-MS from packaging tape and plastic at 50 ng and from cardboard and shipping labels at 100 ng. The impact of cutting agents on PS-MS analysis of fentanyl analogs was explored. No trends of analyte suppression were found at high concentrations of the cutting agents caffeine, diphenhydramine, and lidocaine when recovered from surfaces. A cartridge that required no precise cutting of PSA paper prior to sampling or analysis was evaluated for use in PS-MS for fentanyl screening. Recovery and detection of fentanyl from plastic sheeting was demonstrated with this cut-free cartridge. The cut-free cartridge showed somewhat less consistency and lower analyte signal than the standard cartridge, but performance was suitable for potential screening applications. In combining PSA surface sampling with PS-MS for drug screening, both sampling and detection of fentanyl-related compounds is simple, rapid, and low-cost.     

王安忆小说的叙事建构及读解

王安忆是个高产作家,其创作不仅高产而且有质量,因而吸引了许多评论者的目光,但对王安忆小说创作进行总体研究难度甚大。将王安忆小说文本的叙事修辞与作家的叙事理念相结合,在对其小说文本的叙事探究中注入修辞分析的元素,从修辞对话的层面阐释其小说创作,不失为一个新的视角。     

论从民俗文化视角研究莫言小说的意义

莫言小说创作深受民俗文化的影响。民俗文化既是莫言小说创作的素材,又是莫言小说创作的源泉。因此,从民俗文化角度研究莫言小说创作具有非常重要的意义:从民俗文化的视角探讨莫言小说的创作,可以拓宽莫言小说研究的视野;通过揭示民俗文化对莫言的影响,探索莫言小说创作的源泉;莫言清醒的民俗学意识影响和制约着他的小说理论和创作思维,决定着小说的民俗化倾向;通过分析民俗文化在莫言小说中的影响、表现及其作用,探讨莫言小说中的意象所蕴涵的象征意蕴。     

台湾都市文学与海派文学

本文以林燿德和施蛰存开启的台湾都市文学与海派文学的对话为契机,探讨海峡两岸都市文学的隔海传承与变异。30年代上海新感觉派将都市文化的殖民地摩登属性推向顶峰;40年代的海派作家还原出一个琐碎的市民都市空间;台湾新世代作家则塑造了一个集民间、私我和异彩文化等诸多因子交汇的都市场域,包容了更大的阐释空间。这些都市书写都以“感觉”为媒介,借鉴蒙太奇手段刻意颠覆故事情节的连贯性和人物性格的完整性,对欲望书写异乎寻常的关注,在小说的审美形态、叙述角度、结构方式、语言风格等方面,表现出特有的创新度和开放度。     

Illicit payments for illicit goods: noncontact drug distribution on Russian online drug marketplaces

The distribution or consumption of traditional drugs has become the subject of stringent penalties throughout most of the world and synthetic designer drugs have become the alternative. Novel psychoactive substances, also called ‘legal highs’, are highly varied in terms of chemical composition. These substances are advertised and distributed as an alternative to traditional drugs on the Internet, making identification of new substances and enforcement difficult. For this article, we downloaded and analysed 28 Russian-language online drug marketplaces which distribute traditional and novel psychoactive substances. All marketplaces used a noncontact drug dealing method where the seller and the buyer communicate through the Internet to arrange for payment and delivery of drugs without meeting face-to-face. Geographic information, price, amount, substance type and payment method data were extracted. Findings indicate such marketplaces are able to operate due to the ability of their clients to pay anonymously with the virtual currencies – Qiwi and Bitcoin.     

结盟与分立:中国女性儿童小说作家笔下的母女关系

不同的“女儿经验”沉淀在女性作家的生命感受里,无论母亲在场或缺席,对母爱的眷恋与向往是相同的。但成长的躁动与“第二性”的反抗,使得女儿又要千方百计地脱离那个孕育她的母体,试图分娩一个新的自我。女性儿童小说作家以“女儿的经验”和母性的悲悯对母女关系投去了关注的目光与冷静的反思。     

无法安妥的灵魂--评析贾平凹小说的主人公形象

贾平凹关注着当今的乡村和城市,写了一系列游走于城乡之间的不安分的灵魂.他笔下的主人公游走于城乡之间,他们所处的世界对于他们来说始终是外来者,同时,他们是生活在芸芸众生中的孤独者,是一群"无法安妥的灵魂".     

“War Scar Literature” of Contemporary Japanese Literature——A Case Study of Social Novels of Toyoko Yamasaki

After the Second World War, some Japanese writers began to turn their writing focus to the War itself by referring to the literature and doing field studies. A rising number of realistic works, the so called “war scar literature” were then created focusing on war scenes, individual soldiers and social trends. One of the shared features of figures in these works was their real war experiences. Some figures, however, were presented too high profile, e.g, Tadashi Iki in Fumō Chitai. In such case, the literacy imagination tended to cover historical authenticity, which reflects a lack of complete and objective understanding of hurts brought about by the war. It may mislead the readers by forming a directed sense of nationalism. In this regard, literacy criticism is therefore necessary to help Japanese people to understand and reflect over the history.     

略论时代思潮对清末小说批评的影响

晚清是中国从传统向现代嬗变的转型期.这个时代的一个突出特点,是为了救亡图存、振兴中华,中国人开始大规模地向西方学习.于是,西学大量涌入中国,西方的影响笼罩中国.在这种背景下,清末的小说批评同样深受西学及其在中国形成的各种社会思潮的影响.清末许多人自觉或不自觉地运用来自西方的新的思想观念和思想方法,来解读中国的传统小说,正是这种影响的表征.