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Opioid use disorder (OUD) has become a considerable global public health challenge; however, potential medications for the management of OUD that are effective, safe, and nonaddictive are not available. Accumulating preclinical evidence indicates that antagonists of the dopamine D3 receptor (D3R) have effects on addiction in different animal models. We have previously reported that YQA14, a D3R antagonist, exhibits very high affinity and selectivity for D3Rs over D2Rs, and is able to inhibit cocaine- or methamphetamine-induced reinforcement and reinstatement in self-administration tests. In the present study, our results illustrated that YQA14 dose-dependently reduced infusions under the fixed-ratio 2 procedure and lowered the breakpoint under the progressive-ratio procedure in heroin self-administered rats, also attenuated heroin-induced reinstatement of drug-seeking behavior. On the other hand, YQA14 not only reduced morphine-induced expression of conditioned place preference but also facilitated the extinguishing process in mice. Moreover, we elucidated that YQA14 attenuated opioid-induced reward or reinforcement mainly by inhibiting morphine-induced up-regulation of dopaminergic neuron activity in the ventral tegmental area and decreasing dopamine release in the nucleus accumbens with a fiber photometry recording system. These findings suggest that D3R might play a very important role in opioid addiction, and YQA14 may have pharmacotherapeutic potential in attenuating opioid-induced addictive behaviors dependent on the dopamine system. [ABSTRACT FROM AUTHOR]

Multicomponent polymerizations (MCPs) are powerful tools to synthesize functional polymers with great structural diversity, low cost and high efficiency, which usually generate single polymer product. Herein, a robust one-pot diamines, CS2 and monoisocyanide-participated catalyst-free polymerization was developed at room temperature to produce polythiourea and thioformamide simultaneously in equal equivalent, which was featured with cheap monomers, simple operation and mild condition, affording various polythioureas with high Mws of up to 47500 g/mol in high yields of up to 98%. Polythioureas with varied chain composition and sequence-controlled structure could be synthesized in 62 g-scale from copolymerization or multicomponent tandem polymerization, enabling facile tuning of thermal property, crystallinity, mechanical property, and fluorescence. The abundant irregular hydrogen bonds endowed the polythioureas excellent glassy state self-healing property at room temperature or below 0 °C. This polymerization provided an efficient and economic approach to access functional polythioureas. [ABSTRACT FROM AUTHOR]

Biodegradable poly(lactic acid) (PLA)/poly(butylene adipate‐co‐terephthalate) (PBAT) blends and PLA/PBAT/Al2O3 nanocomposites were fabricated via solution blending. The influence of PBAT and Al2O3 content on the thermal stability, flexural properties, impact strength, and morphology of both the PLA/PBAT blends and the PLA/PBAT/Al2O3 nanocomposites were investigated. The impact strength of the PLA/PBAT/Al2O3 nanocomposites containing 5 wt% PBAT increased from 4.3 to 5.2 kJ/m2 when the Al2O3 content increased from 0 to 1 wt%. This represents a 62% increase compared to the impact strength of pristine PLA and a 20% increase compared to the impact strength of PLA/PBAT blends containing 5 wt% PBAT. Scanning electron microscopy imaging revealed that the Al2O3 nanoparticles in the PLA/PBAT/Al2O3 nanocomposites function as a compatibilizer to improve the interfacial interaction between the PBAT and the PLA matrix. [ABSTRACT FROM AUTHOR]

Abstract: Two facile approaches to two new series of the seven-rings fused benzodithiophene-based polycyclic aromatics are developed in good yields. [Copyright &y& Elsevier]

Abstract: A series of composite catalysts Ni/CeO2–ZrO2 were prepared via impregnation method with Ni as the active metal. A laboratory-scale fixed-bed reactor was employed to investigate the catalyst performance during hydrogen production by steam reforming bio-oil aqueous fraction. Effects of water-to-bio-oil ratio (W/B), reaction temperature, and the loaded weight of Ni and Ce on the hydrogen production performance of Ni/CeO2–ZrO2 catalysts were examined. The obtained results were compared with commercial nickel-based catalysts (Z417). The best performance of Ni/CeO2–ZrO2 catalyst was observed when the Ni and Ce loaded weight were 12% and 7.5% respectively. At W/B = 4.9, T = 800 °C, H2 yield reaches the highest of 69.7% and H2 content of 61.8% were obtained. Under the same condition, H2 yield and H2 content were higher than commercial nickel-based catalysts (Z417). [ABSTRACT FROM AUTHOR]

Since end-stage renal disease leads to a variety of problems such as disability,reduced quality of life,and mental and psychological disorders,it has become a serious public health problem around the globe.Renal palliative care integrates palliative care philosophy in the care for patients with end-stage renal disease.As a planned,comprehensive,patient-centered care,renal palliative care focuses on the patient's symptoms and needs,aiming to reduce the suffering throughout the course of the disease,including but not limited to end-of-life care.This study reports the palliative care practice for a patient on maintenance dialysis in the Blood Purification Center of Peking Union Medical College Hospital and reviews the present situation of palliative care in end-stage renal disease.

Objective: To investigate the regulation of calcineurin (CaN) by endoplasmic reticulum stress (ERS) in podocytes in vitro and in vivo at the stage microalbuminuria in diabetic nehropathy (DN)., Methods: The urinary albumin excretions of C57BLKS/J (Lepr) db/db and db/m mice at the ages of 6, 9, and 12 weeks were measured. The expressions of CaN and synaptopodin of these mice were observed. In immortalized mouse podocytes, the expression of podocyte CaN incubated with different concentrations of paltimate was quantitatively determined by real-time PCR. The changes of CaN incubated with paltimate with or without ursodeoxy-cholic acid (UDCA) were analyzed by confocal microscopy and Western blotting., Results: As urine protein increased, the expression of CaN was enhanced and the expression of synaptopodin was reduced in early stage DN db/db mice potocytes. In immortalized mouse podocytes, as the concentrations of palmitate increased, CaN mRNA increased. By confocal microscopy, the fluorescence intensity of CaN increased in palmitate treatment group. After co-incubation with palmitate and UDCA, the fluorescence intensity decreased. The similar results were shown by Western blotting., Conclusion: At the stage of microalbuminuria in DN, ERS in podocytes up-regulates the expression of CaN.

Objective: To investigate partial anomalous pulmonary venous connection (PAPVC) with echocardiography., Methods: The right ventricular volume overload was detected by routine echocardiography in 37 child patients, who underwent further echocardiography to find the abnormal locations of pulmonary vein opening at superior, inferior vena cava and right atrium. The ultrasound results were compared with surgical findings., Results: In 30 patients the ultrasound diagnosis was consistent with surgery results, 7 were misdiagnosed by ultrasound with a detective rate of 81.1 %. All 37 PAPVC patients presented varying degrees of right heart enlargement; PAPVC combined with atrial septal defect (ASD) was found in 34 cases., Conclusion: The possibility of PAPVC should be considered when unexplained right heart volume overload was detected by echocardiography. Superior, inferior vena cava and right atrium should be inspected when the pulmonary veins were not seen in echocardiography.

Objective: Brucine was encapsulated into stealth liposomes using the ammonium sulfate gradient method to improve therapeutic index., Materials and Methods: Four brucine stealth liposomal formulations were prepared, which were made from different phosphatidylcholines (PCs) with different phase transition temperatures (T(m)). The PCs used were soy phosphatidylcholine (SPC), dipalmitoyl phosphatidylcholine (DPPC), hydrogenated soy phosphatidylcholine (HSPC), and distearoyl phosphatidylcholine (DSPC). The stabilities, pharmacokinetics, and toxicities of these liposomal formulations were evaluated and compared., Results: Size, zeta potential, and entrapment efficiency of brucine-loaded stealth liposomes (BSL) were not influenced by PC composition. In vitro release studies revealed that drug release rate increased with decreased T(m) of PCs, especially with the presence of rat plasma. After intravenous administration, the area under the curve (AUC) values of BSL-SPC, BSL-DPPC, BSL-HSPC, and BSL-DSPC in plasma were 7.71, 9.24, 53.83, and 56.83-fold as large as that of free brucine, respectively. The LD(50) values of brucine solution, BSL-SPC, BSL-DPPC, BSL-HSPC, and BSL-DSPC following intravenous injection were 13.17, 37.30, 37.69, 51.18, and 52.86 mg/kg, respectively. It was found in calcein retention experiments that the order of calcein retention in rat plasma was SPC < DPPC << HSPC < DSPC stealth liposomes., Conclusion: PC composition could exert significant influence on the stabilities, pharmacokinetics, and toxicities of brucine-loaded stealth liposomes. DSPC or HSPC with T(m) above 50°C should be used to prepare the stealth liposomal formulation for the intravenous delivery of brucine. However, it was found in the present paper that the pharmacokinetics and toxicity of BSL were not influenced by the PC composition when the T(m) of the PC was in the range of -20°C to 41°C.