The recent discovery of novel high-affinity and selective dopamine D3 receptor (DA D3R) antagonists and partial agonists has provided tools with which to further elucidate the role DA D3R plays in substance abuse. The present study was conducted to evaluate the transport, metabolism, pharmacokinetics, and brain uptake of the DA D3R-selective fluorenyl amides, NGB 2904 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-9H-fluorene-2-carboxamide] fumarate) and JJC 4-077 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)-3-hydroxybutyl)-9H-fluorene-2-carboxamide hydrochloride], and the 2-pyridylphenyl amides, CJB 090 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butyl)-4-(pyridine-2-yl)benzamide hydrochloride] and PG 01037 [N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)-trans-but-2-enyl)-4-(pyridine-2-yl)benzamide hydrochloride], all of which have been studied in animal models of psychostimulant abuse. Additional screening with a panel of human and rat Supersomes was performed for NGB 2904 and PG 01037. Drugstimulated ATPase activation assays and bidirectional transport and efflux assays were used to test for substrate specificity of NGB 2904 and PG 01037 for human and rat efflux transporters. All compounds exhibited moderate elimination half-lives, ranging from 1.49 to 3.27 h, and large volumes of distribution (5.95-14.19 l/kg). The brain-to-plasma ratios ranged from 2.93 to 11.81 and were higher than those previously reported for cocaine. Brain exposure levels of NGB 2904 and PG 01037 were significantly reduced after intraperitoneal administration compared with intravenous administration. The metabolism of these compounds was mediated primarily by CYP3A subfamilies. PG 01037 was a Pglycoprotein-transported substrate. Higher doses of these compounds are often required for in vivo action, suggesting decreased bioavailability via extravascular administration that may be attributed to high drug efflux and hepatic metabolism. These studies provide important preclinical information for optimization of next-generation D3R selective agents for the treatment of drug addiction.Cocaine and methamphetamine are potent central nervous system stimulants known for their abuse potential and addictive liability. Cocaine's effects are shorter than that of methamphetamine (half-life 0.5 h for cocaine versus 11 h for methamphetamine), making its high abuse liability and chronic use a significant health concern. Despite numerous controlled studies of more than 60 medications, there are currently no conclusive data to support the efficacy of any particular pharmacological agent to treat cocaine abuse (Ross and Peselow, 2009).
We report on the effects of surface treatment with N 2 , O 2 , and N 2 O plasmas on the work function of indium-tin oxide (ITO). UV photoelectron spectroscopy (UPS) showed that the work function on the ITO surface treated with N 2 O plasma increased more than that on the samples treated with N 2 or O 2 plasma. X-ray photoelectron spectroscopy (XPS) showed that the intensity of the O-O bonding peak at 532.3 eV markedly increased owing to the adsorption of O À ions on the ITO surface from breaking bonds in N 2 O gas by the plasma. The dipole layer formed by O À ions on the ITO surface increases the work function of ITO. Accordingly, N 2 O plasma treatment leads to a reduction of the potential barrier between the Fermi level of ITO and the highest occupied molecular orbital (HOMO) level of an organic layer when ITO is used as an anode for organic light-emitting devices (OLEDs) and related devices. Therefore, N 2 O plasma treatment enhances the hole-injection properties from the ITO thin film to the organic layer.
We report a highly effective surface treatment method for planar-type Sb2S3 solar cells by employing a Cs2CO3-modified compact TiO2 (c-TiO2) electron transport layer. It is found that surface treatment using a Cs2CO3 solution can shift the work function of c-TiO2 upward and reduce its surface roughness. As a result, compared with the power conversion efficiency of untreated solar cells, that of the treated solar cells with a glass/FTO/c-TiO2(/Cs2CO3)/Sb2S3/P3HT/Au structure significantly improved from 2.83 to 3.97%. This study demonstrates that the introduction of Cs2CO3 on a c-TiO2 layer is a simple and efficient way to adjust the work function of the electron transport layer and fabricate high-performance planar-type Sb2S3 solar cells.
All-inorganic metal halide perovskite nanocrystals (IPeNCs) have become one of the most promising luminescent materials for next-generation display and lighting technology owing to their excellent color expression ability. However, research on IPeNCs with stable blue emission is limited. In this paper, we report stable blue emissive all-bromide IPeNCs obtained through a modified ligand-assisted reprecipitation method using an ultraviolet (UV)-curable prepolymer as the anti-solvent at a low temperature. We found that the blue emission originates from quantum-confined CsPbBr3 nanoparticles formed together with the colorless wide-bandgap Cs4PbBr6 nanocrystals. When the temperature of the prepolymer was increased from 0 to 50 °C, CsPbBr3 nanoparticles became larger and more crystalline, thereby altering their emission color from blue to green. The synthesized all-bromide blue-emitting IPeNC solution remained stable for over 1 h. It also remained stable when it was mixed with the green-emitting IPeNC solution. By simply exposing the as-synthesized IPeNC–prepolymer solutions to UV light, we formed water-stable composite films that emitted red, green, blue, and white colors. We believe that this synthetic method can be used to develop color-emitting composite materials that are highly suitable for application as the color conversion films of full-color liquid crystal display backlight systems and lighting applications.
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