A series of 1-aryl-2-(((6-aryl)pyrimidin-4-yl)amino)ethanols have been found to be competitive inhibitors of fatty acid amide hydrolase (FAAH). One member of this class, JNJ-40413269, was found to have excellent pharmacokinetic properties, demonstrated robust central target engagement, and was efficacious in a rat model of neuropathic pain.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmcl.2014.01.064DOI Listing

Publication Analysis

Top Keywords

1-aryl-2-6-arylpyrimidin-4-ylaminoethanols competitive
8
competitive inhibitors
8
inhibitors fatty
8
fatty acid
8
acid amide
8
amide hydrolase
8
hydrolase series
4
series 1-aryl-2-6-arylpyrimidin-4-ylaminoethanols
4
hydrolase faah
4
faah member
4

Similar Publications

Sterilization and Filter Performance of Nano- and Microfibrous Facemask Filters - Electrospinning and Restoration of Charges for Competitive Sustainable Alternatives.

Macromol Rapid Commun

December 2024

Empa, Swiss Federal Laboratories for Materials Science and Technology, Laboratory for Biomimetic Membranes and Textiles, St. Gallen, 9014, Switzerland.

Facemask materials have been under constant development to optimize filtration performance, wear comfort, and general resilience to chemical and mechanical stress. While single-use polypropylene meltblown membranes are the established go-to material for high-performing mask filters, they are neither sustainable nor particularly resistant to sterilization methods. Herein an in-depth analysis is provided of the sterilization efficiency, filtration efficiency, and breathing resistance of selected aerosol filters commonly implemented in facemasks, with a particular focus on the benefits of nanofibrous filters.

View Article and Find Full Text PDF

Control charts are commonly used for process monitoring under the assumption that the variable of interest follows a normal distribution. However, this assumption is frequently violated in real-world applications. In this study, we develop an adaptive control chart based on the exponentially weighted moving average (EWMA) statistic to monitor irregular variations in the mean of the Truncated Transmuted Burr-II (TTB-II) distribution, employing Hastings approximation for normalization.

View Article and Find Full Text PDF

Allopregnanolone (Allo) is a positive allosteric modulator of the GABA receptor, and amiloride (Ami) is a competitive antagonist of the GABA receptor. The purpose of this work was to study the combined effect of Allo and Ami on functional activity of GABA receptor. The GABA-induced chloride current (I) was measured in isolated Purkinje cells of rat cerebellum using the patch-clamp technique and a system of fast application.

View Article and Find Full Text PDF

Using a unique dataset on the performance of soccer players in China (retrieved from 632 matches involving 24 teams during the 2014 to 2016 seasons), we investigate the effect of air pollution on different performance indicators that rely on different mixtures of the physical and cognitive inputs of players. To ensure a causal interpretation, we implement an instrumental variable (IV) approach using thermal inversion as the instrument for air pollution. We found that players' performance indicators, especially those more related to cognitive factors, are more strongly influenced by air pollution.

View Article and Find Full Text PDF

Role of horizontal gene transfer and cooperation in rhizosphere microbiome assembly.

Braz J Microbiol

December 2024

Department of Soil Science, "Luiz de Queiroz" College of Agriculture, University of São Paulo, Pádua Dias Av, 11, Piracicaba, SP, 13418-900, Brazil.

Microbes employ a variety of mechanisms, encompassing chemical signaling (e.g., quorum-sensing molecules) and genetic processes like horizontal gene transfer (HGT), to engage in interactions.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!