Results 121 to 130 of about 1,677,689 (317)

Development of indole sulfonamides as cannabinoid receptor negative allosteric modulators [PDF]

, 2016
This Letter was supported by the Biotechnology and Biological Sciences Research Council (BBSRC) and the Scottish Universities Life Sciences Alliance (SULSA) in 2011Peer ...
Abdelrahman, Mostafa Hamed, Baillie, Gemma L., Greig, Iain R., Ross, Ruth A., Trembleau, Laurent   +4 more
core   +1 more source

Human phase‐I metabolism of three synthetic cannabinoids bearing a cumyl moiety and a cyclobutyl methyl or norbornyl methyl tail: Cumyl‐CBMEGACLONE, Cumyl‐NBMEGACLONE, and Cumyl‐NBMINACA

Drug Testing and Analysis, EarlyView.
The human phase‐I metabolism of three SCRAs bearing a cumyl moiety and a CBM or NBM tail, based on LC‐qToF‐MS data of authentic urine specimens. Abstract Synthetic cannabinoid receptor agonists (SCRAs) continue to show high prevalence on the new psychoactive substances drug market.
Arianna Giorgetti, Pietro Brunetti, Belal Haschimi, Benedikt Pulver, Jennifer Paola Pascali, Jan Riedel, Volker Auwärter   +6 more
wiley   +1 more source

Pharmacology of DB844, an orally active aza analogue of pafuramidine, in a monkey model of second stage human African trypanosomiasis [PDF]

, 2012
Novel drugs to treat human African trypanosomiasis (HAT) are still urgently needed despite the recent addition of nifurtimox-eflornithine combination therapy (NECT) to WHO Model Lists of Essential Medicines against second stage HAT, where parasites have ...
Boykin, D. W., Brun, R., Ching, S., Denton, C. L., Hall, J. E., Kagira, J. M., Mdachi, R. E., Murilla, G. A., Paine, M. F., Thuita, J. K., Tidwell, R. R., Wang, M. Z.   +11 more
core   +5 more sources

Annual Banned‐Substance Review 17th Edition—Analytical Approaches in Human Sports Drug Testing 2023/2024

Drug Testing and Analysis, EarlyView.
Scenarios of drug exposure and administration as well as detection assays for drugs and methods of sports doping published between 2023 and 2024 are critically reviewed and evaluated in context with the Prohibited List 2024 as established by the World Anti‐Doping Agency.
Mario  Thevis, Tiia  Kuuranne, Hans  Geyer   +2 more
wiley   +1 more source

Hydroxymethylglutaryl CoA reductase and the modulation of microsomal cholesterol content by the nonspecific lipid transfer protein.

Journal of Lipid Research, 1984
The influence of membrane cholesterol content on 3-hydroxy-3-methylglutaryl CoA reductase (HMG-CoA reductase, EC 1.1.1.34) in rat liver microsomes was investigated.
G P van Heusden, K W Wirtz
doaj  

Identification and Investigation of the Intrinsic Receptor Activation Potential and Metabolization of the New Oxo‐Pyridyl Synthetic Cannabinoid Receptor Agonist CH‐FUBBMPDORA

Drug Testing and Analysis, EarlyView.
Another Chinese generic ban‐evading SCRA, CH‐FUBBMPDORA, has emerged. This study reports its first identification in Europe, its analytical characterization (NMR, Raman, FTIR, GC–MS, and HRMS), its cannabinoid activation potential in a βarr2 recruitment assay, and its metabolization profile.
Marie H. Deventer, Maria Carmela Emanuele, Brianna N. Stang, Katleen Van Uytfanghe, Jessica Masson, Xavier Bouvot, Catherine Lamoureux, Alessandro Proposito, Fabiano Reniero, Margaret V. Holland, Alex J. Krotulski, Luisa Mannina, Christophe P. Stove, Claude Guillou   +13 more
wiley   +1 more source

Exchange of phospholipid classes between liver microsomes and plasma: comparison of rat, rabbit, and guinea pig

Journal of Lipid Research, 1971
Rat and guinea pig liver microsomes labeled with phospholipid 32P were incubated with rat, guinea pig, and rabbit plasma in a KC1–Tris–EDTA buffer. A net transfer of microsomal phosphatidylcholine and phosphatidylethanolamine to plasma was observed.
D.B. ZILVERSMIT
doaj  

EROD and MROD as Markers of Cytochrome P450 1A Activities in Hepatic Microsomes from Entire and Castrated Male Pigs

Sensors, 2009
In the present study, we characterized the kinetic parameters of 7-ethoxy-resorufin O-deethylation (EROD) and 7-methoxyresorufin O-demethylation (MROD) in hepatic microsomes from entire and castrated male pigs.
Vladimir Zlabek, Galia Zamaratskaia
doaj   +1 more source

Gel Electrophoretic Detection of Black Market ACE‐031

Drug Testing and Analysis, EarlyView.
This article presents a study on black market ACE‐031 products and their detection by gel‐electrophoresis and Western blotting. Of the 14 tested products, only 12 contained an ACVR2B‐immunoreactive protein. However, mass spectrometry revealed that the products did not contain the ACVR2B‐Fc fusion protein ACE‐031 but instead the full‐length human ...
Christian Reichel, Thomas Filip, Günter Gmeiner, Mario Thevis   +3 more
wiley   +1 more source

Protein targets of reactive electrophiles in human liver microsomes.

Chemical Research in Toxicology, 2007
Liver microsomes are widely used to study xenobiotic metabolism in vitro, and covalent binding to microsomal proteins serves as a surrogate marker for toxicity mediated by reactive metabolites.
N. Shin, Qinfeng Liu, Sheryl L. Stamer, D. Liebler   +3 more
semanticscholar   +1 more source