Results 101 to 110 of about 170,260 (319)

Opening a hydrophobic gate: the nicotinic acetylcholine receptor as an example [PDF]

open access: yesarXiv, 2009
To what extent must a hydrophobic gate expand for the channel to count as open? We address this question using the nicotinic acetylcholine receptor (nAChR) as the exemplar. The nAChR is an integral membrane protein which forms a cation selective channel gated by neurotransmitter binding to its extracellular domain.
arxiv  

A Phase 1 Randomized Study to Evaluate the Safety, Tolerability, and Pharmacokinetics of Single Escalating Oral Doses of Dordaviprone and the Effects of Food on the Bioavailability of Dordaviprone in Healthy Adult Subjects

open access: yesClinical Pharmacology in Drug Development, EarlyView.
Abstract Dordaviprone (ONC201) is a novel, small molecule imipridone with antitumor effects in glioma patients. This study evaluated the pharmacokinetics and safety of dordaviprone following single escalating doses (Part A), as a capsule content mixed with applesauce or Gatorade (sports drink) [Part B1]), and with or without food [Part B2].
Shamia L. Faison   +7 more
wiley   +1 more source

Proteomic profiling of impaired excitation–contraction coupling and abnormal calcium handling in muscular dystrophy

open access: yesPROTEOMICS, Volume 22, Issue 23-24, December 2022., 2022
Abstract The X‐linked inherited neuromuscular disorder Duchenne muscular dystrophy is characterised by primary abnormalities in the membrane cytoskeletal component dystrophin. The almost complete absence of the Dp427‐M isoform of dystrophin in skeletal muscles renders contractile fibres more susceptible to progressive degeneration and a leaky ...
Paul Dowling   +3 more
wiley   +1 more source

Rapid Analytical Method for Quantification of Gamma‐Hydroxybutyrate (GHB) in Hair by UPLC‐MS/MS

open access: yesDrug Testing and Analysis, EarlyView.
A rapid and simple UPLC‐MS/MS method for quantification of GHB in 10 mg of hair was developed. The method was satisfactorily validated, showing a linear range of 0.5–50 ng/mg, which allows us to quantify endogenous and exogenous GHB concentrations.
Miriam Blanco‐Ces   +5 more
wiley   +1 more source

Boundary lipids of the nicotinic acetylcholine receptor: spontaneous partitioning via coarse-grained molecular dynamics simulation [PDF]

open access: yesarXiv, 2018
Reconstituted nicotinic acetylcholine receptors (nAChRs) exhibit significant gain-of-function upon addition of cholesterol to reconstitution mixtures, and cholesterol affects organization of nAChRs within domain-forming membranes, but whether nAChR partitions to cholesterol-rich liquid-ordered ("raft" or $l_o$) domains or cholesterol-poor liquid ...
arxiv  

Waxy‐ or Putty‐Like Materials as a Novel Drug Preparation for Synthetic Cannabinoid Receptor Agonists: Detection in Prisons and In Vitro Cannabinoid Receptor Activity

open access: yesDrug Testing and Analysis, EarlyView.
Waxy‐ or putty‐like materials has emerged as a novel drug preparation for synthetic cannabinoids and other drugs in UK prisons. An in vitro CB1 bioassay was used to evaluate the CB1 activating potential of MDMB‐INACA and extracts from eight seized samples. MDMB‐INACA had moderate efficacy but low potency at CB1.
Axelle Timmerman   +9 more
wiley   +1 more source

Predicting Smoking Events with a Time-Varying Semi-Parametric Hawkes Process Model [PDF]

open access: yesarXiv, 2018
Health risks from cigarette smoking -- the leading cause of preventable death in the United States -- can be substantially reduced by quitting. Although most smokers are motivated to quit, the majority of quit attempts fail. A number of studies have explored the role of self-reported symptoms, physiologic measurements, and environmental context on ...
arxiv  

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

open access: yesDrug 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   +2 more
wiley   +1 more source

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