From ab initio quantum mechanics to molecular neurobiology: A cation-pi binding site in the nicotinic receptor [PDF]
The nicotinic acetylcholine receptor is the prototype ligand-gated ion channel. A number of aromatic amino acids have been identified as contributing to the agonist binding site, suggesting that cation-pi interactions may be involved in binding the ...
Dougherty, Dennis A.+5 more
core
Monthly buprenorphine depot injection (SUBLOCADE®) for opioid use disorder during pregnancy
Abstract Background and Objectives Untreated opioid use disorder (OUD) in pregnancy is associated with adverse obstetrical outcomes, maternal morbidity, and maternal mortality. This article will inform clinicians about the use of monthly extended‐release buprenorphine (BUP‐XR, SUBLOCADE®) to treat OUD during pregnancy and postpartum.
Melinda Ramage+3 more
wiley +1 more source
Molecular dynamics simulations reveal the role of ceramicine B as novel PPARγ partial agonist against type 2 diabetes [PDF]
Peroxisome proliferator-activated receptors gamma (PPAR{\gamma}) are ligand-activated controllers of various metabolic actions and insulin sensitivity. PPAR{\gamma} is thus considered as an important target to treat type 2 diabetes. Available PPAR{\gamma} drugs (full agonists) have robust insulin-sensitizing properties but are accompanied by severe ...
arxiv
A weighted U statistic for association analysis considering genetic heterogeneity [PDF]
Converging evidence suggests that common complex diseases with the same or similar clinical manifestations could have different underlying genetic etiologies. While current research interests have shifted toward uncovering rare variants and structural variations predisposing to human diseases, the impact of heterogeneity in genetic studies of complex ...
arxiv +1 more source
A fluorophore attached to nicotinic acetylcholine receptor beta M2 detects productive binding of agonist to the alpha delta site [PDF]
To study conformational transitions at the muscle nicotinic acetylcholine (ACh) receptor (nAChR), a rhodamine fluorophore was tethered to a Cys side chain introduced at the beta-19' position in the M2 region of the nAChR expressed in Xenopus oocytes ...
Auyeung, Vincent C.+7 more
core
Tris+/Na+ permeability ratios of nicotinic acetylcholine receptors are reduced by mutations near the intracellular end of the M2 region [PDF]
Tris+/Na+ permeability ratios were measured from shifts in the biionic reversal potentials of the macroscopic ACh-induced currents for 3 wild- type (WT), 1 hybrid, 2 subunit-deficient, and 25 mutant nicotinic receptors expressed in Xenopus oocytes.
Cohen, Bruce N.+4 more
core +2 more sources
Compression‐Expansion: Miniaturization, Modularity, and Logistics Beyond Earth
ABSTRACT If the Cold War space race culminated in a return to Earth, at present we are experiencing a renewed interest in space. Drawing on fieldwork among people working in the space sector in Sweden, this article focuses on some of the imaginaries underpinning this resurgence and the contemporary commercialization of space. Specifically, I hone in on
Chakad Ojani
wiley +1 more source
Three major forms of the nicotinic agonist toxin anabaseine (cyclic iminium, cyclic imine and the monocationic open-chain ammonium-ketone) co-exist in almost equal concentrations at physiological pH.
Kristin Andrud+8 more
doaj +1 more source
Venomous secretions from marine snails of the Terebridae family target acetylcholine receptors [PDF]
Venoms from cone snails (Conidae) have been extensively studied during the last decades, but those from other members of the suborder Toxoglossa, such as of Terebridae and Turridae superfamilies attracted less interest so far. Here, we report the effects
Kauferstein, Silke+8 more
core +2 more sources
Using both in vitro (hippocampal synaptosomes in superfusion) and in vivo (microdialysis) approaches we investigated whether and to what extent β amyloid peptide 1-40 (Aβ 1-40) interferes with the cholinergic modulation of the release of glycine (GLY) in
Stefania eZappettini+7 more
doaj +1 more source