Results 51 to 60 of about 40,056 (270)

Pharmacokinetics and pharmacodynamics of intravenous and oral (S)‐ketamine: Investigating metabolite contribution to subjective effects

British Journal of Clinical Pharmacology, EarlyView.
Aims Oral administration of (S)‐ketamine for treatment‐resistant depression (TRD), as alternative to the registered intranasal or off‐label intravenous administrations, has high potential. However, it is characterized by an extensive first‐pass metabolism, resulting in low (S)‐ketamine exposure and high levels of active metabolites, including (S ...
Marije E. Otto, Gabriël E. Jacobs, Joost C. van Mechelen, Laura G. J. M. Borghans, Johan G. C. van Hasselt, Linda B. S. Aulin   +5 more
wiley   +1 more source

Polyunsaturated fatty acids inhibit a pentameric ligand-gated ion channel through one of two binding sites

eLife, 2022
Polyunsaturated fatty acids (PUFAs) inhibit pentameric ligand-gated ion channels (pLGICs) but the mechanism of inhibition is not well understood. The PUFA, docosahexaenoic acid (DHA), inhibits agonist responses of the pLGIC, ELIC, more effectively than ...
Noah M Dietzen, Mark J Arcario, Lawrence J Chen, John T Petroff II, K Trent Moreland, Kathiresan Krishnan, Grace Brannigan, Douglas F Covey, Wayland WL Cheng   +8 more
doaj   +1 more source

Nicotine Suppresses Human Memory Th Cell Subsets With Preferential Effects on Central Memory Th Cells in an α7 Nicotinic Acetylcholine Receptor-Dependent Manner. [PDF]

Eur J Immunol
Human memory Th cells were separated into Tcm (CD45RO+ CD62L+) and Tem (CD45RO+ CD62L−). Nicotine preferentially suppressed Th1‐, Th2‐, Th17‐, and Tfh‐associated programs in Tcm via an α7nAChR‐dependent mechanism, with minimal effect in Tem. ABSTRACT Memory T helper (Th) cells sustain protective recall responses but can also drive chronic inflammation,
Gholizadeh F, Hajiaghayi M, Rahbari N, Choi JS, Heidt S, Como A, Kazerouni M, Kargar M, Pinard-LaRoche A, Shih SCC, Darlington PJ.   +10 more
europepmc   +2 more sources

Structurally similar allosteric modulators of α7 nicotinic acetylcholine receptors exhibit five distinct pharmacological effects. [PDF]

, 2015
Activation of nicotinic acetylcholine receptors (nAChRs) is associated with the binding of agonists such as acetylcholine to an extracellular site that is located at the interface between two adjacent receptor subunits.
D'Oyley, JM, Dhankher, P, Gill-Thind, JK, Millar, NS, Sheppard, TD   +4 more
core  

Cholinergic modulation of dopamine overflow in the rat neostriatum: A fast cyclic voltammetric study in vitro [PDF]

, 1994
Stimulus-evoked dopamine overflow in rat neostriatal slices was determined using fast cyclic voltammetry. The dopamine efflux induced by intrastriatal stimulation increased with stimulus intensity and was found to be enhanced by more than 100% upon ...
Kudernatsch, Martina, Sutor, Bernd
core   +1 more source

Dried blood spot analysis in antidoping: Technical challenges, analytical advances, and future perspectives

Bulletin of the Korean Chemical Society, EarlyView.
Dried blood spot (DBS) analysis enables minimally invasive blood collection with strong analyte stability and simplified logistics, supporting anti‐doping applications beyond traditional matrices. Recent advances address hematocrit, volume variability, and matrix effects while expanding coverage to steroid esters, World Anti‐Doping Agency‐listed ...
Jihyun Yoon, Jiyeong Hong, Hanbin Oh, Chi Hwan Lee, Ki Hun Kim   +4 more
wiley   +1 more source

Epibatidine Induces Long-Term Potentiation (LTP) via Activation of α4β2 Nicotinic Acetylcholine Receptors (nAChRs) In Vivo in the Intact Mouse Dentate Gyrus: Both α7 and α4β2 nAChRs Essential to Nicotinic LTP

Journal of Pharmacological Sciences, 2003
: Activation of nicotinic acetylcholine receptors (nAChRs) induces nocotinic long-term potentiation (LTPn) in vivo in the mouse dentate gyrus. We have found that α4β2 nAChRs activated by epibatidine induce LTPn, the full size of which requires the ...
Shogo Matsuyama, Akira Matsumoto
doaj   +1 more source

Neurotransmitter-gated ion channels at fast chemical synapses: from structure to pathology [PDF]

, 2005
Fil: Bouzat, Cecilia Beatriz. Consejo Nacional de Investigaciones Científicas y Técnicas. Centro Científico Tecnológico Conicet - Bahía Blanca. Instituto de Investigaciones Bioquímicas de Bahía Blanca. Universidad Nacional del Sur.
Bouzat, Cecilia Beatriz
core  

Hydrocarbon molar water solubility predicts NMDA vs. GABAA receptor modulation. [PDF]

, 2014
BackgroundMany anesthetics modulate 3-transmembrane (such as NMDA) and 4-transmembrane (such as GABAA) receptors. Clinical and experimental anesthetics exhibiting receptor family specificity often have low water solubility. We hypothesized that the molar
Brosnan, Robert J, Pham, Trung L
core   +2 more sources

Atypical nicotinic agonist bound conformations conferring subtype selectivity [PDF]

Proceedings of the National Academy of Sciences, 2008
The nicotinic acetylcholine (ACh) receptor (nAChR) plays a crucial role in excitatory neurotransmission and is an important target for drugs and insecticides. Diverse nAChR subtypes with various subunit combinations confer differential selectivity for nicotinic drugs.
Motohiro, Tomizawa, David, Maltby, Todd T, Talley, Kathleen A, Durkin, Katalin F, Medzihradszky, Alma L, Burlingame, Palmer, Taylor, John E, Casida   +7 more
openaire   +2 more sources