Structural determinants for activity of the antidepressant vortioxetine at human and rodent 5-HT3 receptors

U López-Sánchez, LJ Munro, LK Ladefoged… - Nature structural & …, 2024 - nature.com
Vortioxetine (VTX) is a recently approved antidepressant that targets a variety of serotonin
receptors. Here, we investigate the drug's molecular mechanism of operation at the …

High-resolution structures of multiple 5-HT3AR-setron complexes reveal a novel mechanism of competitive inhibition

S Basak, A Kumar, S Ramsey, E Gibbs, A Kapoor… - Elife, 2020 - elifesciences.org
Serotonin receptors (5-HT3AR) play a crucial role in regulating gut movement, and are the
principal target of setrons, a class of high-affinity competitive antagonists, used in the …

Phylogenetic analyses of 5-hydroxytryptamine 3 (5-HT3) receptors in Metazoa

STRB Rao, I Turek, HR Irving - Plos one, 2023 - journals.plos.org
The 5-hydroxytrptamine 3 (5-HT3) receptor is a member of the'Cys-loop'family and the only
pentameric ligand gated ion channel among the serotonin receptors. 5-HT3 receptors play …

Conformational dynamics of a nicotinic receptor neurotransmitter site

M Singh, DC Indurthi, L Mittal, A Auerbach, S Asthana - eLife, 2024 - elifesciences.org
Agonists enhance receptor activity by providing net-favorable binding energy to active over
resting conformations, with efficiency (η) linking binding energy to gating. Previously, we …

Conformational decoupling in acid-sensing ion channels uncovers mechanism and stoichiometry of PcTx1-mediated inhibition

SA Heusser, CB Borg, JM Colding, SA Pless - Elife, 2022 - elifesciences.org
Acid-sensing ion channels (ASICs) are trimeric proton-gated cation channels involved in fast
synaptic transmission. Pharmacological inhibition of ASIC1a reduces neurotoxicity and …

Mapping the molecular motions of 5-HT3 serotonin-gated channel by Voltage-Clamp Fluorometry

L Peverini, S Shi, K Medjebeur, PJ Corringer - Elife, 2024 - elifesciences.org
The serotonin-gated ion channel (5-HT 3 R) mediates excitatory neuronal communication in
the gut and the brain. It is the target for setrons, a class of competitive antagonists widely …

Combined In-silico and Experimental Approach to Understanding 5-hydroxytryptamine 3 (5-HT3) Receptor Expression.

SR Tata - 2023 - opal.latrobe.edu.au
Combined In-silico and Experimental Approach to Understanding 5-hydroxytryptamine 3 (5-HT3)
Receptor Expression. Page 1 Combined In-silico and Experimental Approach to Understanding …

Factores extrínsecos condicionantes de la función de receptores Cys-loop: Relevancia fisiológica y patológica

C Fabiani - 2021 - repositoriodigital.uns.edu.ar
Dentro de la superfamilia de los canales iónicos activados por ligando (LGIC) se encuentra
la familia de los receptores Cys-loop que incluye a canales catiónicos, como los receptores …