Recent advances with 5‐HT3 modulators for neuropsychiatric and gastrointestinal disorders

R Juza, P Vlcek, E Mezeiova, K Musilek… - Medicinal research …, 2020 - Wiley Online Library
Abstract Serotonin (5‐hydroxytryptophan [5‐HT]) is a biologically active amine expressed in
platelets, in gastrointestinal (GI) cells and, to a lesser extent, in the central nervous system …

Structural basis for partial agonism in 5-HT3A receptors

K Felt, M Stauffer, L Salas-Estrada, PR Guzzo… - Nature Structural & …, 2024 - nature.com
Abstract Hyperactivity of serotonin 3 receptors (5-HT3R) underlies pathologies associated
with irritable bowel syndrome and chemotherapy-induced nausea and vomiting. Setrons, a …

Development of a highly potent analogue and a long-acting analogue of oxytocin for the treatment of social impairment-like behaviors

W Ichinose, SM Cherepanov… - Journal of medicinal …, 2019 - ACS Publications
The nonapeptide hormone oxytocin (OT) has pivotal brain roles in social recognition and
interaction and is thus a promising therapeutic drug for social deficits. Because of its peptide …

[HTML][HTML] Merging cultures and disciplines to create a drug discovery ecosystem at Virginia commonwealth university: Medicinal chemistry, structural biology, molecular …

GE Kellogg, Y Cen, M Dukat, KC Ellis, Y Guo, J Li… - SLAS Discovery, 2023 - Elsevier
Abstract The Department of Medicinal Chemistry, together with the Institute for Structural
Biology, Drug Discovery and Development, at Virginia Commonwealth University (VCU) has …

High-affinity sigma-1 (σ1) receptor ligands based on the σ1 antagonist PB212

M Niso, PD Mosier, R Marottoli, S Ferorelli… - Future Medicinal …, 2019 - Taylor & Francis
Aim: The σ1 receptor is a druggable target involved in many physiological processes and
diseases. To clarify its physiology and derive therapeutic benefit, nine analogs based on the …

N1H- and N1-Substituted Phenylguanidines as α7 Nicotinic Acetylcholine (nACh) Receptor Antagonists: Structure–Activity Relationship Studies

OI Alwassil, S Khatri, MK Schulte… - ACS Chemical …, 2021 - ACS Publications
We previously reported that N-(3-chlorophenyl) guanidine (1) represents a novel α7 nicotinic
ACh (nACh) receptor antagonist chemotype. In the present study, a small series of …

[PDF][PDF] Rapidly Trading Down Depression's 3 Pillars to 5HT3-Receptors Through ECT or Psilocybin?

G RS Treviranus - Psychiatria Danubina, 2024 - hrcak.srce.hr
Depression astonishingly can be stopped instantly by electrotherapies or through some
psychedelics like psilocybin. In explaining this, the traditional approaches to their …

“Methylene Bridge” to 5-HT3 Receptor Antagonists: Conformationally Constrained Phenylguanidines

AS Abdelkhalek, GS Alley, OI Alwassil… - ACS chemical …, 2018 - ACS Publications
Arylguanidines, depending upon their aromatic substitution pattern, display varying actions
at 5-HT3 receptors (eg, partial agonist, agonist, superagonist). Here, we demonstrate that …

Computational analysis of non-competitive antagonist arylguanidine-α7 nAChR complexes

OI Alwassil, GR Abdrakhmanova, M Dukat - Journal of Molecular Graphics …, 2021 - Elsevier
Abstract meta-Chlorophenylguanidine (1) is a non-competitive α7 nicotinic acetylcholine
receptor (nAChR) antagonist. Here we examined the hydrogen bond donor role of the …

Development of a treatment planning algorithm for peptide-receptor radionuclide therapy considering multiple tumour lesions and organs at risk

LD Jiménez Franco - 2018 - archiv.ub.uni-heidelberg.de
Peptide-receptor radionuclide therapy (PRRT) is a modality of molecular radiotherapy in
which patients are administered with radiolabelled peptides targeting peptide-receptors …