Discovery of aryl-biphenyl-2-ylmethylpiperazines as novel scaffolds for 5-HT7 ligands and role of the aromatic substituents in binding to the target receptor

Y Kim, J Kim, J Tae, BL Roth, H Rhim, G Keum… - Bioorganic & medicinal …, 2013 - Elsevier
It has been reported that 5-HT7 receptors are promising targets of depression and
neuropathic pain. 5-HT7 receptor antagonists have exhibited antidepressant-like profiles …

Identification of ginsenoside interaction sites in 5-HT3A receptors

BH Lee, JH Lee, SM Lee, SM Jeong, IS Yoon, JH Lee… - …, 2007 - Elsevier
We previously demonstrated that 20 (S)-ginsenoside Rg3 (Rg3), one of the active
components of Panax ginseng, non-competitively inhibits 5-HT3A receptor channel activity …

Extended N-Arylsulfonylindoles as 5-HT6 Receptor Antagonists: Design, Synthesis & Biological Evaluation

G Vera, CF Lagos, S Almendras, D Hebel, F Flores… - Molecules, 2016 - mdpi.com
Based on a known pharmacophore model for 5-HT6 receptor antagonists, a series of novel
extended derivatives of the N-arylsulfonyindole scaffold were designed and identified as a …

Anti-5-hydroxytryptamine3 effect of galanolactone, diterpenoid isolated from ginger

Q HUANG, M IWAMOTO, S AOKI… - Chemical and …, 1991 - jstage.jst.go.jp
抄録 It has been reported that an acetone extract of ginger and its fractions have anti-5-HT (5-
hydroxytryptamine; serotonin) effects. In the present study, guinea pig ileum, rat stomach …

Novel potent 5-HT3 receptor ligands based on the pyrrolidone structure: synthesis, biological evaluation, and computational rationalization of the ligand–receptor …

A Cappelli, M Anzini, S Vomero, L Mennuni… - Bioorganic & medicinal …, 2002 - Elsevier
Novel conformationally constrained derivatives of classical 5-HT3 receptor antagonists were
designed and synthesized with the aim of probing the central 5-HT3 receptor recognition site …

Pharmacophore Directed Screening of Agonistic Natural Molecules Showing Affinity to 5HT2C Receptor

GK Veeramachaneni, VBSC Thunuguntla, M Bhaswant… - Biomolecules, 2019 - mdpi.com
Obesity prevalence continues to be a foremost health concern across the globe leading to
the development of major health risk conditions like type II diabetes, hyperlipidemia …

Discovery of novel potent and selective ligands for 5-HT2A receptor with quinazoline scaffold

X Deng, L Guo, L Xu, X Zhen, K Yu, W Zhao… - Bioorganic & Medicinal …, 2015 - Elsevier
A series of compounds with quinazoline scaffold were designed, synthesized and evaluated
as novel potent 5-HT 2A receptor ligands. N-(4-Chlorophenyl)-2-(piperazin-1-yl) quinazolin …

New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263

E Ofori, EK Onyameh, UM Gonela, C Voshavar… - European journal of …, 2021 - Elsevier
We have previously reported that dual 5-HT 1A and 5-HT 7 receptor ligands might find utility
as treatment options for various CNS related conditions including cognitive and anxiolytic …

SB-656104-A: a novel 5-HT7 receptor antagonist with improved in vivo properties

IT Forbes, S Douglas, AD Gribble, RJ Ife… - Bioorganic & medicinal …, 2002 - Elsevier
A focused SAR study around the previously reported selective 5-HT7 receptor antagonist,
SB-269970-A has resulted in the identification of a structurally related analogue having an …

Novel quinazolinone derivatives as 5-HT7 receptor ligands

YH Na, SH Hong, JH Lee, WK Park, DJ Baek… - Bioorganic & medicinal …, 2008 - Elsevier
5-HT7 receptor antagonists generated antidepressant-like effects in animal model and the
involvement of the 5-HT7 receptor in other pathophysiological mechanisms such as …