Quinazolindione derivatives as potent 5-HT3A receptor antagonists

BH Lee, MJ Choi, MN Jo, HJ Seo, SY Nah… - Bioorganic & medicinal …, 2009 - Elsevier
5-HT3A receptor antagonists have been used mainly for the treatment of nausea and
vomiting. These days, the antagonists are of special interest due to their therapeutic …

Synthesis and Characterization of 5-Hydroxy-2-(2-phenylethyl)chromone (5-HPEC) and Its Analogues as Non-nitrogenous 5-HT2B Ligands

DA Williams, SA Zaidi, Y Zhang - Journal of natural products, 2015 - ACS Publications
The involvement of the neurotransmitter serotonin (5-HT) in numerous physiological
functions is often attributed to the diversity of receptors with which it interacts. Ligands …

SAR-studies on the importance of aromatic ring topologies in search for selective 5-HT7 receptor ligands among phenylpiperazine hydantoin derivatives

J Handzlik, AJ Bojarski, G Satała, M Kubacka… - European Journal of …, 2014 - Elsevier
The current study is focused on newly developed phenylpiperazine derivatives of aromatic
methylhydantoin differing in mutual positions of methyl and phenyl moieties. The new …

An aqueous extract of Poncirus fructus activates the prokinetic activity of 5-HT receptor subtype 4 without hERG interaction

WS Shim, H Back, SW Jung, JW Kim, Y Jang… - Journal of …, 2010 - Elsevier
AIM OF THE STUDY: Poncirus fructus (PF)–also known as the dried, immature fruit of
Poncirus trifoliata (L.) Raf.(Rutaceae)–is a natural substance that has long been used for …

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 …

Arene-and quinoline-sulfonamides as novel 5-HT7 receptor ligands

P Zajdel, K Marciniec, A Maślankiewicz… - Bioorganic & medicinal …, 2011 - Elsevier
Novel arene-and quinolinesulfonamides were synthesized using different solutions and a
solid-support methodology, and were evaluated for their affinity for 5-HT1A, 5-HT2A, 5-HT6 …

Discovery of Benzamide Analogues as a Novel Class of 5‐HT3 Receptor Agonists

CG Jørgensen, B Frølund, J Kehler… - ChemMedChem, 2011 - Wiley Online Library
A 5‐HT3 receptor agonist based on a benzamide scaffold was identified in a screening of a
small commercial compound library, and an elaborate SAR study originating from this hit …

Synthesis and Pharmacological Characterization of Novel 6-Fluorochroman Derivatives as Potential 5-HT1A Receptor Antagonists

T Yasunaga, T Kimura, R Naito, T Kontani… - Journal of medicinal …, 1998 - ACS Publications
A series of novel 6-fluorochroman derivatives was prepared and evaluated as antagonists
for the 5-HT1A receptor. N-2-[[(6-Fluorochroman-8-yl) oxy] ethyl]-4-(4-methoxyphenyl) …

Mode of action of peppermint oil and (‐)‐menthol with respect to 5‐HT3 receptor subtypes: binding studies, cation uptake by receptor channels and contraction of …

K Heimes, F Hauk, EJ Verspohl - Phytotherapy Research, 2011 - Wiley Online Library
Peppermint oil (Mentha× piperita L.(Lamiaceae) has been shown to exert potent antiemetic
properties, but its mode of action has not yet been elucidated. Among its active constituents …

Mutations of arginine 222 in pre-transmembrane domain I of mouse 5-HT3A receptor abolish 20 (R)-but not 20 (S)-ginsenoside Rg3 inhibition of 5-HT-mediated ion …

BH Lee, JH Lee, IS Yoon, JH Lee, SH Choi… - Biological and …, 2007 - jstage.jst.go.jp
Xenopus oocytes and found that 20 (S)-Rg3 rather than 20 (R)-Rg3 was more stronger
inhibitor of I5-HT. In the present study, we further investigated the effects of 20 (R)-Rg3 and …