Therapeutics of 5-HT3 receptor antagonists: current uses and future directions

TK Machu - Pharmacology & therapeutics, 2011 - Elsevier
The 5-Hydroxytryptamine3 (5-HT3) receptor is a member of the cys-loop family of ligand
gated ion channels, of which the nicotinic acetylcholine receptor is the prototype. All other 5 …

Role of 5-HT3 Receptors in the Antidepressant Response

C Bétry, A Etiévant, C Oosterhof, B Ebert, C Sanchez… - Pharmaceuticals, 2011 - mdpi.com
Serotonin (5-HT) 3 receptors are the only ligand-gated ion channel of the 5-HT receptors
family. They are present both in the peripheral and central nervous system and are localized …

Involvement of mast cells in a mouse model of postoperative pain

SM Oliveira, CC Drewes, CR Silva, G Trevisan… - European journal of …, 2011 - Elsevier
Recent studies have indicated that nearly half of all surgical patients still have inadequate
pain relief; therefore, it is becoming increasingly more important to understand the …

The HTR3A polymorphism c.-42C> T is associated with amygdala responsiveness in patients with irritable bowel syndrome

LA Kilpatrick, JS Labus, K Coveleskie, C Hammer… - Gastroenterology, 2011 - Elsevier
Background & Aims 5-Hydroxytryptamine (5-HT) 3 receptor (5-HT 3 R) antagonists are
effective in treating patients with irritable bowel syndrome (IBS) and have anxiolytic effects …

Serotonin receptor diversity in the human colon: expression of serotonin type 3 receptor subunits 5‐HT3C, 5‐HT3D, and 5‐HT3E

J Kapeller, D Möller, F Lasitschka… - Journal of …, 2011 - Wiley Online Library
Since the first description of 5‐HT3 receptors more than 50 years ago, there has been
speculation about the molecular basis of their receptor heterogeneity. We have cloned the …

5-HT3 receptors: potential of individual isoforms for personalised therapy

B Niesler - Current opinion in pharmacology, 2011 - Elsevier
Serotonin type 3 (5-HT3) receptors are ligand-gated ion channels built by five subunits of
diverse composition. In humans, five subunits exist (5-HT3A-E) which are encoded by the …

Allosteric modulation of the 5-HT3 receptor

PA Davies - Current opinion in pharmacology, 2011 - Elsevier
5-Hydroxytryptamine type 3 (5-HT3) receptors are ligand-gated ion channels that play
important roles in depression, anxiety, substance abuse, emesis, inflammatory pain, spinal …

[HTML][HTML] From toxins targeting ligand gated ion channels to therapeutic molecules

A Nasiripourdori, V Taly, T Grutter, A Taly - Toxins, 2011 - mdpi.com
Ligand-gated ion channels (LGIC) play a central role in inter-cellular communication. This
key function has two consequences:(i) these receptor channels are major targets for drug …

Serotonin receptor 3A polymorphism c.-42C> T is associated with severe dyspepsia

S Mujakovic, JJM ter Linde, NJ de Wit… - BMC medical …, 2011 - Springer
Background The association between anxiety and depression related traits and dyspepsia
may reflect a common genetic predisposition. Furthermore, genetic factors may contribute to …

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 …