Efficacy of selective 5‐HT6 receptor ligands determined by monitoring 5‐HT6 receptor‐mediated cAMP signaling pathways

G Romero, E Sánchez, M Pujol, P Pérez… - British journal of …, 2006 - Wiley Online Library
1 Two novel selective 5‐HT6 receptor ligands E‐6801 (6‐chloro‐N‐(3‐(2‐(dimethylamino)
ethyl)‐1H‐indol‐5‐yl) imidazo [2, 1‐b] thiazole‐5‐sulfonamide) and E‐6837 (5‐chloro‐N‐(3 …

Characterization of Ro 04‐6790 and Ro 63‐0563: potent and selective antagonists at human and rat 5‐HT6 receptors

AJ Sleight, FG Boess, M Bös… - British journal of …, 1998 - Wiley Online Library
This study describes the in vitro characterization of two potent and selective 5‐HT6 receptor
antagonists at the rat and human recombinant 5‐HT6 receptor. In binding assays with [3H] …

Characterization of a 5‐HT1B receptor on CHO cells: functional responses in the absence of radioligand binding

H Giles, SJ Lansdell, ML Bolofo… - British journal of …, 1996 - Wiley Online Library
1 Chinese hamster ovary (CHO) cells have been reported to be devoid of 5‐HT receptors
and have frequently been used as hosts for the expression of cloned 5‐HT receptors …

New insights into the human 5‐HT4 receptor binding site: exploration of a hydrophobic pocket

L Rivail, M Giner, M Gastineau… - British journal of …, 2004 - Wiley Online Library
A body of evidences suggests that a hydrophobic pocket of the human 5‐HT4 receptor
contributes to the high affinity of some bulky 5‐HT4 ligands. A thorough study of this pocket …

Whole spectrum analysis of ligand efficacy at constitutively active human wild-type and S267K 5-HT6 receptors in HEK-293F cells

G Romero, M Pujol, P Pérez, H Buschmann… - … of pharmacological and …, 2007 - Elsevier
Introduction: Modulation of constitutive activity by the recombinant wild-type human 5-HT6
receptor was investigated with a series of 5-HT6 receptor ligands by monitoring the cAMP …

Site-directed mutagenesis of the 5-HT1B receptor increases the affinity of 5-HT for the agonist low-affinity conformation and reduces the intrinsic activity of 5-HT

C Grånäs, J Nordquist, N Mohell… - European journal of …, 2001 - Elsevier
The antagonist radioligand [3H] GR125743 and the agonist radioligand [3H] 5-HT were
used to investigate the pharmacological characteristics of the G protein uncoupled agonist …

A comparison of the pharmacological properties of guinea‐pig and human recombinant 5‐HT4 receptors

RG Vickery, N Mai, E Kaufman… - British journal of …, 2007 - Wiley Online Library
Background and purpose: 5‐HT4 receptor agonists are used therapeutically to treat
disorders of reduced gastrointestinal motility. Since such compounds are evaluated in …

Small molecule 5-HT6R ligands: a comprehensive insight into their selectivity and activity

AV Ivachtchenko, YA Ivanenkov - Current Bioactive …, 2013 - ingentaconnect.com
In recent years, considerable research efforts have focused on the role of serotonin in
various pathological states, as well as on the identification of the respective serotonin …

The 5‐HT4 receptor agonist, tegaserod, is a potent 5‐HT2B receptor antagonist in vitro and in vivo

DT Beattie, JAM Smith, D Marquess… - British journal of …, 2004 - Wiley Online Library
Tegaserod (Zelnorm®) is a potent 5‐hydroxytryptamine4 (5‐HT4) receptor agonist with
clinical efficacy in disorders associated with reduced gastrointestinal motility and transit. The …

(+)‐WAY 100135, a partial agonist, at native and recombinant 5‐HT1B/1D receptors

C Davidson, M Ho, GW Price, BJ Jones… - British journal of …, 1997 - Wiley Online Library
We have studied the effects of the purportedly selective 5‐HT1A receptor antagonist (+)‐
WAY100135 on electrically stimulated 5‐hydroxytryptamine (5‐HT) efflux in the ventrolateral …