Article
New insights into the human 5-HT4 receptor binding site: exploration of a hydrophobic pocket.
British journal of pharmacology - 1 Oct 2004
Rivail Lucie, Giner Mireille, Gastineau Monique, Berthouze Magali, Soulier Jean-Louis, Fischmeister Rodolphe, Lezoualc'h Frank, Maigret Bernard, Sicsic Sames, Berque-Bestel Isabelle
Abstract excerpt
A body of evidences suggests that a hydrophobic pocket of the human 5-HT(4) receptor contributes to the high affinity of some bulky 5-HT(4) ligands. A thorough study of this pocket was performed using mutagenesis and molecular modeling. Ligand binding or competition studies with selected bulky ligands (RS39604, RS100235, [(3)H]GR113808 and ML11411) and small ligands (5-HT and ML10375) were carried out on...
Topics
- Amino Acids
- Aminobenzoates
- Animals
- Binding Sites
- Binding, Competitive
- COS Cells
- Chlorocebus aethiops
- Humans