| Literature DB >> 7608898 |
K H Buchheit1, R Gamse, R Giger, D Hoyer, F Klein, E Klöppner, H J Pfannkuche, H Mattes.
Abstract
The design and synthesis of a new class of potent and selective 5-HT4 receptor agonists containing an indole nucleus linked to a carbazimidamide are presented. A conformational study of the 5-HT4 receptor agonists serotonin and zacopride led to the identification of an initial pharmacophore and to the definition of a three-dimensional map of the 5-HT4 agonist recognition site. 1, a representative member of our new class of 5-HT4 receptor agonists, incorporates all reference structural features and matched perfectly with these models. 1 is a highly potent, full agonist at 5-HT4 receptors present in the isolated electrically stimulated guinea pig ileum preparation, with a pD2 value of 8.8, displaying selectivity (ranging from 40- to over 10,000-fold) versus other members of the serotonin receptor family.Entities:
Mesh：
Substances：
Year: 1995 PMID： 7608898 DOI： 10.1021/jm00013a009
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446