| Literature DB >> 7608899 |
K H Buchheit1, R Gamse, R Giger, D Hoyer, F Klein, E Klöppner, H J Pfannkuche, H Mattes.
Abstract
A number of substituted indole carbazimidamides were prepared and evaluated as 5-HT4 receptor agonists by using the isolated field-stimulated guinea pig ileum preparation. Their selectivity for the 5-HT4 receptor was established by examining their affinity for other 5-HT receptors using radioligand-binding techniques. Several selective and highly potent full as well as partial agonists emerged from this study. For example, 1b,d were found to be the most potent, full 5-HT4 receptor agonist described so far (EC50 = 0.5 and 0.8 nM, respectively), being 6 and 4 times more potent than serotonin itself. On the other hand, 5b and 1h appeared as partial 5-HT4 receptor agonists in the nonstimulated guinea pig ileum preparation with potencies, evaluated against serotonin action, respectively similar (5b, Ki = 12 nM) to and 300-fold higher (1h, Ki = 0.04 nM) than serotonin.Entities:
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Year: 1995 PMID： 7608899 DOI： 10.1021/jm00013a010
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446