upf-596 and tryptamine
upf-596 has been researched along with tryptamine* in 1 studies
Other Studies
1 other study(ies) available for upf-596 and tryptamine
| Article | Year |
|---|---|
5-Fluorotryptamine is a partial agonist at 5-HT3 receptors, and reveals that size and electronegativity at the 5 position of tryptamine are critical for efficient receptor function.
Antagonists, but not agonists, of the 5-HT3 receptor are useful therapeutic agents, and it is possible that partial agonists may also be potentially useful in the clinic. Here we show that 5-fluorotryptamine (5-FT) is a partial agonist at both 5-HT3A and 5-HT3AB receptors with an Rmax (Imax/Imax 5-HT) of 0.64 and 0.45 respectively. It is about 10 fold less potent than 5-HT: EC50=16 and 27 microM, and Ki for displacement of [3H]granisetron binding=0.8 and 1.8 microM for 5-HT3A and 5-HT3AB receptors respectively. We have also explored the potencies and efficacies of tryptamine and a range of 5-substituted tryptamine derivatives. At 5-HT3A receptors tryptamine is a weak (Rmax=0.15), low affinity (EC50=113 microM; Ki=4.8 microM) partial agonist, while 5-chlorotryptamine has a similar affinity to 5-FT (EC50=8.1 microM; Ki=2.7 microM) but is a very weak partial agonist (Rmax=0. 0037). These, and data from 5-methyltryptamine and 5-methoxytryptamine, reveal the importance of size and electronegativity at this location for efficient channel opening. Topics: 5-Methoxytryptamine; Amino Acid Sequence; Animals; Bridged Bicyclo Compounds; Cell Line; Dose-Response Relationship, Drug; Drug Partial Agonism; Electrophysiology; Female; Glycine; Granisetron; Humans; Mice; Molecular Sequence Data; Molecular Structure; Oocytes; Radioligand Assay; Receptors, Drug; Receptors, Serotonin, 5-HT3; Sequence Homology, Amino Acid; Serotonin 5-HT3 Receptor Agonists; Serotonin Antagonists; Tryptamines; Xenopus | 2008 |