Journal article
Near native binding of a fluorescent serotonin conjugate to serotonin type 3 receptors
Bioorganic & medicinal chemistry letters, Vol.23(3), pp.773-775
02/01/2013
Handle:
https://hdl.handle.net/2376/107743
PMID: 23265874
Abstract
Described is the synthesis of 5-hydroxytryptamine-tetramethylrhodamine (5HT∗); an indole nitrogen linked fluorescent conjugate of serotonin. Through a series fluorescence quenching experiments and experiments in the presence of a known competitive antagonist (Granisetron), it was shown that 5HT∗ specifically binds to purified homo-pentameric type-3 human serotonin receptors (5HT3A). The measured dissociation constant and Hill coefficient are Kd=83±3nM and n=3.1±0.3, respectively which is indicative of multi-ligand binding and cooperativity similar to that of unconjugated serotonin.
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Details
- Title
- Near native binding of a fluorescent serotonin conjugate to serotonin type 3 receptors
- Creators
- Elsa I Silva-LopezAdam O BardenJames A Brozik
- Publication Details
- Bioorganic & medicinal chemistry letters, Vol.23(3), pp.773-775
- Academic Unit
- Chemistry, Department of
- Publisher
- Elsevier Ltd
- Identifiers
- 99900546963601842
- Language
- English
- Resource Type
- Journal article