Chemical Name: 6-(4-Fluorophenoxy)-2-methyl-3-[[(3S)-1-(1-methylethyl)-3-piperidinyl]methyl]-4(3H)-quinazolinone
Biological ActivityGhrelin receptor antagonist (GHS-R1a) (Ki = 17 nM). Displays no significant affinity for the motilin receptor (Ki = 6 μM). Blocks the effects of ghrelin on insulin secretion both in vivo and in vitro. Improves glucose homeostasis in vivo.
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss.
Esler et al.
Gut peptides: targets for antiobesity drug development?
Moran and Dailey
Citations for YIL 781
The citations listed below are publications that use Tocris products. Selected citations for YIL 781 include:
3 Citations: Showing 1 - 3
Ghrelin receptor antagonism of hyperlocomotion in cocaine-sensitized mice requires βarrestin-2.
Authors: T?th Et al.
G Protein and β-arrestin signaling bias at the ghrelin receptor.
Authors: Evron Et al.
J Biol Chem 2014;289:33442
Ghrelin modulates lateral amygdala neuronal firing and blocks acquisition for conditioned taste aversion.
Authors: Song Et al.
PLoS One 2013;8:e65422
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