Ghrelin receptor antagonist (GHS-R1a) (Ki
= 17 nM). Displays no significant affinity for the motilin receptor (Ki
= 6 μ
M). Blocks the effects of ghrelin on insulin secretion both in vivo
and in vitro
. Improves glucose homeostasis in vivo
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All Tocris products are intended for laboratory research use only.
Gut peptides: targets for antiobesity drug development?
Moran and Dailey
Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss.
Esler et al.