High affinity and potent ghrelin receptor inverse agonist (Ki
values are 4.9 and 31 nM in COS7 and HEK293T cells, respectively). Blocks ghrelin receptor-mediated Gq
- and G13
-dependent signaling pathways.
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An aromatic region to induce a switch between agonism and inverse agonism at the ghrelin receptor.
Els et al.
Agonism, antagonism, and inverse agonism bias at the ghrelin receptor signaling.
M'Kadmi et al.