Identification and Pharmacological Profile of an Indane Based Series of Ghrelin Receptor Full Agonists

Cachexia and muscle
wasting are very common among patients suffering
from cancer, chronic obstructive pulmonary disease, and other chronic
diseases. Ghrelin stimulates growth hormone secretion via the ghrelin
receptor, which subsequently leads to increase of IGF-1 plasma levels.
The activation of the GH/IGF-1 axis leads to an increase of muscle
mass and functional capacity. Ghrelin further acts on inflammation,
appetite, and adipogenesis and for this reason was considered an important
target to address catabolic conditions. We report the synthesis and
properties of an indane based series of ghrelin receptor full agonists;
they have been shown to generate a sustained increase of IGF-1 levels
in dog and have been thoroughly investigated with respect to their
functional activity.