3 research outputs found
Development of a Large-Scale Route to an MCH<sub>1</sub> Receptor Antagonist: Investigation of a Staudinger Ketene–Imine Cycloaddition in Batch and Flow Mode
A practical large-scale route to
an MCH<sub>1</sub> receptor antagonist
is described. A Staudinger β-lactam synthesis of an imine and
an in situ generated ketene was utilized as a key step for the preparation
of a spiro-azetidine building block. The reaction was demonstrated
in both batch and flow mode and a comparison of these techniques is
described
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
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