Beschreibung:
<jats:p>Extensive biochemical and pharmacological studies have determined three
different subtypes of imidazoline receptors: I1-imidazoline receptors (I1-IR)
involved in central inhibition of sympathicus that produce hypotensive
effect; I2-imidazoline receptors (I2-IR) modulate monoamine oxidase B
activity (MAO-B); I3-imidazoline receptors (I3-IR) regulate insulin secretion
from pancreatic ?-cells. Therefore, the I1/I2/I3 imidazoline receptors are
selected as new, interesting targets for drug design and discovery. Novel
selective I1/I2/I3 agonists and antagonists have been recently developed. In
the present review, we provide a brief update to the field of imidazoline
research, highlighting some of the chemical diversity and progress made in
the 2D-QSAR, 3D-QSAR and quantitative pharmacophore development studies of
I1-IR and I2-IR imidazoline receptor ligands. Theoretical studies of I3-IR
ligands are not yet performed because of insufficient number of synthesized
I3-IR ligands.</jats:p>