BU98008, a Highly Selective Imidazoline1-Receptor Ligand.

BU98008 (1-(4, 5-dihydro-1H-imidazol-2-yl)isoquinoline) is a novel isoquinoline derivative. Radioligand binding studies revealed it had high affinity for the I₁ receptor in rat kidney membranes but low affinity for the I₂ binding site and a₂-adrenoceptor in rat brain membranes. Further evaluation of BU98008 in vivo revealed no effect on blood pressure following peripheral administration. These preliminary data suggest BU98008 may be an antagonist at I₁ receptors. Further evaluation following central administration must be performed before a hypotensive action can be excluded. [ABSTRACT FROM AUTHOR]