Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.

A series of ring-substituted (i.e., methoxy and bromo) 3,4-dihydro- and 1,2,3,4-tetrahydro-beta-carbolines was examined at I(2) imidazoline receptors, as was the effect of ring-opening, ring-expansion, and translocation of the piperidinyl nitrogen atom. Several analogues were identified that bind with K(i) <20 nM at I(2) sites and with reduced affinity at alpha(2)-adrenergic receptors, and 1,2,3,4-tetrahydro-gamma-carbolines were identified as a novel class of I(2) imidazoline receptor ligand.