Initial evaluation of novel selective ligands for imidazoline(2) receptors in rat whole brain.

Indazim, the indazole analogue of 2BFI, and four methyl-substituted analogues were tested for their affinity at the imidazoline(2) binding site (I(2)-BS), and this affinity was compared with their affinity at the alpha(2)-adrenoceptor to determine their structure, affinity relationship, and selectivity at the I(2)-BS. These studies showed that these ligands were highly selective for the I(2)-BS compared with 2BFI and that substitution at the 4 and 7 positions increased affinity without affecting selectivity.