Region-dependent effects of acute and chronic tranylcypromine in vivo on [3H]2-BFI binding to brain imidazoline I(2) sites.

An imidazoline I(2) site has been localised to monoamine oxidase. However, in vitro studies of the effect of monoamine oxidase inhibitors on imidazoline I(2)-site radioligand binding have produced conflicting findings. Using the technique of autoradiography, we examined the effect of in vivo administration of the irreversible monoamine oxidase inhibitor tranylcypromine on binding of the imidazoline I(2) site-specific ligand [3H]2-(-2-benzofuranyl)-2-imidazoline ([3H]2-BFI) in four rat brain nuclei which are known to possess a high density of imidazoline I(2) sites, together with cerebral cortex and cerebellum which show weaker binding. A single acute pre-treatment with tranylcypromine significantly increased imidazoline I(2) site-specific binding in four regions: arcuate nucleus, interpeduncular nucleus, pineal gland and area postrema, but effects in cortical areas and cerebellum were not significant. The extent of the increase was proportional to the control binding in each region. In contrast, five daily treatments with the same dose of tranylcypromine significantly reduced [3H]2-BFI binding in these same areas. The potential role of monoamine oxidase isoforms in these changes is discussed.