Changes in specific binding sites of girisopam after chemical and surgical lesions in the striato-nigral system

Neurotoxin (AMPA)-induced lesions in the caudate nucleus as well as unilateral surgical transection of the striato-nigral pathway strongly depleted the binding of a homophthalazine (formerly called 2,3-benzodiazepines) girisopam (GYKI-51189, EGIS 5810) selectively in the substantia nigra of the rat, ipsilateral to the lesions. In contrast to this, AMPA injections into the substantia nigra failed to effect on girisopam binding to either components of the nigro-striatal system. Data indicate that this homophthalazine may bind to a descending component of the striatum (striato-nigral projecting neurons), or its binding capacity to substantia nigra neurons depends on the integrity of striatal afferent pathways to the substantia nigra.