Acetylcholinesterase inhibitor SDZ ENA 713 (Rivastigmine) increases brain pyrrolidone carboxyl peptidase activity

Abstract Pyroglutamyl-ended forms of amyloid-β-peptide are present in senile plaques in some individuals with Alzheimer type dementia. Single oral administration of the acetylcholinesterase inhibitor SDZ ENA 713 (rivastigmine (+)-( S )- N -ethyl-3-[(1-dimethylamino)ethyl]- N -methylphenylcarbamate hydrogen tartrate) increases basal and K + -stimulated pyrrolidone carboxyl peptidase (Pcp) activity in mice frontal cortex synaptosomes in a dose-dependent manner. These results suggest that this drug may ameliorate ATD cognitive deficits acting not only facilitating cholinergic transmission but also avoiding the formation of pyroglutamyl-ended amyloid-β-peptides (Aβ pE) deposition through the activation of Pcp.