Acetylcholinesterase inhibitor SDZ ENA 713 (Rivastigmine) increases brain pyrrolidone carboxyl peptidase activity.
Pyroglutamyl-ended forms of amyloid-beta-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-beta-peptides (A beta pE) deposition through the activation of Pcp.
Ramírez-Expósito
M J
MJ
Unit of Physiology, Faculty of Experimental and Health Sciences, University of Jaén, Paraje Las Lagunillas s/n, E-23071, Jaén, Spain.
Robert-Baudouy
J
J
Mayas
M D
MD
García
M J
MJ
Ramírez
M
M
Martínez-Martos
J M
JM
D000818:Animals; D001522:Behavior, Animal / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000201:enzymology*; D002219:Carbamates / Q000494:pharmacology*; D002540:Cerebral Cortex / Q000187:drug effects / Q000201:enzymology; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects; D008297:Male; D051379:Mice; D008807:Mice, Inbred BALB C; D048448:Phenylcarbamates; D017397:Prefrontal Cortex / Q000187:drug effects / Q000201:enzymology; D011751:Pyroglutamyl-Peptidase I / Q000378:metabolism*; D000068836:Rivastigmine; D013574:Synaptosomes / Q000187:drug effects / Q000378:metabolism
D002219:Carbamates; D002800:Cholinesterase Inhibitors; D048448:Phenylcarbamates; D011751:Pyroglutamyl-Peptidase I; D000068836:Rivastigmine