Psychotropic profile of S 17092, a prolyl endopeptidase inhibitor, using quantitative EEG in young healthy volunteers.
The central activity of S 17092, a prolyl endopeptidase (PEP) inhibitor, was investigated by quantitative electroencephalography (qEEG) in 48 young healthy men participating in a double-blind, randomized, placebo-controlled, cross-over study. S 17092 (100, 200, 400 or 600 mg) and placebo were administered once daily for 10 days in a rising multiple-dose scheme. EEG recordings were performed before and repeatedly from 0.5 to 24 h after dose on day 1 and day 10. PEP activity in plasma was also measured for the same periods. S 17092 appeared as a potent inhibitor of PEP activity at all doses, after both single and repeated administrations. EEG changes after acute doses were slight and of short duration, mainly characterized by increased relative alpha 1 power, suggesting a vigilance-promoting EEG profile. After repeated doses and more strikingly after a superimposed dose, increases in relative alpha 1 power were still present with additional increase in relative delta power and decreases in absolute fast alpha, fast beta, theta powers and total power at all doses. These EEG findings suggest that S 17092 might possess some mood-stabilizing potential in addition to its cognition-enhancing properties.
Morain
P
P
IRIS, Institut de Recherches Internationales SERVIER, Courbevoie, France. philippe.morain@fr.netgrs.com
Boeijinga
P H
PH
Demazières
A
A
De Nanteuil
G
G
Luthringer
R
R
D000293:Adolescent; D000328:Adult; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D004311:Double-Blind Method; D004334:Drug Administration Schedule; D004569:Electroencephalography / Q000187:drug effects*; D006801:Humans; D007211:Indoles / Q000097:blood / Q000494:pharmacology*; D008297:Male; D011619:Psychotropic Drugs / Q000097:blood / Q000494:pharmacology*; D053778:Thiazolidines / Q000097:blood / Q000494:pharmacology*; D013997:Time Factors
D007211:Indoles; D011619:Psychotropic Drugs; C118986:S 17092-1; D053778:Thiazolidines