ANTICONVULSANT EFFICACY SAFETY PROPERTIES OF 2-AMINO-N-(1,2-DIPHENYLETHYL)ACETAMIDE HYDROCHLORIDE

Citation
Gc. Palmer et al., ANTICONVULSANT EFFICACY SAFETY PROPERTIES OF 2-AMINO-N-(1,2-DIPHENYLETHYL)ACETAMIDE HYDROCHLORIDE, The Journal of pharmacology and experimental therapeutics, 273(3), 1995, pp. 1023-1031
Citations number
36
Categorie Soggetti
Pharmacology & Pharmacy
ISSN journal
00223565
Volume
273
Issue
3
Year of publication
1995
Pages
1023 - 1031
Database
ISI
SICI code
0022-3565(1995)273:3<1023:AESPO2>2.0.ZU;2-W
Abstract
mino-N-(1,2-diphenylethyl)-acetamide-hydrochloride (FPL 13950) was pro filed preclinically in rodents for efficacy against convulsions, as we ll as for acute safety/behavioral observations. FPL 13950 exhibited go od oral efficacy and duration of action with respect to prevention of seizures elicited by maximal electroshock-shock in both rats and mice. Tolerance to protection against maximal electroshock and hexobarbital -induced sleep-time was not evident after subchronic drug administrati on. FPL 13950 also prevented convulsions/mortality in mice after i.v. dosing with N-methyl-D, L-aspartate, however, it was ineffective again st other types of chemically induced convulsions, as well as bicorneal kindling. High oral doses produced neural impairment in both mice and rats and hyperactivity in rats. Sequential administration of yet high er doses elicited tonic/clonic convulsions culminating in death. Durin g i.v. infusion of metrazol in mice, high i.p. doses of FPL 13950 shor tened the latency to first twitch and clonus. No increase in the start le response or phencyclidine-like behavior was evident after oral dosi ng in rats.