PMID- 11588608
DA - 20011005
DCOM- 20011204
IS - 0959-4965
VI - 12
IP - 13
DP - 2001 Sep 17
TI - The AMPA receptor allosteric potentiator PEPA ameliorates post-ischemic memory impairment.
PG - 2947-50 AB - PEPA (4-[2-(Phenylsulphonylamino)ethylthio]-2,6-difluorophenoxyacetamide) is a recently developed allosteric potentiator of AMPA receptors that preferentially affects flop splice variants. We tested the effects of PEPA on ischemia-induced memory deficit in rats. Permanent unilateral occlusion of the middle cerebral artery induced severe impairment of performance of rats in the Morris water maze test. Repeated intravenous administration of PEPA (1, 3, 10 mg/kg/day for 10 days) improved test performance. In contrast, a corresponding dose of aniracetam, a representative potentiator of AMPA receptor, did not significantly improve test performance. Thus, PEPA is more effective than aniracetam in reversing impaired memory function as assessed by the Morris water maze test; and PEPA may be an effective compound for the treatment of impaired memory.
AD - Department of Degenerative Neurological Diseases, National Institute of
Neuroscience, National Center of Neurology and Psychiatry, 4-1-1
Ogawahigashi, Kodaira, Tokyo 187-8502, Japan.
FAU - Sekiguchi, M
AU - Sekiguchi M
FAU - Yamada, K
AU - Yamada K
FAU - Jin, J
AU - Jin J
FAU - Hachitanda, M
AU - Hachitanda M
FAU - Murata, Y
AU - Murata Y
FAU - Namura, S
AU - Namura S
FAU - Kamichi, S
AU - Kamichi S
FAU - Kimura, I
AU - Kimura I
FAU - Wada, K
AU - Wada K
LA - eng
PT - Journal Article
CY - England
TA - Neuroreport
JID - 9100935
RN - 0 (4-(2-(phenylsulfonylamino)ethylthio)-2,6-difluorophenoxyacetamide)
RN - 0 (Excitatory Amino Acid Agonists)
RN - 0 (Nootropic Agents)
RN - 0 (Phenoxyacetates)
RN - 0 (Pyrrolidinones)
RN - 0 (Receptors, AMPA)
RN - 72432-10-1 (aniracetam)
SB - IM
MH - Allosteric Regulation/drug effects/physiology
MH - Animal
MH - Brain/*drug effects/metabolism/physiopathology
MH - Brain Ischemia/complications/*drug therapy/physiopathology
MH - Dose-Response Relationship, Drug
MH - Excitatory Amino Acid Agonists/*pharmacology
MH - Infarction, Middle Cerebral Artery/complications/drug
therapy/physiopathology
MH - Male
MH - Maze Learning/drug effects/physiology
MH - Memory Disorders/*drug therapy/etiology/physiopathology
MH - Nootropic Agents/*pharmacology
MH - Phenoxyacetates/*pharmacology
MH - Pyrrolidinones/pharmacology
MH - Rats
MH - Rats, Inbred SHR
MH - Receptors, AMPA/*drug effects/metabolism
MH - Support, Non-U.S. Gov't
EDAT- 2001/10/06 10:00
MHDA- 2002/01/05 10:01
PST - ppublish
SO - Neuroreport 2001 Sep 17;12(13):2947-50.