Effects of 9-amino-1,2,3,4-tetrahydroacridine (THA) on ATP diphosphohydrolase (EC 3.6.1.5) and 5'-nucleotidase (EC 3.1.3.5) from rat brain synaptosomes.
1. 9-Amino-1,2,3,4-tetrahydroacridine (THA), an acetylcholinesterase inhibitor, significantly inhibited in vitro the ATP diphosphohydrolase activity of synaptosomes from the cerebral cortex and hippocampus of adult rats. 2. THA did not inhibit in vitro the 5'-nucleotidase activity of synaptosomes from cerebral cortex and hippocampus of rats. 3. THA exerted an uncompetitive inhibition on ATP diphosphohydrolase activity. This mechanism of inhibition was the same in the 2 different synaptosomal fractions (cerebral cortex and hippocampus) studied. 4. THA, proposed as a drug for the treatment of Alzheimer's disease, can alter in vitro ATP degradation in synaptosomes from the central nervous system.
Bonan
C D
CD
Department of Biochemistry, Institute of Biosciences, Federal University of Rio Grande Do Sul, Porto Alegre, RS, Brazil.
Battastini
A M
AM
Schetinger
M R
MR
Moreira
C M
CM
Frassetto
S S
SS
Dias
R D
RD
Sarkis
J J
JJ
D015720:5'-Nucleotidase / Q000378:metabolism*; D000244:Adenosine Diphosphate / Q000378:metabolism; D000255:Adenosine Triphosphate / Q000378:metabolism; D000818:Animals; D001081:Apyrase / Q000037:antagonists & inhibitors*; D001921:Brain / Q000187:drug effects* / Q000201:enzymology / Q000648:ultrastructure; D002540:Cerebral Cortex / Q000187:drug effects / Q000201:enzymology; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D006624:Hippocampus / Q000187:drug effects / Q000201:enzymology; D006868:Hydrolysis / Q000187:drug effects; D007700:Kinetics; D008297:Male; D051381:Rats; D017208:Rats, Wistar; D013574:Synaptosomes / Q000187:drug effects* / Q000201:enzymology; D013619:Tacrine / Q000494:pharmacology*
D002800:Cholinesterase Inhibitors; D013619:Tacrine; D000244:Adenosine Diphosphate; D000255:Adenosine Triphosphate; D015720:5'-Nucleotidase; D001081:Apyrase