L-arginine methylester reduces Ca2+/Cl(-)-dependent L-[3H]glutamate binding and Ca2+-activated neutral protease activity in rat hippocampal membranes.
Specific binding of L-[3H]glutamate was measured in Tris-HCl buffer in rat hippocampal membranes. In these experimental conditions 1 mM CaCl2 induced an increase in binding due to an increase in Bmax. L-Arginine methylester did not modify the Cl(-)-dependent binding of L-[3H]glutamate, but it decreased Ca2+/Cl(-)-stimulated binding in a dose-dependent manner, decreasing Bmax without changing KD. L-Arginine methylester reduced calcium-activated neutral protease activity in a dose-dependent manner. Serine protease inhibitors (aprotinin and di-isopropylfluorophosphate) did not affect L-[3H]glutamate binding, whereas leupeptin reduced it in a dose-dependent manner. L-Arginine did not mimic the effect of L-arginine methylester in either model.
Bennardini
F
F
Dipartimento di Farmacologia Preclinica e Clinica Mario Aiazzi Mancini, Universitá degli Studi di Firenze, Florence, Italy.
Failli
P
P
Matucci
R
R
Bartolini
A
A
Malcangio
M
M
Massari
M
M
Franconi
F
F
Giotti
A
A
D000818:Animals; D001120:Arginine / Q000031:analogs & derivatives* / Q000494:pharmacology; D002122:Calcium Chloride / Q000494:pharmacology*; D004789:Enzyme Activation / Q000187:drug effects; D005971:Glutamates / Q000378:metabolism*; D006624:Hippocampus / Q000201:enzymology*; D066298:In Vitro Techniques; D007976:Leupeptins / Q000494:pharmacology; D008297:Male; D010447:Peptide Hydrolases / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains
D005971:Glutamates; D007976:Leupeptins; C026512:arginine methyl ester; D001120:Arginine; D010447:Peptide Hydrolases; D002122:Calcium Chloride