The in vivo inhibition of transport enzyme activities by chloroquine in different organs of rat is reversible.
The antimalarial drug chloroquine is found to inhibit Na+, K(+)-ATPase, Ca2+, Mg(2+)-ATPase, Ca(2+)-ATPase, pNPPase and acetylcholinesterase activities in different organs of rat in vivo when injected for a certain periods of time. The inhibition seems to be due to the changes in the level of phospholipid, cholesterol and the fatty acid of the lipid and the alteration of the fluidity of the microsomal membranes. However, the enzyme activities return to the normal level in about 2-3 weeks after the discontinuation of the drug suggesting that the drug effect is reversible.
Chandra
S
S
Department of Chemistry, Bose Institute, Calcutta, India.
Adhikary
G
G
Sikdar
R
R
Sen
P C
PC
D009597:4-Nitrophenylphosphatase / Q000037:antagonists & inhibitors*; D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000187:drug effects / Q000201:enzymology*; D017301:Ca(2+) Mg(2+)-ATPase / Q000037:antagonists & inhibitors*; D000252:Calcium-Transporting ATPases / Q000037:antagonists & inhibitors*; D002738:Chloroquine / Q000494:pharmacology*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D007668:Kidney / Q000187:drug effects / Q000201:enzymology*; D007700:Kinetics; D008297:Male; D008861:Microsomes / Q000201:enzymology*; D009928:Organ Specificity; D051381:Rats; D011919:Rats, Inbred Strains; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors*; D013154:Spleen / Q000187:drug effects / Q000201:enzymology*; D013737:Testis / Q000187:drug effects / Q000201:enzymology*
D002800:Cholinesterase Inhibitors; D002738:Chloroquine; D000110:Acetylcholinesterase; D009597:4-Nitrophenylphosphatase; D017301:Ca(2+) Mg(2+)-ATPase; D000252:Calcium-Transporting ATPases; D000254:Sodium-Potassium-Exchanging ATPase