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Diethylcarbamazine: inhibitory effect on acetylcholinesterase of Dirofilaria immitis and Brugia pahangi.

Yasunori Fujimaki, Makoto Sakamoto, Muneaki Shimada, E Kimura, Y. Aoki

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Abstract

Anti-acetylcholinesterase activity of diethylcarbamazine (DEC) was studied. Acethylcholinesterase (AchE) of adult worms of Dirofilaria immitis, those of the 4th-stage larvae, early 5th-stage larvae and adults worms of Brugia pahangi, and that of hamster brain tissue were all inhibited by DEC. Michaelis constant (Km) of D. immitis and B. pahangi adult worm AchE were 1.47 x 10(-4) and 1.81 x 10(-4) M respectively. DEC was a competitive inhibitor of the filarial AchE. Inhibition constant (Ki) for AchE of D. immitis and B. pahangi adult worms were 2.56 x 10(-4) and 6.39 x 10(-4) M, respectively. DEC is a less potent anticholinesterase inhibitor, because Ki of DEC is 10(4) times higher than that of eserine, a potent anti-cholinesterase agent.

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Anti-acetylcholinesterase activity of diethylcarbamazine (DEC) was studied. Acethylcholinesterase (AchE) of adult worms of Dirofilaria immitis, those of the 4th-stage larvae, early 5th-stage larvae and adults worms of Brugia pahangi, and that of hamster brain tissue were all inhibited by DEC. Michaelis constant (Km) of D. immitis and B. pahangi adult worm AchE were 1.47 x 10(-4) and 1.81 x 10(-4) M respectively. DEC was a competitive inhibitor of the filarial AchE. Inhibition constant (Ki) for AchE of D. immitis and B. pahangi adult worms were 2.56 x 10(-4) and 6.39 x 10(-4) M, respectively. DEC is a less potent anticholinesterase inhibitor, because Ki of DEC is 10(4) times higher than that of eserine, a potent anti-cholinesterase agent.

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Available abstract

Anti-acetylcholinesterase activity of diethylcarbamazine (DEC) was studied. Acethylcholinesterase (AchE) of adult worms of Dirofilaria immitis, those of the 4th-stage larvae, early 5th-stage larvae and adults worms of Brugia pahangi, and that of hamster brain tissue were all inhibited by DEC. Michaelis constant (Km) of D. immitis and B. pahangi adult worm AchE were 1.47 x 10(-4) and 1.81 x 10(-4) M respectively. DEC was a competitive inhibitor of the filarial AchE. Inhibition constant (Ki) for AchE of D. immitis and B. pahangi adult worms were 2.56 x 10(-4) and 6.39 x 10(-4) M, respectively. DEC is a less potent anticholinesterase inhibitor, because Ki of DEC is 10(4) times higher than that of eserine, a potent anti-cholinesterase agent.

Key concepts: Brugia pahangi, Dirofilaria immitis, Diethylcarbamazine, Acetylcholinesterase, Aché, Cholinesterase, Filariasis, Hamster

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Diethylcarbamazine: inhibitory effect on acetylcholinesterase of Dirofilaria immitis and Brugia pahangi. — Research Paper | ScholarLens