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PubMed1984

Interaction of amoscanate with the cyclic AMP-phosphodiesterases from Schistosoma mansoni, Onchocerca volvulus and bovine heart.

The anthelmintic compounds amoscanate (4-isothiocyanato-4'-nitrodiphenylamine) and its derivatives CGP 6140 and CGP 8045 are potent inhibitors of the activities of cyclic AMP-phosphodiesterases from schistosomal and filarial worms as well as from both the calmodulin-dependent and the -independent enzyme of bovine heart. As shown for CGP 8045 the type of inhibition is non-competitive with respect to the substrate and the inhibition constants were determined to be in the range of 50 micrograms/ml for the enzymes of parasites and mammalian. It is proposed that the inhibition of cyclic AMP-phosphodiesterase-activity by amoscanate and derivatives - resulting in accumulation of cyclic AMP - might subsequently lead to disturbances in the regulation of metabolic areas like glycogen metabolism which are controlled by cyclic AMP-dependent protein kinases.

3',5'-Cyclic-AMP Phosphodiesterases↗
PubMed1982

Attempts to establish Onchocerca volvulus infection in primates and small laboratory animals.

Attempts were made to transmit O. volvulus infection to small laboratory animals and several species of primates to identify a practical laboratory host for human onchocerciasis. Infective larvae of O. volvulus of Guatemalan origin were inoculated into the following animals: rhesus monkeys, bonnet monkeys, golden spider monkeys, black spider monkeys, galagos, opossums, jirds, newborn and adult Swiss mice, kinkajou, cebus monkey, normal and splenectomized multimammate rats, and a calf. The animals were examined for signs of developing infection for up to two years after inoculation. None of the animals tested developed a patent infection, and neither larvae nor O. volvulus adults were found during the necropsy of all the animals which died or were killed during or at the end of the examination period. It is concluded that none of the animals tested is susceptible to infection with O. volvulus.

Animals↗