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- W2068585929 abstract "Abstract The present investigation was prompted by our previous finding that in the liver fluke, Fasciola hepatica , some phosphodiesterase inhibitors, instead of potentiating the rise in endogenous cAMP caused by 5-hydroxytryptamine (5-HT), antagonized it. Papaverine, 1-ethyl-4-(isopropylidenehydrazino)-1H-pyrazolo-(3,4-b)-pyridine-5-carboxylic acid, ethyl ester, HCl (SQ 20009), 6,7-dimethyl-4 ethyl-quinazoline (Quazodine) and caffeine inhibited 5-HT-activated adenylate cyclase from particulate fractions of the liver fluke. This may explain their in vivo antagonism to the 5-HT-mediated rise in endogenous cAMP levels. Isobutylmethylxanthine (IBMX), which did not antagonize the 5-HT effect in vivo , did not inhibit 5-HT-activated adenylate cyclase in fluke particles. None of the above compounds inhibited the NaF-activated adenylate cyclase. Kinetic studies showed that inhibition of 5-HT-activated adenylate cyclase by papaverine or SQ 20009 was not competitive with the substrate, ATP, or with GTP. While high levels of 5-HT decreased the degree of inhibition by papaverin and SQ 20009. the kinetics of inhibition does not appear to be strictly competitive." @default.
- W2068585929 created "2016-06-24" @default.
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- W2068585929 date "1979-06-01" @default.
- W2068585929 modified "2023-09-25" @default.
- W2068585929 title "Effect of some phosphodiesterase inhibitors on adenylate cyclase from the liver fluke, Fasciola hepatica" @default.
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- W2068585929 doi "https://doi.org/10.1016/0006-2952(79)90648-8" @default.
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