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Medizin - Open Access LMU - Teil 07/22 Podcast
The low KM-phosphodiesterase inhibitor denbufylline enhances neuronal excitability in guinea pig hippocampus in vitro

The low KM-phosphodiesterase inhibitor denbufylline enhances neuronal excitability in guinea pig hippocampus in vitro

Medizin - Open Access LMU - Teil 07/22 vor 36 Jahren

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The actions of the phosphodiesterase inhibitor denbufylline on the
excitability of hippocampal neurons were investigated by means of
extracellular and intracellular recordings. Denbufylline, which has
been shown to selectively inhibit a low KM,
Ca2+/calmodulin-independent phosphodiesterase isozyme,
concentration-dependently increased the amplitude of the
extracellularly recorded CAI population spike evoked by electrical
stimulation of the Schaffer collateral/commissural pathway.
Concentration-response-curves yielded an EC50 for denbufylline of
0.76 M. In comparison, the nonselective phosphodiesterase inhibitor
3-isobutyl-lmethylxanthine (IBMX) also produced an increase in the
amplitude of the population spike. From the
concentration-response-curve, which was steeper than that of
denbufylline, an EC50 for IBMX of 1.04 M was obtained. However,
despite their similar EC50 values, denbufylline was found to be
significantly more potent at lower concentrations (