Why the study?
Does nicardipine demonstrate brain uptake in normal and ischemic rats?
Does nicardipine demonstrate brain uptake in normal and ischemic rats?
Nicardipine demonstrates significant first-pass extraction into the brain, particularly in ischemic regions, suggesting availability to neuronal calcium channels.
Nicardipine reaches ischemic rat brain targets; leaves open translation to human neuroprotection trials.
Dihydropyridine calcium channel blockers may be effective treatment for acute cerebral ischemia, but the uptake of these drugs into the brain is unknown. A 0.2-ml bolus of [14C]nicardipine hydrochloride and [3H]water was injected into the common carotid arteries of 7 normal and 7 ischemic rats. The corrected first-pass extraction of nicardipine, compared to water, was calculated to be 30.7% into the hemispheres and 42.3% into the hippocampi. The uptake was greater into the ischemic hemispheres (p less than 0.001). These data suggest that dihydropyridines are available to binding sites and calcium channels in neurons.
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Grotta et al. (1987) studied this question.
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