Brain extraction of a calcium channel blocker.
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.
D000818:Animals; D001921:Brain / Q000378:metabolism*; D002545:Brain Ischemia / Q000378:metabolism; D002121:Calcium Channel Blockers / Q000378:metabolism*; D006624:Hippocampus / Q000378:metabolism; D008297:Male; D009529:Nicardipine / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains
D002121:Calcium Channel Blockers; D009529:Nicardipine