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Brain extraction of a calcium channel blocker

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 ≤ 0.001). These data suggest that dihydropyridines are available to binding sites and calcium channels in neurons. http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Annals of Neurology Wiley

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References (33)

Publisher
Wiley
Copyright
Copyright © 1987 American Neurological Association
ISSN
0364-5134
eISSN
1531-8249
DOI
10.1002/ana.410210209
pmid
3827225
Publisher site
See Article on Publisher Site

Abstract

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 ≤ 0.001). These data suggest that dihydropyridines are available to binding sites and calcium channels in neurons.

Journal

Annals of NeurologyWiley

Published: Feb 1, 1987

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