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Updated: Jul 14, 2026

A Computerized Test Battery to Study Pharmacodynamic Effects on the Central Nervous System of Cholinergic Drugs in Early Phase Drug Development
Published on: February 11, 2019
Effect of caffeine on quinidine transport to the central nervous system in rats
V Vasović1, B Banić, Vida Jakovljević
1Department of Pharmacology and Toxicology, Faculty of Medicine, University of Novi Sad, Hajduk Veljkova 3, 21000 Novi Sad, Republic of Serbia. vasovicv@neobee.net
Abstract:
We studied the effect of caffeine on the transport of quinidine through the blood-brain barrier (BBB) to the central nervous system (CNS) in rats. The anesthetized animals received quinidine in the form of a retrograde intra-arterial bolus injection (15 s) into the right axillary artery 30 min after receiving a subcutaneous injection of caffeine (test group) or physiological solution (control group). Rats were decapitated at 30, 60, 90, 120, and 240 s after quinidine administration. Blood samples were taken from the left jugular vein. Upon washing, the brain, was divided into the brainstem, cerebellum, and cerebral hemispheres to determine the quinidine content in each section, using a standard spectrofluorimetric method. Quninidine attained maximal concentrations in the CNS with a latency compared with that in blood; the CNS values were higher. Quinidine kinetics showed two compartments in the CNS, one consisting of the brainstem and cerebellum, in which quinidine concentrations were higher, and the other the cerebral hemispheres. Caffeine caused a significant deceleration of quinidine transition through the BBB to the CNS.
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