Transport Mechanism of an H_1-Antagonist at the Blood-Brain Barrier : Transport Mechanism of Mepyramine Using the Carotid Injection Technique

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The blood-brain barrier (BBB) permeability of mepyramine was measured by the carotid injection technique to elucidate the transport mechanism of an H_1-antagonist in the central nervous system. Mepyramine was found to enter the brain by saturable and carrier-mediated transport. The in vivo kinetic parameters were estimated as follows : the maximum uptake rate (J_<max>) was 7.12±1.37μmol/min/g of brain, the Michaelis constant (K_d) was 4.40±2.00mM, and the nonsaturable first order rate (K_d) was 0.28±0.02ml/min/g of brain. The mepyramine transport was not inhibited either by nutrients or by choline, hemicholinium-3,though it was inhibited by the classical H_1-antagonists such as diphenhydramine, diphenylpyraline, and also by propranolol. The above inhibitory effects suggest that a transport system different from the amine transport system exists for the BBB transport of mepyramine, and that this transporter is common not only for H_1-antagonists but also for basic drugs.
社団法人日本薬学会の論文
1994-05-15