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Diphenhydramine as a selective probe to study H⁺-antiporter function at the blood-brain barrier: Application to [¹¹C]diphenhydramine positron emission tomography imaging.

ABSTRACT: Diphenhydramine, a sedative histamine H₁-receptor (H₁R) antagonist, was evaluated as a probe to measure drug/H⁺-antiporter function at the blood-brain barrier. In situ brain perfusion experiments in mice and rats showed that diphenhydramine transport at the blood-brain barrier was saturable, following Michaelis-Menten kinetics with a K_m = 2.99 mM and V_max = 179.5 nmol s^-1 g^-1. In the pharmacological plasma concentration range the carrier-mediated component accounted for 77% of diphenhydramine influx while passive diffusion accounted for only 23%. [¹⁴C]Diphenhydramine blood-brain barrier transport was proton and clonidine sensitive but was influenced by neither tetraethylammonium, a MATE1 (SLC47A1), and

SUBMITTER: Auvity S

PROVIDER: S-EPMC5464711 | biostudies-literature | 2017 Jun

REPOSITORIES: biostudies-literature

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Diphenhydramine as a selective probe to study H⁺-antiporter function at the blood-brain barrier: Application to [¹¹C]diphenhydramine positron emission tomography imaging.

OmicsDI is part of the ELIXIR infrastructure

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Dataset Information

Diphenhydramine as a selective probe to study H+-antiporter function at the blood-brain barrier: Application to [11C]diphenhydramine positron emission tomography imaging.

OmicsDI is part of the ELIXIR infrastructure

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Diphenhydramine as a selective probe to study H⁺-antiporter function at the blood-brain barrier: Application to [¹¹C]diphenhydramine positron emission tomography imaging.