PubMed · 1967 · 306 citations · 0 references
Life SciencesNeurosciencePharmacologyMetabolismNeurochemistryNeuropharmacologyDrug DispositionMonoamine NeurochemistryNeuronal MetabolismNeurotransmissionSerotonergic PharmacologySerotonergic SignalingBlood-brain Barrier Drug TransportBrain Drug MetabolismBrain-to-plasma RatioCentral Nervous System PharmacokineticsPharmacokinetics Of Neuroactive DrugsRenal Tubular SecretionSerotonin PharmacokineticsSteady-state Kinetics
Probenecid, a drug that competitively inhibits the renal tubular secretion of a number of acidic substances, also blocks the efflux of 5-hy-droxyindoleacetic acid (5-HIAA) from rat brain. The rate at which 5-HIAA is accumulated after probenecid administration almost exactly equals the rate of formation of this acid from serotonin (5-HT). These results imply that 5-HIAA and perhaps other acidic products of brain metabolism are transferred directly from brain to plasma by a specialized process.