Regional distribution of unbound eletriptan and sumatriptan in the CNS and PNS in rats: implications for a potential central action.

ABSTRACT:

Background

Triptans are potent 5-HT_1B/1D/1F receptor agonists used in migraine therapy, thought to act through peripheral mechanisms. It remains unclear whether triptans cross the blood-brain barrier (BBB) sufficiently to stimulate central 5-HT_1B/1D/1F receptors. This study investigates the disposition of eletriptan and sumatriptan in central nervous system (CNS) and peripheral nervous system (PNS) regions and predicts regional 5-HT_1B/1D/1F receptor occupancies at clinically relevant concentrations.

Methods

Using the Combinatory Mapping Approach (CMA) for regions of interest (ROI), we assessed the unbound tissue-to-plasma concentration ratio (K_{p, uu, ROI}) in rats at steady state across CNS (hypothalamus, brain stem, cerebellum, fro

SUBMITTER: Svane N 

PROVIDER: S-EPMC11523665 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature