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Papers of the Week
Regional distribution of unbound eletriptan and sumatriptan in the CNS and PNS in rats: implications for a potential central action.
Authors
Svane N, Bällgren F, Ginosyan A, Kristensen M, Brodin B, Loryan IAbstract
Triptans are potent 5-HT 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 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 receptor occupancies at clinically relevant concentrations.